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Vapreotide

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

Catalog No. T13306Cas No. 103222-11-3

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Vapreotide

Catalog No. T13306Cas No. 103222-11-3

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

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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.
Alias	BMY 41606, RC160

Chemical Properties

Molecular Weight	1131.38
Formula	C₅₇H₇₀N₁₂O₉S₂
Cas No.	103222-11-3

Storage & Solubility Information

Storage

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

H2O: 60 mg/mL (53.03 mM)

Solution Preparation Table

H2O

	1mg	5mg	10mg	50mg
1 mM	0.8839 mL	4.4194 mL	8.8388 mL	44.1938 mL
5 mM	0.1768 mL	0.8839 mL	1.7678 mL	8.8388 mL
10 mM	0.0884 mL	0.4419 mL	0.8839 mL	4.4194 mL
20 mM	0.0442 mL	0.2210 mL	0.4419 mL	2.2097 mL
50 mM	0.0177 mL	0.0884 mL	0.1768 mL	0.8839 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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

Keywords

VapreotideRC-160BMY41606BMY-41606RC 160