Vapreotide acetate (BMY-41606 acetate; RC160 acetate) is a neurokinin-1 (NK1) receptor antagonist with IC50 value of 330 nM. Vapreotide inhibits SP-induced IL-8 and MCP-1 production in HEK293-NK1R and U373MG cell lines. Vapreotide also inhibits HIV-1 infection of human MDM in vitro, an effect that is reversible by SP pretreatment. Vapreotide inhibits serum-induced proliferation of CHO cells expressing SSTR2 and SSTR5 with EC50 of 53 and 150 pM, respectively.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||Water 11 mg/mL|
Analog of somatostatin vapreotide exhibits biological effects in vitro via interaction with neurokinin-1 receptor
Sergei Spitsin, et al. Neuroimmunomodulation. 2013;20(5):247-55. PMID: 23921645.
Hemodynamic effects of acute and chronic administration of vapreotide in rats with cirrhosis
Nary Veal, et al. Dig Dis Sci. 2003 Jan;48(1):154-61. PMID: 12645803.
Relative potencies of the somatostatin analogs octreotide, BIM-23014, and RC-160 on the inhibition of hormone release by cultured human endocrine tumor cells and normal rat anterior pituitary cells
L J Hofland, et al. Endocrinology. 1994 Jan;134(1):301-6. PMID: 7903931.
Inhibition of cell proliferation by the somatostatin analogue RC-160 is mediated by somatostatin receptor subtypes SSTR2 and SSTR5 through different mechanisms
L Buscail, et al. Proc Natl Acad Sci U S A. 1995 Feb 28;92(5):1580-4. PMID: 7878022.
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