Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vapreotide acetate (BMY-41606 acetate) is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 14 mg/mL (11.75 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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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