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Vapreotide acetate

Catalog No. T13306L   CAS 849479-74-9
Synonyms: RC-160 acetate, BMY-41606 acetate

Vapreotide acetate (BMY-41606 acetate) is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).

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Vapreotide acetate Chemical Structure
Vapreotide acetate, CAS 849479-74-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 80.00
10 mg In stock $ 122.00
25 mg In stock $ 198.00
50 mg In stock $ 369.00
100 mg In stock $ 531.00
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Purity: 99.89%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Vapreotide acetate (BMY-41606 acetate) is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).
Targets&IC50 NK1:330 nM
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 [1]. 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) [2]. 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) [3].
In vivo Bleeding by rupture of oesophagogastric varices is a severe complication of portal hypertension in cirrhosis. The acute administration of vapreotide to rats decreases collateral circulation blood flow while chronic administration attenuated its development [4]. Tumor volumes and weights are reduced by about 40% by RC-160 by s.c. injections at doses of 100 μg/day/animal. When the therapy is started at an early stage of tumor development Vapreotide can inhibit the growth of androgen-independent prostate cancer [5].
Synonyms RC-160 acetate, BMY-41606 acetate
Molecular Weight 1191.42
Formula C59H74N12O11S2
CAS No. 849479-74-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 14 mg/mL (11.75 mM), sonification is recommended.

TargetMolReferences and Literature

1. Spitsin S, et al. Analog of somatostatin vapreotide exhibits biological effects in vitro via interaction with neurokinin-1 receptor. Neuroimmunomodulation. 2013;20(5):247-55. 2. Hofland LJ, et al. Relative potencies of the somatostatin analogs octreotide, BIM-23014, and RC-160 on theinhibition of hormone release by cultured human endocrine tumor cells and normal rat anterior pituitary cells. Endocrinology. 1994 Jan;134(1):301-6. 3. Buscail L, et al. Inhibition of cell proliferation by the somatostatin analogue RC-160 is mediated by somatostatin receptor subtypes SSTR2 and SSTR5 through different mechanisms. Proc Natl Acad Sci U S A. 1995 Feb 28;92(5):1580-4. 4. Veal N, et al. Hemodynamic effects of acute and chronic administration of vapreotide in rats with cirrhosis. Dig Dis Sci. 2003 Jan;48(1):154-61. 5. Pinski J, et al. Effect of somatostatin analog RC-160 and bombesin/gastrin releasing peptide antagonist RC-3095 on growth of PC-3 human prostate-cancer xenografts in nude mice.

Related compound libraries

This product is contained In the following compound libraries:
Peptide Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Immunology/Inflammation Compound Library Inhibitor Library NO PAINS Compound Library

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Keywords

Vapreotide acetate 849479-74-9 GPCR/G Protein Neuroscience Neurokinin receptor Vapreotide BMY-41606 BMY41606 RC-160 acetate BMY41606 Acetate RC-160 Acetate NK receptor Tachykinin receptor BMY 41606 Acetate RC160 Acetate RC 160 BMY 41606 Vapreotide Acetate RC 160 Acetate BMY-41606 Acetate RC160 Inhibitor RC-160 inhibit BMY-41606 acetate Neurokinin Receptor inhibitor

 

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