Bezeparsen , CAS No.2639640-84-7

CAS: 2639640-84-7 Cat. No.: B1440997 Formula: C₂₃₈H₃₃₅N₆₇O₁₁₃P₁₆S₁₅ Molecular Weight: 6919.13

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

Bezeparsen is a PCSK9 synthesis inhibitor.

Specifications

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• Molecular Weight: 6919.13

Application Protocols

• Item-specific validated applications and dilutions: Not specified for this item; refer to CoA/Spec Sheet.

• General guidance (not item-specific; examples only)

  • Stock preparation: If soluble, prepare a concentrated sterile stock (e.g., in nuclease-free water or DMSO as appropriate), filter through 0.22 µm if compatible, and aliquot for single use.
  • Cell-based studies: Titrate across a broad range (e.g., 0.1–50 µM for small molecules; 1–100 nM for oligonucleotide-like reagents) to establish a response curve; include vehicle-only controls and cytotoxicity counterscreens.
  • Nucleic-acid workflows (if applicable): For oligo-like materials, use RNase/DNase-free disposables. For transfection, follow the reagent manufacturer’s protocol and optimize dose and timing for the chosen cell type.
  • Analytical verification: Confirm identity/purity by LC–MS/HPLC prior to critical experiments; re-check after storage or conjugation.

• Important

  • The above are general research practices and not validated protocols for this SKU. Consult the CoA or contact Technical Support for lot-specific recommendations.

Biological Roles

• Item-specific biological targets or pathways: Not specified for this item; refer to CoA/Spec Sheet.

• General context (not item-specific)

  • Small molecules: often function as ligands or modulators of enzymes/receptors in cell-based assays; their roles are highly scaffold- and substitution-dependent.
  • Oligonucleotide-based reagents (if applicable): can modulate gene expression through Watson–Crick base pairing with target RNA. Two common mechanisms are RNase H-mediated degradation of RNA in RNA–DNA hybrids and steric-blocking of splicing or translation when endonuclease recruitment is not desired.
  • Chemical modifications (e.g., phosphorothioate linkages, 2′-O-alkyl sugars) are frequently used in research oligonucleotides to alter nuclease resistance, binding affinity, and biodistribution; confirm presence/absence via CoA.

• Experimental considerations

  • Verify sequence/structure and purity, then titrate concentration to define potency ranges and off-target windows in the intended cell line or system.
  • Monitor on-target engagement using qPCR, RT–PCR splice assays, or reporter systems, paired with cytotoxicity controls.
  • For uptake studies, consider delivery aids (lipid transfection, gymnotic uptake in select cell types) while controlling for vehicle effects.

• Important caveat

  • No therapeutic or clinical uses are claimed or implied. This product is supplied strictly for research purposes as indicated in the Product Data.

Buffer Applications

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

• General guidance (not item-specific)

  • For small molecules: prepare assay buffers that maintain solubility and target stability; include minimal DMSO and surfactant only if required (e.g., 0.01–0.05% Tween-20).
  • For oligonucleotide-like reagents (if applicable): common working buffers include
    • Nuclease-free water (pH ~6–8)
    • 1× PBS (phosphate 10 mM, 137 mM NaCl, 2.7 mM KCl), pH 7.2–7.6
    • 10 mM HEPES with 100 mM NaCl, pH 7.4
    • TE buffer (10 mM Tris, 1 mM EDTA), pH 7.5–8.0 for storage; EDTA chelates divalent cations that may catalyze degradation
  • Sterile-filter through 0.22 µm PVDF/nylon if sterility is essential and compatible with the molecule.

• Practical tips

  • Avoid repeated freeze–thaw of buffered solutions; prepare aliquots sized for single use.
  • If adsorption losses are suspected, pre-condition plastics with buffer or add carrier (e.g., 0.1 mg/mL non-interfering protein) after confirming assay compatibility.
  • Track pH and ionic strength, as these parameters strongly influence hybridization and stability for nucleic acid-like materials.

Green Alternatives

Because item-specific solvent and hazard data are not provided, consider general greener-practice options appropriate to the working hypothesis of the compound class.

• If preparing small-molecule stocks

  • Prefer aqueous buffers when feasible; use minimal DMSO compatible with the assay.
  • Replace DMF and dichloromethane with safer alternatives (e.g., dimethyl carbonate, 2-MeTHF, Cyrene) when reaction chemistry permits.

• If working with aqueous oligonucleotide materials

  • Use water-based buffers (PBS, HEPES) rather than high-organic systems.
  • Employ ethanol or isopropanol for precipitation/cleanup instead of halogenated solvents where possible.

