1. Vapreotide

Vapreotide  (Synonyms: RC160; BMY 41606)

Cat. No.: HY-P0061 Purity: 98.06%
COA Handling Instructions

Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.

For research use only. We do not sell to patients.

Vapreotide Chemical Structure

Vapreotide Chemical Structure

CAS No. : 103222-11-3

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Vapreotide:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Vapreotide

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • Customer Review

Description

Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.

IC50 & Target

330 nM (NK1R)[1].

In Vitro

Vapreotide attenuates the effect of SP on calcium release in a concentration-dependent manner. 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. Vapreotide reduces HIV-1 replication in MDM as indicated by limited HIV gag mRNA expression compared to control MDM. In addition, SP treatment (10 μM) reverses Vapreotide inhibition of HIV-1 replication in MDM. This observation indicates that the inhibition of HIV-1 replication by Vapreotide is most likely due to its interaction with NK1R[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

1131.37

Formula

C57H70N12O9S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H](NC([C@H](CSSC[C@H](NC([C@@H](NC([C@@H](NC1=O)CCCCN)=O)C(C)C)=O)C(N[C@H](C(N)=O)CC2=CNC3=CC=CC=C23)=O)NC([C@H](N)CC4=CC=CC=C4)=O)=O)CC5=CC=C(C=C5)O)N[C@@H]1CC6=CNC7=CC=CC=C67

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (88.39 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8839 mL 4.4194 mL 8.8388 mL
5 mM 0.1768 mL 0.8839 mL 1.7678 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
Cell Assay
[1]

The HEK293-NK1R cells and U373MG cells are incubated with or without Vapreotide (0, 5, 10, 20 μM) for 10 minutes and then incubated with or without SP for 3 hours. In some experiments, cells are first incubated with CYN for 10 minutes, and then Vapreotide is added and incubated for an additional 10 minutes, followed by stimulation with SP for 3 hours. Mock treated cells are used as controls[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.8839 mL 4.4194 mL 8.8388 mL 22.0971 mL
5 mM 0.1768 mL 0.8839 mL 1.7678 mL 4.4194 mL
10 mM 0.0884 mL 0.4419 mL 0.8839 mL 2.2097 mL
15 mM 0.0589 mL 0.2946 mL 0.5893 mL 1.4731 mL
20 mM 0.0442 mL 0.2210 mL 0.4419 mL 1.1049 mL
25 mM 0.0354 mL 0.1768 mL 0.3536 mL 0.8839 mL
30 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7366 mL
40 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5524 mL
50 mM 0.0177 mL 0.0884 mL 0.1768 mL 0.4419 mL
60 mM 0.0147 mL 0.0737 mL 0.1473 mL 0.3683 mL
80 mM 0.0110 mL 0.0552 mL 0.1105 mL 0.2762 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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