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Vapreotide

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Catalog No. T13306Cas No. 103222-11-3
Alias RC160, BMY 41606

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

Vapreotide

Vapreotide

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Catalog No. T13306Alias RC160, BMY 41606Cas No. 103222-11-3
Vapreotide is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
Vapreotide is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).
Targets&IC50
NK1R:330 nM
In vitro
In a concentration-dependent manner, Vapreotide attenuates the effect of SP on calcium release . The concentration required for Vapreotide to completely inhibit the effect of SP is about 100 times higher than that required for the NK1R antagonist aprepitant. The effect of Vapreotide on cell proliferation is mediated primarily by SSTR2. In order to further establish the NK1R antagonist effect of Vapreotide, U373MG cells are pretreated with SSTR2 selective antagonist CYN followed by incubation with Vapreotide and SP stimulation. The results show that pretreatment with CYN does not reverse the inhibitory effect of Vapreotide on SP-stimulated IL-8 mRNA expression. As compared to control MDM, limited HIV gag mRNA expression may indicate that Vapreotide can reduce HIV-1 replication in MDM. In addition, SP treatment (10 μM) reversed the inhibitory effect of pentoprofen on HIV-1 replication in MDM. This observation indicates that the inhibitory effect of Vapreotide on HIV-1 replication is most likely due to its interaction with NK1R.
SynonymsRC160, BMY 41606
Chemical Properties
Molecular Weight1131.38
FormulaC57H70N12O9S2
Cas No.103222-11-3
Smiles[H][C@@]1(Cc2ccc(O)cc2)NC(=O)[C@H](CSSC[C@H](NC(=O)C(NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)NC(=O)[C@H](N)Cc1ccccc1 |@:49|
Relative Density.1.4 g/cm3
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: 60 mg/mL (53.03 mM), Sonication is recommended.
Solution Preparation Table
H2O
1mg5mg10mg50mg
1 mM0.8839 mL4.4194 mL8.8388 mL44.1938 mL
5 mM0.1768 mL0.8839 mL1.7678 mL8.8388 mL
10 mM0.0884 mL0.4419 mL0.8839 mL4.4194 mL
20 mM0.0442 mL0.2210 mL0.4419 mL2.2097 mL
50 mM0.0177 mL0.0884 mL0.1768 mL0.8839 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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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