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Vapreotide acetate

Cat. No. M10332
Vapreotide acetate Structure
Synonym:

BMY-41606; RC160; Octastatin acetate

Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 150  USD150 In stock
25mg USD 250  USD250 In stock
50mg USD 450  USD450 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 1191.39
Formula C59H74N12O11S2
CAS Number 849479-74-9
Purity >99%
Solubility Water 11 mg/mL
Storage -20°C, sealed
References

[1] Sergei Spitsin, et al. Neuroimmunomodulation. Analog of somatostatin vapreotide exhibits biological effects in vitro via interaction with neurokinin-1 receptor

[2] Nary Veal, et al. Dig Dis Sci. Hemodynamic effects of acute and chronic administration of vapreotide in rats with cirrhosis

[3] L J Hofland, et al. Endocrinology. 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

[4] L Buscail, et al. Proc Natl Acad Sci U S A. Inhibition of cell proliferation by the somatostatin analogue RC-160 is mediated by somatostatin receptor subtypes SSTR2 and SSTR5 through different mechanisms

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Keywords: Vapreotide acetate, BMY-41606; RC160; Octastatin acetate supplier, Neurokinin Receptor, inhibitors
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