2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. Vapreotide

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

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

Custom Peptide Synthesis

Vapreotide Chemical Structure

Vapreotide Chemical Structure

CAS No. : 103222-11-3

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Vapreotide Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Vapreotide

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NK1R NK2R NK3R

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

NK1R

 

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.

Vapreotide Related Antibodies
Clinical Trial
Molecular Weight

1131.37

Formula

C57H70N12O9S2
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

{d-Phe}-Cys-Tyr-{d-Trp}-Lys-Val-Cys-Trp-NH2 (Disulfide bridge: Cys2-Cys7)
Sequence Shortening

{d-Phe}-CY-{d-Trp}-KVCW-NH2 (Disulfide bridge: Cys2-Cys7)
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)

Purity & Documentation
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
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Vapreotide Related Classifications

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The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

Vapreotide103222-11-3RC160 BMY 41606RC 160RC-160BMY41606BMY 41606BMY-41606Neurokinin ReceptorNK receptorTachykinin receptorInhibitorinhibitorinhibit

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