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Vapreotide acetate

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Catalog No. T13306LCas No. 849479-74-9
Alias RC-160 acetate, BMY-41606 acetate

Vapreotide acetate (BMY-41606 acetate) is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).

Vapreotide acetate

Vapreotide acetate

🥰Excellent
Purity: 99.89%
Catalog No. T13306LAlias RC-160 acetate, BMY-41606 acetateCas No. 849479-74-9
Vapreotide acetate (BMY-41606 acetate) is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$64In StockIn Stock
10 mg$106In StockIn Stock
25 mg$198In StockIn Stock
50 mg$328In StockIn Stock
100 mg$531In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.89%
Appearance:Solid
Color:White
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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.
SynonymsRC-160 acetate, BMY-41606 acetate
Chemical Properties
Molecular Weight1191.42
FormulaC59H74N12O11S2
Cas No.849479-74-9
SmilesCC(O)=O.O=C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N1)=O)C(C)C)=O)CCCCN)=O)CC2=CNC3=C2C=CC=C3)=O)CC4=CC=C(C=C4)O)=O)CSSC[C@H]1C(N[C@H](C(N)=O)CC5=CNC6=C5C=CC=C6)=O)[C@H](N)CC7=CC=CC=C7
Relative Density.no data available
Sequence{d-Phe}-Cys-Tyr-{d-Trp}-Lys-Val-Cys-Trp-NH2 (Disulfide bridge: Cys2-Cys7)
Sequence Short{d-Phe}-CY-{d-Trp}-KVCW (Disulfide bridge: Cys2-Cys7)
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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