DOTA-JR¹¹, Antagonist of SST 2 receptor, CAS No.rp173896, Antagonist of SST 2 receptor

CAS: rp173896 Cat. No.: rp173896
Disponibile su ordine
GRADE & PURITY Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.
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Size
Germania (EU)
USA*
Price
Qty
500μg
rp173896-500μg
Su ordinazione · 8–12 settimane
2.082,49€
1mg
rp173896-1mg
Su ordinazione · 8–12 settimane
3.470,87€
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Why this grade

Moligand™ Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Room temperature Ships Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Specifications

Product Name
DOTA-JR¹¹, Antagonist of SST 2 receptor, CAS No.rp173896
Grado
Moligand™
Specifiche e purezza
Moligand™
Tipo di azione
ANTAGONIST
Meccanismo d'azione
Antagonist of SST 2 receptor
CAS
rp173896
Tipo di molecola
Peptidi
Product Line
Prodotti biologici
Stoccaggio e spedizione
Condizioni di conservazione di stoccaggio
Room temperature

Documentazione

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

Download SDS →

✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

Look up COA →

📊 Datasheet

Quick-reference summary of product specifications and applications.

View datasheet →

🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Obiettivi associati (umani)
SSTR2 Tclin Somatostatin receptor type 2 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Certificati (CoA, COO, BSE/TSE e tabella di analisi)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Informazioni genetiche
Reference
  • 1. Kinetics and inhibition of recombinant human cystathionine gamma-lyase. Toward the rational control of transsulfuration., The Journal of biological chemistry, Steegborn, C C and 7 more authors.
  • 2. Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences., Proceedings of the National Academy of Sciences of the United States of America, Strausberg, Robert L RL and 83 more authors.
  • 3. Genomic basis of cystathioninuria (MIM 219500) revealed by multiple mutations in cystathionine gamma-lyase (CTH)., Human genetics, Wang, Jian J and Hegele, Robert A RA.
  • 4. Cloning and nucleotide sequence of human liver cDNA encoding for cystathionine gamma-lyase., Biochemical and biophysical research communications, Lu, Y Y, O'Dowd, B F BF, Orrego, H H and Israel, Y Y.
  • 5. Single nucleotide polymorphism in CTH associated with variation in plasma homocysteine concentration., Clinical genetics, Wang, J J, Huff, A M AM, Spence, J D JD and Hegele, R A RA.
  • 6. Cystathionine gamma-lyase overexpression inhibits cell proliferation via a H2S-dependent modulation of ERK1/2 phosphorylation and p21Cip/WAK-1., The Journal of biological chemistry, Yang, Guangdong G, Cao, Kun K, Wu, Lingyun L and Wang, Rui R.
  • 7. The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)., Genome research, Gerhard, Daniela S DS and 115 more authors.
  • 8. Towards a proteome-scale map of the human protein-protein interaction network., Nature, Rual, Jean-François JF and 37 more authors.
  • 9. The DNA sequence and biological annotation of human chromosome 1., Nature, Gregory, S G SG and 178 more authors.
  • 10. Polymorphisms in one-carbon metabolism and trans-sulfuration pathway genes and susceptibility to bladder cancer., International journal of cancer, Moore, Lee E LE and 14 more authors. more
Calcolatori di soluzioni
Recensioni

Recensioni dei clienti

Application Protocols
  • Item-specific: No tested applications or in‑house protocols are provided for SKU rp173896.

  • General starting points (not item-specific; adapt and validate):

    • Stock solution: Prepare 10 mM in metal‑free water or DMSO; verify complete dissolution. Filter (0.22 µm) if using in cell‑free binding assays.
    • Metal loading (analytical scale): Dissolve ligand to 100 µM in 0.2 M sodium acetate, pH 4.5. Add 1.2 equiv metal salt (e.g., GaCl3). Incubate 15–30 min at 50 °C. Quench with buffer or dilute; analyze by LC‑MS/HPLC.
    • Purification: RP‑SPE wash with water, elute with 20–40% acetonitrile in water (0.1% TFA or formic acid if compatible), or perform analytical/semiprep HPLC.
    • Storage of solutions: Aliquot and store chilled if needed; avoid repeated freeze–thaw. See Storage & Reconstitution for item‑specific storage.
  • Reminder: These are literature‑style generic procedures for DOTA‑type ligands and are not validated for this SKU. Optimize conditions for your system and consult the item’s CoA/Spec Sheet before critical experiments.

