Norleual TFA - ≥99% , CAS No.N659268

CAS: N659268 Cat. No.: N659268 Formula: C₄₃H₅₉F₃N₈O₉ Peso molecolare: 888.97

QUALITÀ & PUREZZA ≥99%

Storage

Protected from light,Argon charged,Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC 50 of 3 pM. Norleual TFA is an AT4 receptor antagonist and exhibits potent antiangiogenic activities.

Appearance:Solid

In Vitro:\Norleual TFA at 20 and 50 pM significantly reduces HGF-dependent c-Met and Gab1 phosphorylation. 20 pM Norleual TFA dramatically reduces HGF-initiated association between Gab1 and c-Met in HEK293 cells. Norleual TFA markedly attenuates HGF-dependent c-Me

In Vivo:Norleual TFA (50 μg/kg; intraperitoneal injection; daily; for 2 weeks; C57BL/6 mice) suppresses pulmonary colonization by B16-F10 murine melanoma cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Biological Activity:Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC 50 of 3 pM. Norleual TFA is an AT4 receptor antagonist and exhibits potent antiangiogenic activities.

Specifiche

Specifiche e purezza

≥99%

Condizioni di conservazione di stoccaggio

Protected from light,Argon charged,Desiccated,Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

ANTAGONIST

Purezza

≥99%

Nomi e identificatori

Peso molecolare

888.97

Application Protocols

No validated, item-specific application protocols are provided for Norleual TFA (SKU N659268).

• General guidance for solution preparation (informational; verify for your lot):

  • Bring vial to room temperature in a desiccator before opening to prevent moisture condensation.
  • Prepare a concentrated stock in an appropriate solvent (commonly anhydrous DMSO), then dilute into assay buffer with mixing to avoid precipitation.
  • Filter sterilize (0.22 µm) if sterility is required and the compound is stable; avoid adsorption by pre-rinsing the filter with solvent/buffer.

• Controls and documentation:

  • Include vehicle controls for any organic co-solvents.
  • Record lot number, concentration by mass, purity adjustment, counter-ion content (if known), and final assay conditions.

• For analytical methods:

  • LC–MS using water/acetonitrile with 0.1% formic acid is generally compatible; TFA can be used for improved chromatographic performance but may suppress MS signal.

Please consult the CoA/Spec Sheet for any lot-specific recommendations or example protocols once available.

Biological Roles

No specific biological role, target, or mechanism has been provided for Norleual TFA (SKU N659268). The following general information pertains to peptide/peptidomimetic research compounds and should not be taken as item-specific claims.

• General context (informational):

  • Peptidomimetics are commonly explored as ligands for enzymes, transporters, and receptors, leveraging side-chain topology and backbone geometry resembling natural peptides while potentially enhancing stability.
  • The presence of leucine/norleucine-like aliphatic side chains (as suggested by the conventional name “Norleual”) typically increases hydrophobic character, which can influence membrane association, binding pockets preference, and solubility.

• Experimental use-cases:

  • Structure–activity relationship (SAR) studies to delineate the contribution of aliphatic residues to binding affinity.
  • Probe development for pathway interrogation in cell-free or cellular assays, under strictly research-use conditions.

• Assay considerations:

  • TFA counter-ion can impact assay pH and ionic strength; precondition solutions or exchange counter-ions if biological sensitivity demands it.
  • Adsorptive losses to plastics can occur for hydrophobic/peptidic analytes; use low-bind plastics or glassware, include carrier proteins (e.g., 0.1% BSA) where appropriate, and validate recovery.

• Data integrity:

  • Confirm identity and purity for each lot by orthogonal methods (HPLC, MS, elemental/counter-ion analysis) before interpreting biological results, as minor impurities or variable salt content can confound outcomes.

For any definitive biological roles or targets of this specific item, consult the CoA/Spec Sheet and supporting literature once the exact structure is confirmed.

Buffer Applications

This product is not a buffering agent and is not typically used to prepare laboratory buffers.

