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Vapreotide acetate

Vapreotide acetate
Vapreotide acetate (BMY-41606 acetate) is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).
Catalog No. T13306LCas No. 849479-74-9
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Purity:99.89%
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Vapreotide acetate

Catalog No. T13306LCas No. 849479-74-9
Vapreotide acetate (BMY-41606 acetate) is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$30In Stock
5 mg$64In Stock
10 mg$106In Stock
25 mg$198In Stock
50 mg$328In Stock
100 mg$531In Stock
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Product Introduction

Bioactivity
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
Acute vapreotide administration in rats reduces blood flow in collateral circulation, a critical factor in oesophagogastric variceal bleeding due to portal hypertension in cirrhosis, while its prolonged use slows down the development of such complications. Concurrently, RC-160 significantly diminishes tumor size and weight by approximately 40% through subcutaneous injections at a dosage of 100 μg/day/animal. Early-stage intervention with vapreotide is effective in curbing the progression of androgen-independent prostate cancer.
AliasRC-160 acetate, BMY-41606 acetate
Chemical Properties
Molecular Weight1191.42
FormulaC59H74N12O11S2
Cas No.849479-74-9
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: 14 mg/mL (11.75 mM), Sonication is recommended.
Solution Preparation Table
H2O
1mg5mg10mg50mg
1 mM0.8393 mL4.1967 mL8.3933 mL41.9667 mL
5 mM0.1679 mL0.8393 mL1.6787 mL8.3933 mL
10 mM0.0839 mL0.4197 mL0.8393 mL4.1967 mL

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