Biological Roles
  • Item-specific: No biological role or target information is provided for SKU rp173896.

  • Literature/general context (not item-specific):

    • DOTA is a coordination cage used to attach metal ions to biomolecules, enabling biochemical tracking, assay readouts, and affinity studies. When conjugated to a targeting motif (e.g., a peptide often abbreviated “JR11” in publications), the construct can serve as a molecular probe in vitro to interrogate binding phenomena.
    • In biological media, charge state and hydrophilicity govern nonspecific binding and cellular uptake; DOTA generally increases hydrophilicity and can reduce membrane permeability, which may be advantageous for surface‑receptor binding assays.
    • Metal‑loaded forms can be used as elemental tags for ICP‑MS readouts or as surrogates for optimizing labeling and purification workflows prior to specialized detection.
  • Caution:

    • No medical or clinical claims apply to this catalog item. Any references to targeting motifs or receptors are provided as general literature background only; confirm the actual target and composition of DOTA‑JR¹¹ for this SKU from the CoA/Spec Sheet.
Buffer Applications
  • Applicability to this item: DOTA‑conjugated ligands are not used as buffering agents. Therefore, classical buffer system design (pH capacity, ionic strength) does not apply directly.

  • Literature/general notes for handling (not item-specific):

    • Common buffers for metal complexation include acetate (0.1–1.0 M, pH 4.0–5.5) and MES (pH 5.5–6.5). Avoid phosphate when labeling certain metals that form insoluble phosphates.
    • For biological binding assays, HEPES or PBS (metal‑reduced) can be used for incubation/wash steps once labeling is complete. Exclude competing chelators (e.g., EDTA) during metal loading.
  • Item-specific buffer recommendations: Not specified for this item; refer to CoA/Spec Sheet and your assay’s requirements.

Green Alternatives
  • Context: DOTA‑conjugated ligands are typically handled in water or benign polar solvents; thus, their workflows can already align with green chemistry principles.

  • Literature/general guidance:

    • Prefer aqueous buffers over high‑boiling polar aprotics when feasible. Use DMSO only for stock solutions and minimize final assay concentrations (<1–2% v/v) to reduce solvent burden.
    • Employ room‑temperature labeling where kinetics permit; consider microwave‑free thermal profiles to save energy.
    • Adopt metal‑free, reusable plasticware where compatible, and avoid excessive acid/base neutralizations by choosing buffering systems with minimal waste.
  • Comparison (general):

    • Aqueous acetate/citrate buffers (pH 4–6): renewable, low toxicity, easy disposal compared with DMF/DMAC.
    • Ethanol/water cosolvent: greener alternative to acetonitrile for some purifications or preparative HPLC gradients (when compatible with stationary phase and analyte stability).
  • Trade‑offs:

    • Highly aqueous systems may slow some conjugation reactions; adding minimal DMSO or switching to water‑miscible green solvents (e.g., glycerol carbonate, propylene carbonate) can help but may affect metal chelation.
    • Avoid chelating additives such as EDTA in wash buffers during labeling, as they compete with DOTA and increase waste complexity.
  • Item-specific green notes: Not specified for this item; refer to internal method development and the CoA/Spec Sheet for compatibility guidance.

Pharmaceutical Uses
  • Item-specific: No pharmacopeial status, excipient role, or formulation guidance is provided for SKU rp173896.

  • Research‑only note: For research use only. Not for human or veterinary use, diagnostics, or clinical applications.

  • Literature/general background (not item-specific):

    • DOTA‑based chelators are widely explored in preclinical research to attach metals to biomolecules for imaging probe development and analytical tagging. In formulation research, salt form (e.g., TFA vs acetate) and counter‑ion content can influence solubility and adsorption to plastics.
    • If formulating for in vitro assays, typical vehicles include metal‑reduced saline or HEPES buffer with trace polysorbate to mitigate surface adsorption, verifying that surfactants do not interfere with binding.
  • Compliance reminder: Any GMP, ICH, or pharmacopeial attributes (residual solvents, bioburden/endotoxin, elemental impurities) are not specified for this catalog item; consult CoA/Spec Sheet if such attributes are required for your workflow.