• Operational green tactics

  • Right-size reaction volumes and employ high-throughput microscale methods to reduce solvent use.
  • Recycle and segregate solvent waste streams; switch to solvent-free or flow methodologies when applicable.

• Comparison snapshot (general, not item-specific)

  • DCM vs 2-MeTHF: 2-MeTHF offers lower toxicity and partial renewability, but different polarity and water miscibility; may require condition re-optimization.
  • DMF vs Cyrene: Cyrene can substitute in some amide-coupling contexts; viscosity and base compatibility differ.
  • High % DMSO vs buffered aqueous: aqueous systems reduce VOC exposure but may limit solubility for hydrophobic chemotypes.

Pharmaceutical Uses

• Item-specific pharmacopeial status or excipient role: Not specified for this item; refer to CoA/Spec Sheet.

• Research/formulation context (general, not item-specific; no therapeutic claims)

  • Small molecules: Preformulation work typically explores solubility (pH–solubility profiles), polymorph screening, and compatibility with excipients; enabling formulations may use cyclodextrins, lipid vehicles, or buffered cosolvents for in vitro/in vivo research.
  • Oligonucleotide-like agents (if applicable): Research formulations often employ isotonic saline or buffered saline, with optional stabilizers (e.g., sugars like sucrose or trehalose) for lyophilized storage. Sequence/backbone dictate ionic interactions and viscosity.

• Analytical controls

  • Establish stability-indicating methods (LC–MS, ion-pair HPLC for oligos, or capillary electrophoresis) and define storage conditions through accelerated stability studies.

• Regulatory note

  • This product is labeled for research use only. It is not intended for human or veterinary use, diagnostic procedures, or as an Active Pharmaceutical Ingredient. No compliance with pharmacopeial monographs is implied unless explicitly stated on the CoA.

Physical Properties

• Item-specific properties (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.
  • Molecular formula: Not specified for this item; refer to CoA/Spec Sheet.
  • Melting point: Not specified for this item; refer to CoA/Spec Sheet.
  • Boiling point: Not specified for this item; refer to CoA/Spec Sheet.
  • Density: Not specified for this item; refer to CoA/Spec Sheet.
  • Refractive index: Not specified for this item; refer to CoA/Spec Sheet.
  • LogP/logD: Not specified for this item; refer to CoA/Spec Sheet.
  • Solubility: Not specified for this item; refer to CoA/Spec Sheet.

• Guidance for planning (general/literature, not item-specific)

  • If Bezeparsen is supplied as a research small molecule, solubility screening typically begins with DMSO (analytical grade), followed by aqueous cosolvent systems (e.g., 10–50% v/v DMSO in water or buffer) and volatile organics (MeOH, ACN) for stock solutions.
  • If it is an oligonucleotide-based entity (nomenclature suggests this possibility but is not confirmed here), it would more typically be supplied as a lyophilized solid or aqueous concentrate, readily soluble in nuclease-free water and common biological buffers (e.g., PBS, HEPES), and insoluble in most nonpolar organics.

• Recommendations

  • Verify exact solubility and any pH-dependent behavior on the CoA/Spec Sheet before committing to formulation, stock preparation, or plate-format dispensing.
  • When property values are absent, run a small-scale solubility panel and record conditions (solvent, pH, ionic strength, temperature) for reproducibility.

Quality & Grades

• Item-specific grade/purity

  • Grade/Purity: Not specified for this item; refer to CoA/Spec Sheet.

• How to interpret grade (general guidance)

  • For small molecules: Typical research grades include “research grade,” “>95%” by HPLC/GC, or specified chromatographic purity with NMR/LC–MS identity confirmation. Low UV-absorbance or “HPLC grade” refers to solvents/reagents optimized for chromatography, not applicable unless stated.
  • For sequence-defined biomolecules (if applicable): Purity is commonly denoted as “desalted,” “cartridge-purified,” “HPLC-purified,” or by PAGE, with identity confirmed by LC–MS and sequence verified. Additional attributes may include counterion (e.g., Na+), residual solvent, water content, and endotoxin/bioburden for certain workflows.

• Documentation expected on request

  • CoA with batch-specific purity method and result, identity data (NMR/LC–MS or sequence mass), residual solvents, water content (Karl Fischer if applicable), and storage guidance.
  • For plate-format libraries: well map, concentration, solvent matrix, and barcode mapping.

• Practical tips

  • If working under regulated settings or performing quantitative biology, request analytical traces (chromatogram, mass spectrum) and method details to understand co-eluting impurities and to ensure compatibility with downstream assays (e.g., UV interference, LC–MS ion suppression).

Reaction & Applications

• Item-specific manufacturer applications: Not provided in Product Data.

