Vapreotide acetate

Research use only, not for human use.

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

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

RC-160 acetate; BMY-41606 acetate

GPCR/G Protein

Neurokinin Receptor

Human Endogenous Metabolite; serotonin

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849479-74-9

1191.4

C57H70N12O9S2.xC2H4O2

>98% (HPLC)

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OC(C)=O.[FCYWKVCW-NH2(Disulfide bridge: Cys2-Cys7)]

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(-20℃)

With Ice Pack

≥ 2 years