Physical Properties
  • Item-specific (from Product Data):

    • Appearance: Not specified for this item; refer to CoA/Spec Sheet.
    • Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
    • Other specifications (bp/mp, density, UV cutoff, water/peroxide/metals): Not specified for this item; refer to CoA/Spec Sheet.
  • Literature/general expectations for DOTA–conjugated ligands (not item-specific):

    • Physical state: usually solid (amorphous or lyophilized) with high hygroscopicity due to multiple carboxylates and amines.
    • Solubility: high in water and aqueous buffers (especially when deprotonated or as salts); readily soluble in polar aprotic solvents such as DMSO; limited solubility in nonpolar organics.
    • Acid–base behavior: multiple basic nitrogens (macrocycle) and acidic carboxylates; overall charge state is pH‑dependent. Metal complexation is favored in mildly acidic buffers (e.g., acetate, pH ~4–5) for many trivalent radiometals (literature).
    • LogP: typically strongly negative for free DOTA conjugates (literature), reflecting hydrophilicity.
    • UV characteristics: peptide‑containing conjugates may show peptide bond π→π* absorption at ~214–220 nm and, if aromatic residues/linkers are present, additional bands near 254–280 nm (literature). Exact extinction coefficients are conjugate‑specific.
  • Important: Do not treat the above as specifications. Verify actual values for SKU rp173896 from the CoA/Spec Sheet prior to experimental design.

Quality and Grades
  • Item-specific (from Product Data):

    • Grade/Purity: Moligand™.
    • Additional purity details (assay, residual solvents, metals, water, counter‑ion content): Not specified for this item; refer to CoA/Spec Sheet.
  • Interpretation and practical guidance (general):

    • Moligand™ indicates inclusion in a small‑molecule/ligand library suitable for research screening and discovery workflows. Such items are typically intended for in vitro research, assay development, and structure–activity studies, not for clinical use.
    • For chelator‑bearing ligands, quality considerations often include: identity confirmation (HRMS/NMR), purity by HPLC, residual solvent profile, and counter‑ion specification (e.g., trifluoroacetate vs acetate). These parameters affect solubility, assay background, and metal‑binding performance.
    • If you require low‑metal or metal‑free material for chelation studies, request the specific metals specification and test method from the CoA. For UV‑sensitive analytics (HPLC/UPLC), low baseline absorbance of excipients and defined salt form are advantageous.
  • Recommendations:

    • Obtain and review the CoA/Spec Sheet for this SKU prior to regulated or quantitative work.
    • If consistency across lots is critical (e.g., screening campaigns), consider reserving a single lot and documenting reconstitution and storage conditions to minimize variability.
Reaction and Applications
  • Item-specific manufacturer applications: Not provided in Product Data.

  • Literature/general applications for DOTA‑bearing ligand constructs (not item-specific):

    • Metal complexation: DOTA forms highly stable complexes with trivalent and divalent hard metal ions (e.g., Ga3+, Lu3+, Y3+, In3+, Cu2+), used to generate defined metal–ligand complexes for analytical, imaging probe development, and materials research.
    • Conjugation chemistry: DOTA can be installed via amide coupling, click chemistry, or thiol–maleimide strategies onto targeting motifs. Resulting conjugates serve in affinity capture, receptor binding studies, or as metal–tagged tracers in in vitro assays.
    • Assay utilities: DOTA–metal complexes can be applied as nonradioactive surrogates (e.g., natLu, natGa) for method development, ICP‑MS quantification, or TR‑ICP workflows.
    • Separation science: metal‑tagging can facilitate mass‑tag encoding of ligands for multiplexed screening using elemental detection.
  • Practical tips:

    • Use metal‑free reagents, plasticware, and chelex‑treated buffers to minimize background metals.
    • Verify pH and buffer composition; acetate (0.1–1.0 M, pH 4–5.5) is commonly employed for many trivalent ions (literature).
    • Following complexation, apply rapid purification (SPE/HPLC) to remove unbound metal and buffer salts; confirm complex formation by LC‑MS and, where applicable, radio‑iTLC or HPLC with appropriate detectors.
  • Note: Specific reactivity and conditions for SKU rp173896 must be confirmed experimentally; see Reaction Conditions for literature benchmarks.

Reaction Conditions
  • Item-specific: No tested conditions are provided for SKU rp173896; validate empirically.