• General research applications (not item-specific)

  • If Bezeparsen is a conventional small molecule: may be used in screening libraries, target validation, and SAR studies. Operations include stock solution preparation, plate dispensing, and analytical method development (LC–MS/MS quantitation, stability indicating assays).
  • If Bezeparsen is an oligonucleotide-like reagent (nomenclature suggests this possibility; confirm via CoA): commonly employed in gene knockdown or splice-switching research, RNA–DNA hybridization assays, and biochemical pull-downs when equipped with a tag or handle.

• Conjugation and labeling (general)

  • Amine-, thiol-, or azide-modified sequences can be coupled to small molecules, fluorophores, or affinity tags via NHS ester coupling, maleimide–thiol addition, or CuAAC/SPAAC click chemistry. Reaction conditions should be aqueous-compatible (pH 6.5–8.5) and oxygen-controlled for thiol chemistry.

• Practical considerations

  • Validate integrity by LC–MS or analytical HPLC before and after manipulations.
  • For cellular assays, pre-wet plastics with buffer containing carrier (e.g., 0.1 mg/mL BSA) if nonspecific adsorption is suspected; verify that carriers do not interfere with readouts.
  • Conduct preliminary stability studies (e.g., in buffer, serum, or at intended incubation temperatures) to bracket assay conditions and timelines.

Reaction Conditions

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

• General conditions (not item-specific)

  • Small-molecule derivatizations
    • Amidation/acylation: amine + NHS ester in DMF/DMSO or aqueous buffer (pH 7.5–8.5) with base (e.g., DIPEA) at RT–40°C, 0.5–4 h.
    • Click chemistry (CuAAC): azide + alkyne with CuSO4/sodium ascorbate and TBTA ligand in t-BuOH/H2O (1:1) at RT, 1–4 h; for biological contexts, consider SPAAC (DBCO–azide) in aqueous buffer with no copper.
  • Oligonucleotide conjugations
    • Amine-modified oligo + NHS ester dye: 50–100 mM sodium bicarbonate, pH 8.3, RT, 1–2 h; purify by desalting/HPLC.
    • Thiol-modified oligo + maleimide: pH 6.8–7.2 phosphate buffer, RT, 1–2 h under inert atmosphere; avoid excess base to suppress thiol oxidation.

• Analytical follow-up

  • Monitor reactions by LC–MS or ion-pair HPLC (for oligos), or by analytical HPLC/UPLC (for small molecules). Confirm removal of copper or other catalysts if used.

• Yield expectations

  • Highly method- and substrate-dependent; pilot 0.1–1 µmol reactions are recommended to optimize stoichiometry, pH, and time before scale-up. All values above are general literature guidance and not specifications for this item.

Safety & Handling

• Hazard classification (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/pictograms: Not specified for this item; refer to SDS.

• General laboratory precautions (not item-specific; follow SDS/CoA)

  • Use standard PPE: lab coat, safety glasses, and appropriate disposable gloves (e.g., nitrile). Work in a fume hood or biosafety cabinet as appropriate for dust/aerosol control and contamination prevention.
  • Avoid inhalation of powders and contact with skin/eyes. Prevent environmental release—collect waste in labeled, compatible containers.
  • If this item is an oligonucleotide or peptide-like material, minimize nuclease/bioburden contamination (use nuclease-free water, sterile tips/tubes) and avoid repeated freeze–thaw.

• Incompatibilities and stability considerations (general)

  • Avoid strong oxidizers and strong acids/bases until compatibility is confirmed from the CoA/SDS. For sulfur-containing backbones (if applicable), limit exposure to oxidants and elevated temperatures.
  • Hygroscopic materials should be handled quickly at room temperature and promptly re-sealed or stored under inert atmosphere/desiccation.

• First aid (general guidance; defer to SDS)

  • Eye/skin contact: Rinse with water for several minutes; remove contaminated clothing. Seek medical advice.
  • Inhalation: Move to fresh air; seek medical attention if symptoms develop.
  • Ingestion: Rinse mouth; do not induce vomiting; seek medical attention.

• Authoritative source

  • Always consult the product’s SDS for definitive hazard, exposure limits, disposal codes, and emergency response information.

Solvent Selection

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

• General strategies based on likely chemotypes

  • For small molecules of unknown polarity: Start with anhydrous DMSO to prepare a concentrated stock (e.g., 10–50 mM), then dilute into assay buffer or media with attention to final DMSO ≤0.1–1% v/v to avoid biological interference.
  • For oligonucleotide-like materials (if applicable): Use nuclease-free water or low-ionic-strength buffers (e.g., 1× PBS, 10 mM HEPES, pH 7.2–7.6). Avoid strong acids/bases and high-organic content unless sequence/backbone compatibility is confirmed.