• Practical note:

  • If dissolving the compound for assays, select a compatible buffer (e.g., PBS, HEPES, or assay-specific media) based on your biological system. Optimize pH/ionic strength to maintain the compound in solution and preserve activity.
  • Avoid assuming compatibility with any given buffer; confirm stability and solubility empirically for your specific lot.

• Item-specific buffer recipes or pKa values: Not specified for this item; refer to CoA/Spec Sheet if provided.

Green Alternatives

While Norleual TFA is a discrete research compound (not a solvent or bulk reagent), greener practices focus on solvent choice, counter-ion management, and waste minimization.

• Solvent selection (general guidance):

  • Prefer water or aqueous buffers whenever feasible. Use minimal DMSO seed stocks and dilute promptly to reduce organic solvent use.
  • For chromatographic workups, consider formic acid (FA) over TFA for LC–MS compatibility and reduced ion-pair persistence, acknowledging that TFA can improve chromatographic peak shape for hydrophobic peptides.

• Counter-ion considerations:

  • TFA contributes to fluorinated waste. If compatible with your assays, exchange TFA for acetate, hydrochloride, or formate via desalting/SPE, reducing persistent fluorinated residues in waste streams.

• Process and analytical choices:

  • Employ micro-scale assays and low-volume LC to reduce solvent consumption.
  • Favor acetonitrile recovery/reuse where permitted; optimize gradients to shorten runs and cut solvent.

• Example comparison (general; not item-specific):

  • TFA vs FA in RP-HPLC:
    • TFA: better peak shape/hydrophobic retention; can suppress MS signal; generates fluorinated waste.
    • FA: MS-friendly, greener profile; may give broader peaks for some peptides; often adequate at 0.1%.

• Packaging/handling:

  • Maintain desiccated, argon atmosphere and subdivide into single-use aliquots to minimize repeated thaw/solvent use and reduce material loss.

Adopt institutionally approved green-chemistry practices and assess alternatives based on assay tolerance and data quality.

Pharmaceutical Uses

No pharmaceutical-grade designation, pharmacopeial monograph, or excipient/processing role is provided for Norleual TFA (SKU N659268).

• Research-only status:

  • Labeled “For research use only.” Not for human or veterinary use, clinical diagnostics, or therapeutic applications.

• General context (informational):

  • Peptide/peptidomimetic TFA salts are often encountered at discovery stage as tool compounds or reference standards. Transition to development typically necessitates counter-ion exchange (e.g., acetate, hydrochloride) and strict control of residual solvents, TFA levels, and peptide content (mass-by-assay).

• If considering formulation research (non-clinical):

  • Establish solubility in candidate vehicles (aqueous, co-solvent, lipidic) and quantify TFA stoichiometry.
  • Assess stability under intended storage and use conditions (pH, temperature, light). Implement forced-degradation studies to design stability-indicating analytical methods.

• Regulatory note:

  • Any use beyond basic research requires comprehensive CMC characterization (identity, purity, impurities, counter-ion content) and adherence to applicable regulations; none of these attributes are specified for this item.

Physical Properties

Item-specific physical constants are not provided for this SKU.

• Item-specific values (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.
  • Melting point, boiling point, density, refractive index, UV cutoff, water/peroxide content, metal limits: Not specified for this item; refer to CoA/Spec Sheet.

• Storage-related properties (from Product Data):

  • Storage: Protected from light, argon charged, desiccated, store at −80 °C.
  • Shipping: Dry ice packs + cold packs.

• General/literature expectations for peptide/peptidomimetic TFA salts (informational, not item-specific specs):

  • Physical state: typically white to off-white amorphous solids or lyophilizates; frequently hygroscopic due to the TFA counter-ion.
  • Solubility behavior: often soluble in polar aprotic solvents (DMSO, DMF) and in aqueous buffers depending on sequence and charge state; co-solvent strategies (e.g., DMSO→buffer) are commonly used.
  • pKa/logP: highly sequence-dependent; peptidic species often exhibit multiple ionizable groups and low logP in water; values must be determined experimentally for the specific compound.