  • Literature/general labeling conditions for DOTA chelation (not item-specific; typical ranges):

    • Metals: Ga3+, Lu3+, Y3+, In3+, Cu2+ among others.
    • Buffer: Sodium acetate (0.1–1.0 M), pH 4.0–5.5 for many trivalent metals; for Cu2+, ammonium acetate or MES at pH ~5–6 is common.
    • Temperature/time: 25–95 °C, 5–60 min depending on metal and ligand architecture; Ga3+ often labels efficiently at 25–60 °C, while Lu3+/Y3+ may require 60–95 °C (literature).
    • Stoichiometry: 1.0–1.5 equivalents of metal per ligand; excess metal can expedite kinetics but must be removed post‑labeling.
    • Concentration: 10–500 µM ligand typical in small‑scale labeling; higher concentrations can promote aggregation for some peptides—optimize as needed.
    • Purification: SPE (cation exchange or RP) or semi‑prep HPLC. Assess radiochemical/chemical purity by HPLC, iTLC, or LC‑MS.
  • Conjugation (if further derivatization is needed):

    • Amide couplings: EDC/NHS or HATU in aqueous‑compatible mixed solvents (water/DMSO or DMF) at pH 7–8 for carboxylate activation; control for hydrolysis.
    • Click reactions: CuAAC under ligand‑assisted copper catalysis; remove copper thoroughly to protect downstream chelation.
  • Notes:

    • Exclude competing chelators (EDTA, citrate in excess) during metal loading.
    • Validate pH precisely; small deviations can markedly affect chelation kinetics and yield.
Safety and Handling
  • Item-specific (from Product Data):

    • GHS Classification: Not specified for this item; refer to SDS.
    • Signal Word: Not specified for this item; refer to SDS.
    • H‑Statements/Pictograms: Not specified for this item; refer to SDS.
    • Storage conditions: Room temperature (per Product Data).
  • General laboratory safety (literature/general):

    • PPE: wear lab coat, gloves (nitrile), and safety glasses. Handle powders in a fume hood to minimize inhalation of particulates and exposure to dust.
    • Hygiene: avoid ingestion and contact with skin/eyes; wash thoroughly after handling. Prevent cross‑contamination if using for high‑sensitivity binding/chelation experiments.
    • Incompatibilities: strong oxidants and strong mineral acids/bases may degrade peptide or linker motifs; avoid metal‑contaminated glassware if trace‑metal–free conditions are required (e.g., radiometal labeling). Use metal‑free plasticware when chelation performance is critical.
    • Special risks: polyaminocarboxylate chelators can sequester metal ions; avoid contact with essential metal salts and supplements in shared spaces. For radiometal studies, follow institutional radiation safety procedures (if applicable to your lab; not part of this product’s specification).
    • First‑aid overview: if inhaled—move to fresh air; if on skin—wash with soap and water; if in eyes—rinse cautiously with water for several minutes; if ingested—rinse mouth and seek medical advice. Always consult the SDS for authoritative guidance.
  • Disposal: follow local regulations; aqueous solutions may require chelation‑aware waste handling due to potential for mobilizing metals.

Solvent Selection
  • Item-specific: No solvent recommendations are specified for this item; consult the CoA/Spec Sheet.

  • Literature/general guidance for DOTA‑conjugated ligands:

    • Primary choices: water, aqueous buffers (e.g., acetate, citrate, phosphate), and DMSO for stock solutions. The DOTA domain confers high polarity; peptide/linker composition modulates solubility.
    • Working concentrations: 1–10 mM stocks are commonly prepared in DMSO or water depending on hydrophilicity; filter‑sterilize if necessary for biological assays (0.22 µm).
    • pH considerations: deprotonation of carboxylates improves solubility in basic media; however, for metal complexation, mildly acidic buffers (pH ~4–5) are typical to favor complexation kinetics (literature).
    • Avoid: alcohols/ketones with residual metal content if performing high‑affinity chelation; nonpolar solvents generally give poor solubility.
  • Small comparison (literature):

    • Water/buffer: best for bioassays and chelation; controllable pH and ionic strength.
    • DMSO: excellent for concentrated stocks and cosolvent use up to 1–2% v/v in assays; ensure compatibility with assay components.
    • DMF: alternative polar aprotic solvent; consider residual metal content and potential for aminolysis with activated linkers.
  • Tip: Pre‑rinse vials with metal‑free water or acid‑washed to minimize adventitious metals before chelation experiments.