• Polarity and miscibility (general references)

  • DMSO: highly polar aprotic, miscible with water; facilitates dissolution of many heterocycles and aromatic scaffolds.
  • Water/aqueous buffers: preferred for polyanionic biopolymers and salt forms; supports downstream bioassays.
  • MeOH/ACN: useful for LC–MS sample prep or precipitation protocols; verify stability.

• Practical tips

  • Perform a small solubility screen (water, PBS, HEPES, DMSO, DMF, MeOH, ACN). Warm gently (≤37°C) and vortex/sonicate as needed; avoid prolonged heating.
  • Filter sterilize through 0.22 µm if sterility is required and the compound is compatible.
  • Record solvent lot, pH, ionic strength, and temperature to ensure reproducibility across studies.

Storage & Reconstitution

• Item-specific storage and shipping (from Product Data)

  • Storage conditions: Store at -20°C.
  • Shipped in: Ice chest + Ice pads.
  • Research use note: For research use only.

• Reconstitution (item-specific details not provided; general guidance)

  • If supplied as a solid: Allow container to equilibrate to room temperature in a desiccator before opening to minimize moisture uptake. Dissolve in an appropriate solvent (e.g., nuclease-free water or DMSO), based on CoA solubility. Mix gently by inversion or brief vortex; avoid foaming.
  • If supplied as a solution: Inspect for particulates or discoloration; mix gently. Record concentration, buffer composition, and pH.

• Aliquoting and stability (general)

  • Prepare single-use aliquots to avoid repeated freeze–thaw. Store working solutions at 2–8°C for short-term use if stability allows; otherwise, -20°C or below as recommended by the CoA.
  • Protect from light if chromophores or photo-labile groups are present (unknown for this item).

• Documentation

  • Label aliquots with compound name/sku, lot, concentration, solvent/buffer, and date of preparation. Consult the CoA/Spec Sheet for any additional stabilizers, compatible buffers, or expiration/retest intervals specific to this item.

Structure & Identity

Overview: Bezeparsen is listed as a small-molecule/compound library entry without structural identifiers provided in the Product Data for this SKU.

• Item-specific identifiers (from Product Data)

  • CAS: 2639640-84-7
  • 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.
  • Synonyms/Names: Bezeparsen (no additional names provided)

• Structural features

  • Item-specific 2D/3D structural data were not provided with this listing. Please consult the CoA/Spec Sheet for definitive identifiers needed for cheminformatics registration (SMILES/InChI) and for drawing or rendering the structure in ELN/LIMS systems.

• Literature/general context (not item-specific)

  • The “-parsen” suffix has been used in the literature for certain sequence-defined oligonucleotide agents; however, no sequence or backbone information is provided here. Do not assume oligonucleotide identity for this catalog item without confirming the CoA.

• Practical identity guidance

  • For internal registration, tie this SKU to the CAS (2639640-84-7) and vendor lot/CoA. If your workflow requires exact structural strings (SMILES/InChI), request the current CoA/Spec Sheet or analytical package before use in modeling, property prediction, or controlled-substance screening.

Synthetic Utility

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

• General perspectives (not item-specific)

  • If Bezeparsen is a small molecule: it may serve as a reference standard, screening hit, or intermediate in medicinal chemistry SAR. Utility would include derivatization for probe development (e.g., introduction of reporter tags) contingent on known functional groups.
  • If it is an oligonucleotide-like material: synthetic utility centers on bioconjugation and assembly into higher-order constructs (e.g., probe–dye conjugates, nanoparticles, or ligand–oligo chimeras). Common chemistries include NHS-ester/amine coupling, maleimide/thiol addition, copper-free click (DBCO–azide), and enzymatic 3′/5′-end labeling.

• Retrosynthetic considerations (general)

  • Small molecules: map potential handles (amines, alcohols, halides) for cross-coupling, acylation, or heterocycle elaboration.
  • Oligonucleotides: sequence-defined synthesis is typically conducted by solid-phase phosphoramidite chemistry with protecting-group strategies; post-synthetic modifications are introduced either on-resin or in solution.

• Practical tip

  • Before planning derivatization, obtain definitive structural information from the CoA and confirm presence/position of reactive handles to avoid uncontrolled side reactions or loss of activity.

Target Specificity

• Item-specific target, pathway, or epitope: Not specified for this item; refer to CoA/Spec Sheet.

• Notes

  • No gene, protein, or pathway specificity is provided in the Product Data. Do not infer biological selectivity without primary documentation.
  • If target information is essential for your application, request the latest CoA, technical note, or sequence disclosure (if applicable) to confirm intended specificity and off-target risk assessment.