• Practical notes (general):

  • Hygroscopicity and TFA content can alter apparent mass; for quantitative work, determine counter-ion content (e.g., by 19F NMR or ion chromatography) and use mass-by-assay or perform neutralization/exchange if required.
  • Avoid extended exposure to ambient humidity and light; use chilled, anhydrous conditions during handling to preserve integrity.

Quality and Grades

• Item-specific grade/purity: Not specified for this item; refer to CoA/Spec Sheet.

• Interpreting grade for peptide/peptidomimetic salts (general guidance):

  • Research grade peptides/peptidomimetics are typically specified by HPLC area purity (e.g., >95% by RP-HPLC at 214/220 nm) and confirmed by MS (ESI/HRMS) and, when relevant, by amino acid analysis or NMR. Without explicit values, no assumption can be made for this SKU.
  • TFA counter-ion: Peptides purified in TFA-containing eluents often contain variable TFA equivalents; this can influence salt mass, solubility, and bioassay readouts. If your application is sensitive to TFA, consider counter-ion exchange (e.g., acetate or HCl) or desalting.

• What to request/verify for this item:

  • Certificate of Analysis with: identity confirmation (MS), chromatographic purity (method and detection wavelength), residual solvents, water content, counter-ion content, and where appropriate, optical rotation and peptide content (mass-by-assay).
  • Batch-to-batch consistency: verify lot-specific purity and salt form; small changes in counter-ion stoichiometry can affect dosing calculations.

• Stabilizers and additives:

  • No stabilizers are listed for this item. If stabilizers are important for your use case (e.g., to prevent oxidation of Met/Nle or other sensitive residues), confirm absence/presence on the CoA.

• Practical tip:

  • For quantitative assays, re-calculate dosing based on lot-specific assay/purity and counter-ion content to achieve accurate molar concentrations.

Reaction and Applications

No specific manufacturer application notes are provided for Norleual TFA (SKU N659268). The following describes typical research applications for peptide/peptidomimetic trifluoroacetate salts (general guidance; not item-specific claims):

• Screening and probe studies:

  • Utilized as tool compounds in biochemical or cell-based assays to explore protein–ligand interactions, receptor engagement, or pathway modulation. Peptidomimetics can provide high target affinity and selectivity profiles worth exploring in early discovery.

• Analytical reference and method development:

  • Employed as reference standards for LC–MS method establishment (e.g., retention behavior of hydrophobic vs hydrophilic peptide motifs; ionization under positive ESI). TFA salts frequently yield strong signals in positive-ion mode; note potential TFA adducts.

• Physicochemical characterization workflows:

  • Counter-ion quantification (19F NMR or ion chromatography), purity profiling by RP-HPLC (C18/C8, water/acetonitrile + 0.1% FA or TFA), and stability-indicating methods (acid/base/oxidative stress) are common.

• Assay design considerations:

  • TFA can interfere with some bioassays (pH, salt effects). If required, perform counter-ion exchange to acetate or HCl via solid-phase extraction or lyophilization from volatile acid media.
  • Hydrophobic sequences may require DMSO seed stocks and staged dilution to avoid precipitation upon buffer addition.

• Not typically used as a reaction solvent or general reagent. If synthetic transformations are desired (e.g., derivatization, labeling), confirm reactive handles (amines, carboxylates) from the item-specific structure before planning chemistry.

Reaction Conditions

This product is not offered as a reagent for named synthetic transformations, and no item-specific reaction conditions are provided.

• General notes (informational for peptidomimetic handling, not item-specific):

  • If derivatization is attempted (e.g., amide coupling, labeling), conduct reactions under inert atmosphere and anhydrous conditions to minimize hydrolysis and side reactions.
  • Typical solvents for peptide couplings include DMF, NMP, or DCM with coupling agents such as HATU/HBTU/EDC and bases like DIPEA; however, applicability depends entirely on the actual functional groups present.
  • Temperature: often 0–25 °C for solution-phase couplings to limit racemization; monitor by LC–MS.

• Critical caveat:

  • Do not proceed with any reaction planning without the definitive structure of Norleual TFA (SKU N659268). Refer to the CoA/Spec Sheet to confirm reactive sites and compatibility.

