Vapreotide acetate

SKU: orb1308953

Description

Vapreotide acetate

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 849479-74-9
• MW: 1191.42
• Purity: 99.89%
• Formula: C₅₉H₇₄N₁₂O₁₁S₂
• SMILES: CC(O)=O.O=C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N1)=O)C(C)C)=O)CCCCN)=O)CC2=CNC3=C2C=CC=C3)=O)CC4=CC=C(C=C4)O)=O)CSSC[C@H]1C(N[C@H](C(N)=O)CC5=CNC6=C5C=CC=C6)=O)[C@H](N)CC7=CC=CC=C7
• Target: Neurokinin receptor
• Solubility: H2O:14 mg/mL (11.75 mM)

Bioactivity

• Target IC50:
  NK1:330 nM
• In Vivo:
  Acute vapreotide administration in rats reduces blood flow in collateral circulation, a critical factor in oesophagogastric variceal bleeding due to portal hypertension in cirrhosis, while its prolonged use slows down the development of such complications. Concurrently, RC-160 significantly diminishes tumor size and weight by approximately 40% through subcutaneous injections at a dosage of 100 μg/day/animal. Early-stage intervention with vapreotide is effective in curbing the progression of androgen-independent prostate cancer.
• In Vitro:
  In a dose-dependent manner, Vapreotide attenuates the Substance P (SP)-triggered intracellular calcium increases and NF-κB activation.in HEK293-NK1R and U373MG cell lines, Vapreotide inhibits SP-induced IL-8 and MCP-1 production. In vitro, Vapreotide inhibits HIV-1 infection of human MDM, an effect that is reversible by SP pretreatment . Vapreotide significantly inhibits GH-, PRL, and/or alpha-subunit release by human GH-secreting pituitary adenoma cells in concentrations as low as 10(-12)-10(-14) M. Vapreotide inhibits GH release (IC50: 0.1 pM) . Vapreotide exhibits moderate-to-high affinities for SSTR2, -3, and -5 with IC50 of 0.17, 0.1, and 21 nM, respectively, and low affinity for SSTR1 and -4 with IC50 of 200 and 620 nM, respectively. RC-160 inhibits serum-induced proliferation of CHO cells expressing SSTR2 and SSTR5 (EC50s: 53 and 150 pM) .

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMY41606, BMY-41606, BMY41606 Acetate, BMY-41606 Acetate, BMY-41606 acetate, BMY 41606, BMY 41606 Acetate, inhibit, NK receptor, NK1, Neurokinin Receptor, Neurokininreceptor, Neurokinin receptor, Inhibitor, RC-160 acetate, RC-160 Acetate, RC 160, RC 160 Acetate, RC160, RC-160, RC160 Acetate, Tachykinin receptor, Vapreotide acetate, Vapreotide Acetate, Vapreotide

Compound Identifiers

PubChem CID

154732000