1. GPCR/G Protein Neuronal Signaling
  2. CGRP Receptor
  3. HCGRP-(8-37)

HCGRP-(8-37)  (Synonyms: Human α-CGRP (8-37))

Cat. No.: HY-P1014 Purity: 99.51%
Handling Instructions Technical Support

HCGRP-(8-37) (Human α-CGRP (8-37)) is a fragment of human calcitonin gene-related peptide (hCGRP) and an antagonist of the CGRP receptor, with an IC50 of 32.1 pM against the CGRP receptor. HCGRP-(8-37) blocks adenylate cyclase activation induced by CGRP receptor ligands and attenuates vascular responses triggered by CGRP. HCGRP-(8-37) reduces capsaicin-induced vasodilation in porcine nasal mucosa and superficial skin. HCGRP-(8-37) serves as a research tool to distinguish effects mediated by CGRP or calcitonin receptors, and to investigate CGRP-induced vascular effects.

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

Custom Peptide Synthesis

HCGRP-(8-37)

HCGRP-(8-37) Chemical Structure

CAS No. : 119911-68-1

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500 μg In-stock
1 mg In-stock
5 mg In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HCGRP-(8-37) (Human α-CGRP (8-37)) is a fragment of human calcitonin gene-related peptide (hCGRP) and an antagonist of the CGRP receptor, with an IC50 of 32.1 pM against the CGRP receptor. HCGRP-(8-37) blocks adenylate cyclase activation induced by CGRP receptor ligands and attenuates vascular responses triggered by CGRP. HCGRP-(8-37) reduces capsaicin-induced vasodilation in porcine nasal mucosa and superficial skin. HCGRP-(8-37) serves as a research tool to distinguish effects mediated by CGRP or calcitonin receptors, and to investigate CGRP-induced vascular effects[1][2].

IC50 & Target

CGRP receptor[1]

In Vitro

HCGRP-(8-37) (10 min at 37°C) acts as a CGRP receptor antagonist in rat liver plasma membranes. It inhibits CGRP- and calcitonin-induced adenylate cyclase activation in a dose-dependent manner, but does not affect basal, epinephrine- or glucagon-stimulated activities[1].
HCGRP-(8-37) (60 min at 37°C) binds to calcitonin receptors in LLC-PK1 porcine kidney cells in a dose-dependent manner[1].
HCGRP-(8-37) (15 min at 37°C) acts as a calcitonin receptor agonist in LLC-PK1 porcine kidney cells, which dose-dependently stimulates cAMP production without antagonizing calcitonin- or CGRP-induced cAMP production[1].
HCGRP-(8-37) potently inhibits CGRP-mediated adenylate cyclase activation in cell-free rat liver plasma membrane preparations[2].

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

In Vivo

HCGRP-(8-37) (16 µM; local intra-arterial infusion; 20 minutes) significantly attenuates both CGRP- and capsaicin-mediated vasodilation in the pig nasal mucosa and reduces the integrated and duration-based capsaicin- and CGRP-mediated skin vasodilation responses, confirming it acts as a functional CGRP receptor antagonist in vivo[2].

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

Animal Model: Domestic pigs (either sex, 17-22 kg)[2]
Dosage: 16 µM
Administration: local intra-arterial infusion; 20 minutes
Result: Significantly attenuated capsaicin-evoked increases in nasal vascular conductance and decreases in nasal cavity volume.
Significantly reduced capsaicin-evoked superficial skin blood flow when calculated as area under the curve (AUC); capsaicin-induced skin peak blood flow remained unchanged (96% of control, not significant), but the duration of the skin response was significantly reduced to 69% of control .
Significantly reduced CGRP-evoked increases in nasal vascular conductance and decreases in nasal cavity volume.
Significantly attenuated CGRP-evoked superficial skin blood flow, with reductions seen in AUC, peak response, and response duration.
Molecular Weight

3125.59

Formula

C139H230N44O38

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Val-Thr-His-Arg-Leu-Ala-Gly-Leu-Leu-Ser-Arg-Ser-Gly-Gly-Val-Val-Lys-Asn-Asn-Phe-Val-Pro-Thr-Asn-Val-Gly-Ser-Lys-Ala-Phe

Sequence Shortening

VTHRLAGLLSRSGGVVKNNFVPTNVGSKAF

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

Solvent & Solubility
In Vitro: 

H2O : ≥ 20 mg/mL (6.40 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.3199 mL 1.5997 mL 3.1994 mL
5 mM 0.0640 mL 0.3199 mL 0.6399 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). 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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 20 mg/mL (6.40 mM); Clear solution; Need ultrasonic

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

Purity: 99.51%

References

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). 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 0.3199 mL 1.5997 mL 3.1994 mL 7.9985 mL
5 mM 0.0640 mL 0.3199 mL 0.6399 mL 1.5997 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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  • 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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HCGRP-(8-37)
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HY-P1014
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