Safety and Handling

Safety details for this specific item are not provided; consult the product SDS for authoritative guidance.

• Item-specific hazard data (from Product Data):

  • Signal word: Not specified for this item; refer to SDS.
  • H-statements: Not specified for this item; refer to SDS.
  • GHS classification: Not specified for this item; refer to SDS.
  • Pictograms: Not specified for this item; refer to SDS.

• General precautions for peptide/peptidomimetic TFA salts (informational, not item-specific):

  • Potential hazards: may cause irritation to eyes, skin, and respiratory tract; avoid inhalation of dusts and aerosols.
  • PPE: laboratory coat, safety glasses, and suitable disposable gloves; handle powders in a fume hood or ventilated enclosure to minimize inhalation/contamination.
  • Incompatibilities: avoid strong oxidizers and bases that could induce degradation; avoid moisture which can alter salt content and promote hydrolysis.
  • Light sensitivity: follow the provided instruction to protect from light; amber containers or foil wrap recommended during handling and storage.

• First-aid overview (general):

  • Inhalation: move to fresh air; seek medical attention if symptoms persist.
  • Skin/eye contact: rinse with copious water for at least 15 minutes; remove contaminated clothing; seek medical attention as needed.
  • Ingestion: rinse mouth; do not induce vomiting; obtain medical advice.

• Waste disposal (general):

  • Collect solid/solution waste as organic laboratory waste; dispose of according to institutional and local regulations. Always defer to the SDS and institutional EHS policies.

Solvent Selection

This item is expected to behave like a peptide/peptidomimetic TFA salt; exact solubility for SKU N659268 is not specified. Below are general, practical strategies (informational; verify empirically with your lot).

• Polarity profile (general):

  • Peptidic TFA salts are polar and often dissolve in water and polar aprotic solvents (DMSO, DMF). Hydrophobic content of the sequence may necessitate co-solvent systems (DMSO→aqueous buffer).

• Recommended dissolution workflow (general):

  1. Start with high-purity anhydrous DMSO to prepare a concentrated stock (e.g., 10–50 mM).
  2. Dilute into assay buffer while maintaining final DMSO ≤0.1–1% v/v as required by the assay.
  3. If aqueous solubility is low, add minimal acetonitrile or 10–20% v/v ethanol as co-solvent, or adjust pH to favor ionization (if amine/acid groups are present).

• Common solvent choices (general):

  • Water/PBS: suitable for polar sequences; may require gentle warming and sonication.
  • DMSO or DMF: high solvating power; ensure compatibility with downstream Biology/Chemistry.
  • Aqueous buffers with 0.1% TFA or 0.1% formic acid: useful for analytical injections (LC/MS) but may not be suitable for biological assays due to acidity.

• Comparison notes (general):

  • DMSO vs DMF: DMSO is more bio-compatible for small v/v; DMF is excellent for stock preparation but less favored for biological assays.
  • Methanol/ethanol: acceptable co-solvents; monitor stability if acid- or base-labile functionalities may transesterify.

• Do not assume solubility; determine empirically and record concentration by mass and confirmed assay purity.

Storage and Reconstitution

• Item-specific storage (from Product Data):

  • Store at −80 °C.
  • Protect from light.
  • Maintain under argon (argon-charged) and keep desiccated.
  • Shipped on dry ice packs + cold packs to preserve integrity during transit.

• Stability considerations (general for peptide/peptidomimetic TFA salts; not item-specific specifications):

  • Hygroscopic; minimize headspace and exposure to ambient humidity. Light and moisture can promote hydrolysis or side reactions.
  • Recommended to aliquot into single-use portions upon first thaw to avoid repeated freeze–thaw cycles.

• Reconstitution guidance (general):

  • Allow vial to warm to room temperature in a desiccator before opening.
  • For initial dissolution, use anhydrous DMSO or DMF to prepare a concentrated stock (e.g., 10–50 mM), then dilute into assay buffer. If aqueous solubility is adequate, dissolve directly in water or buffer with gentle agitation.
  • Verify concentration by mass and adjust for assay purity/counter-ion content if provided on CoA.

