1. Peptides

Vapreotide (Synonyms: RC160; BMY 41606)

Cat. No.: HY-P0061
Handling Instructions

Vapreotide is a NK1R antagonist, with an IC50 of 330 nM. Sequence: Phe-Cys-Tyr-Trp-Lys-Val-Cys-Trp-NH2(Disulfide bridge: Cys2-Cys7).

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

Custom Peptide Synthesis

Vapreotide Chemical Structure

Vapreotide Chemical Structure

CAS No. : 103222-11-3

Size Price Stock Quantity
10 mM * 1 mL in Water USD 418 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 336 In-stock
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50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
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Other Forms of Vapreotide:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Vapreotide is a NK1R antagonist, with an IC50 of 330 nM. Sequence: Phe-Cys-Tyr-Trp-Lys-Val-Cys-Trp-NH2(Disulfide bridge: Cys2-Cys7).

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

H2O : ≥ 60 mg/mL (53.03 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.0884 mL 0.4419 mL 0.8839 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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.

References
Molecular Weight

1131.37

Formula

C₅₇H₇₀N₁₂O₉S₂

CAS No.

103222-11-3

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Vapreotide
Cat. No.:
HY-P0061
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Vapreotide

Cat. No.: HY-P0061