Vapreotide acetate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Vapreotideacetate 是神经激肽-1 (NK1) 受体的拮抗剂 (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 .

Vapreotide attenuates the Substance P (SP)-triggered intracellular calcium increases and NF-κB activation in a dose-dependent manner. Vapreotide also inhibits SP-induced IL-8 and MCP-1 production in HEK293-NK1R and U373MG cell lines. Vapreotide inhibits HIV-1 infection of human MDM in vitro, 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 with an IC50 of 0.1 pM. Vapreotide exhibits moderate-to-high affinities for SSTR2, -3, and -5 (IC50=0.17, 0.1 and 21 nM, respectively) and low affinity for SSTR1 and -4 (IC50=200 and 620 nM, respectively). RC-160 inhibits serum-induced proliferation of CHO cells expressing SSTR2 and SSTR5 (EC50=53 and 150 pM, respectively).

In cirrhosis, bleeding by rupture of oesophagogastric varices is a severe complication of portal hypertension. 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. Vapreotide can inhibit the growth of androgen-independent prostate cancer when the therapy is started at an early stage of tumor development.

RC-160 acetate | BMY-41606 acetate

GPCR/G Protein

Neurokinin Receptor

Human Endogenous Metabolite| serotonin

——

——

849479-74-9

1191.39

C57H70N12O9S2.xC2H4O2

>98% (HPLC)

In Vitro:?H2O : 14.29 mg/mL (11.99 mM)

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

——

(-20℃)

With Ice Pack

≥ 2 years