• Working solution handling:

  • Store short-term working stocks at 2–8 °C if chemically stable; for longer-term storage, keep frozen (≤ −20 °C) in tightly sealed, inerted vials. Avoid multiple freeze–thaw cycles.

• Shelf-life and retest:

  • Not specified for this item; refer to CoA/Spec Sheet and perform periodic QC (HPLC/MS) on stored aliquots to confirm integrity over time.

Always defer to the lot-specific CoA and SDS for definitive handling and stability information.

Structure and Identity

Concise overview: Norleual TFA is presented as a research-use small molecule/peptide-like reagent. Detailed structural identifiers for this specific catalog item have not been provided.

• Item-specific identifiers (from Product Data):

  • CAS: N659268 (catalog placeholder)
  • InChIKey: Not specified for this item; refer to CoA/Spec Sheet.
  • SMILES: Not specified for this item; refer to CoA/Spec Sheet.
  • Molecular formula: Not specified for this item; refer to CoA/Spec Sheet.
  • Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.

• Naming notes (general/literature context, not item-specific):

  • “Norleual” is commonly used in the literature to denote a peptide-mimetic motif incorporating norleucine (Nle) and leucine (Leu) residues or related isosteres. The suffix “TFA” indicates the trifluoroacetate salt form, frequently used for peptide and peptidomimetic isolates after RP-HPLC purification with TFA-containing eluents.
  • Without a provided sequence or structure, the exact connectivity, stereochemistry, and presence of any reduced/peptidomimetic linkages (e.g., ψ[CH2–NH]) for this item cannot be confirmed.

• Structural features (general possibilities for “Norleual”-type entities; literature context):

  • Aliphatic side chains (from leucine and/or norleucine), chiral alpha-centers (L-configuration typical in peptide chemistry), amide bonds or amide isosteres, terminal amine/acid or protected termini depending on formulation.

• 2D structure description (item-specific):

  • Not available. Please consult the CoA/Spec Sheet for the definitive structure and identifiers of SKU N659268.

Synthetic Utility

Norleual TFA, as supplied, is intended as a research compound rather than a general-purpose synthetic reagent. Specific reactive handles and functional groups for SKU N659268 are not disclosed; therefore, the following are general considerations for peptide/peptidomimetic salts (informational only):

• Potential functional handles (sequence-dependent):

  • Primary/secondary amines, carboxylic acids, alcohols, or protected termini suitable for conjugation (e.g., NHS ester coupling, carbodiimide-mediated amidation, click chemistry if azide/alkyne tags are present). Presence/absence of these must be confirmed from the item’s structure.

• Utility scenarios:

  • Preparation of labeled analogs for assay readout (fluorophores, biotin) after verification of available functional groups.
  • Solid-support immobilization for affinity studies, provided there is a defined conjugation site away from the pharmacophore.

• Constraints:

  • TFA counter-ion can complicate coupling reactions and downstream analytics; exchange to a different counter-ion or free base/acid form when necessary.
  • Protect sensitive residues from oxidation or epimerization; perform reactions under inert atmosphere as already indicated for storage.

• Verification:

  • Prior to any derivatization, obtain the exact structure and purity profile from the CoA/Spec Sheet and confirm with analytical data (HPLC, MS, where applicable NMR). Without these details, synthetic planning cannot be reliably executed.

Target Specificity

No target, binding partner, or specificity information is provided for Norleual TFA (SKU N659268).

• Item-specific target data: Not specified for this item; refer to CoA/Spec Sheet and any associated technical notes.

• General note:

  • If used as a tool compound in screening, determine target engagement empirically via appropriate biochemical/biophysical assays (e.g., enzyme kinetics, SPR/ITC, radioligand displacement) and confirm with orthogonal methods. Report conditions, concentrations, and controls alongside results for reproducibility.

Domande frequenti

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?80 °C, protected from light, desiccated, under argon. It is supplied under an argon blanket; reseal under inert gas after each use.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is N659268, the molecular formula is C43H59F3N8O9, and the molecular weight is 888.97 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.