Storage and Reconstitution
  • Item-specific (from Product Data):

    • Storage conditions: Room temperature.
    • Shipped in: Not specified for this item; refer to CoA/Spec Sheet.
    • Appearance/physical form: Not specified for this item; refer to CoA/Spec Sheet.
  • Reconstitution (general guidance; not item-specific):

    • For solid materials, allow the container to equilibrate to room temperature in a desiccator before opening to minimize moisture uptake.
    • Prepare concentrated stocks in metal‑free water or DMSO. Typical research stocks: 1–10 mM. Record exact solvent, concentration, and date.
    • If using aqueous buffers, choose metal‑reduced, chelator‑free solutions to preserve chelation capacity.
  • Solution stability (general):

    • Aqueous solutions of DOTA‑conjugates are usually stable for hours to days at 2–8 °C; for longer storage, aliquot and freeze (−20 to −80 °C) to avoid microbial growth and degradation. Avoid multiple freeze–thaw cycles by using single‑use aliquots.
    • Protect from adventitious metals if the apo‑ligand is to be stored; use plasticware verified to be metal‑free.
  • Documentation:

    • Because detailed specifications are not provided in the Product Data, consult the CoA/Spec Sheet for the exact salt form, counter‑ion, and any stabilizers, and adjust storage and reconstitution accordingly.
  • Research Use Note: For research use only.

Structure and Identity
  • Item-specific (from Product Data):

    • Product name: DOTA-JR¹¹ (SKU: rp173896)
    • CAS: rp173896 (internal)
    • Molecular formula: Not specified for this item; refer to CoA/Spec Sheet.
    • Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
    • SMILES: Not specified for this item; refer to CoA/Spec Sheet.
    • InChIKey: Not specified for this item; refer to CoA/Spec Sheet.
  • Literature/general context (not item-specific):

    • “DOTA–JR11” in the literature typically denotes a bifunctional chelator–ligand construct in which a macrocyclic tetraazacyclododecane tetraacetic acid (DOTA) is conjugated to a peptide or peptidomimetic motif (often denoted JR11). DOTA is a 12‑membered tetraaza macrocycle bearing four pendant acetate arms capable of octadentate binding to hard trivalent/di‑valent metal ions.
    • Structural features of a generic DOTA–ligand conjugate include: a saturated macrocyclic ring (1,4,7,10‑tetraazacyclododecane), four carboxylates (as acids or salts), and a linker to the targeting motif. The conjugate is typically highly polar, zwitterionic/anion at neutral pH, and amenable to aqueous handling.
    • 2D description (generic): central 12‑membered tertiary amine ring (four tertiary nitrogens) with –CH2CO2H arms at 1,4,7,10 positions; one nitrogen or a pendant arm bears a linker to the JR11 moiety.
  • Note: Because no structure identifiers are supplied in the Product Data, all structure‑level properties for this catalog item must be confirmed from the item’s CoA/Spec Sheet prior to use.

Synthetic Utility
  • Item-specific: Structural details enabling specific synthetic transformations are not supplied; consult the CoA/Spec Sheet.

  • Literature/general utility of DOTA‑functionalized ligands (not item-specific):

    • Chelation platform: DOTA’s octadentate coordination allows formation of kinetically inert complexes with many hard metal ions. This provides a modular handle to introduce metals onto targeting ligands for downstream applications (analytical probes, tags).
    • Conjugation hub: Free amine or carboxylate handles on the ligand/peptide enable amide formation (HATU/EDC/NHS strategies), CuAAC “click” reactions (if azide/alkyne handles are present), or thiol–maleimide linkages (for cysteine‑containing motifs).
    • Orthogonality: DOTA’s chelation chemistry is largely orthogonal to many bioconjugation reactions, allowing “label then conjugate” or “conjugate then label” workflows.
    • Purification leverage: The high polarity of DOTA‑bearing constructs facilitates RP‑HPLC purification with aqueous gradients and can reduce co‑elution with hydrophobic impurities.
  • Practical considerations:

    • Protect functional groups judiciously to prevent intramolecular chelation during coupling steps; use buffered conditions and avoid strong bases that can induce lactamization or hydrolysis.
    • Characterization: LC‑MS with metal adduct analysis, HRMS for isotope patterns of metal complexes, and analytical HPLC for purity. Metal‑binding can shift retention times and mass; characterize both apo‑ and metal‑loaded forms as needed.
Target Specificity
  • Item-specific: Not specified for this item; refer to CoA/Spec Sheet.

  • Clarification: No antigen, receptor, clone, isotype, or species reactivity information is provided in the Product Data for SKU rp173896. Any target associations found in external literature for similarly named constructs should not be inferred to this catalog item without verification.

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