Date published: 2025-10-15

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CGRP1 Inhibitors

CGRP1 inhibitors are a class of compounds that specifically target and inhibit the activity of the calcitonin gene-related peptide 1 (CGRP1) receptor, which is involved in various physiological processes such as vasodilation, pain signaling, and neurogenic inflammation. CGRP1 is a receptor that binds to the calcitonin gene-related peptide (CGRP), a neuropeptide released from sensory nerves, particularly in response to stimuli like stress or injury. When activated, the CGRP1 receptor plays a key role in regulating vascular tone by inducing relaxation of smooth muscles in blood vessels and modulating neurogenic communication pathways. Inhibiting CGRP1 prevents the receptor from responding to CGRP, thereby blocking its downstream signaling effects.

The mechanism of action for CGRP1 inhibitors involves binding to the CGRP1 receptor or its ligand-binding site, preventing CGRP from interacting with the receptor and activating its signaling pathways. This inhibition is useful in research aimed at understanding the specific role of CGRP1 in physiological functions such as vascular regulation, neurotransmission, and the modulation of inflammatory responses. By inhibiting CGRP1, scientists can explore how this receptor influences various biological processes and the broader impact of CGRP signaling on systems such as the nervous and circulatory systems. CGRP1 inhibitors are valuable tools for dissecting the molecular and cellular pathways regulated by CGRP and its receptor, offering insights into how these pathways maintain normal physiological functions and respond to environmental or internal stimuli.

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Items 1 to 10 of 12 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Capsazepine

138977-28-3sc-201098
sc-201098A
5 mg
25 mg
$145.00
$450.00
11
(1)

Capsazepine potentially downregulates CGRP1 expression by antagonizing the TRPV1 receptor, which when activated, can lead to an increase in CGRP release.

Corticosterone

50-22-6sc-300391
sc-300391A
100 mg
500 mg
$57.00
$108.00
2
(2)

Corticosterone may decrease CGRP1 expression by binding to glucocorticoid receptors, initiating a cascade that culminates in the suppression of gene expression, including that of CGRP1.

Ketoconazole

65277-42-1sc-200496
sc-200496A
50 mg
500 mg
$62.00
$260.00
21
(1)

Ketoconazole could lead to reduced CGRP1 expression by inhibiting cytochrome P450 enzymes that synthesize steroid hormones, which are known to play a role in the expression of various genes.

SB 203580

152121-47-6sc-3533
sc-3533A
1 mg
5 mg
$88.00
$342.00
284
(5)

SB 203580 might inhibit the p38 MAPK pathway, which is speculated to be involved in the pathway leading to CGRP1 expression, thereby potentially decreasing its levels.

Forskolin

66575-29-9sc-3562
sc-3562A
sc-3562B
sc-3562C
sc-3562D
5 mg
50 mg
1 g
2 g
5 g
$76.00
$150.00
$725.00
$1385.00
$2050.00
73
(3)

Forskolin has the ability to increase intracellular cAMP, which may reduce CGRP1 expression through a protein kinase A (PKA)-dependent mechanism that suppresses gene transcription.

Y-27632, free base

146986-50-7sc-3536
sc-3536A
5 mg
50 mg
$182.00
$693.00
88
(1)

Y-27632, by inhibiting the Rho-associated protein kinase (ROCK), might downregulate cellular processes that contribute to the promotion of CGRP1 expression.

PD 98059

167869-21-8sc-3532
sc-3532A
1 mg
5 mg
$39.00
$90.00
212
(2)

PD 98059, a MEK inhibitor, could decrease ERK phosphorylation, leading to reduced transcriptional activity of genes, including the one encoding CGRP1.

SP600125

129-56-6sc-200635
sc-200635A
10 mg
50 mg
$40.00
$150.00
257
(3)

SP600125 selectively inhibits the JNK pathway, which is thought to be involved in the upstream signaling that promotes CGRP1 expression, possibly leading to decreased expression levels.

Wortmannin

19545-26-7sc-3505
sc-3505A
sc-3505B
1 mg
5 mg
20 mg
$66.00
$219.00
$417.00
97
(3)

Wortmannin can inhibit the PI3K/AKT pathway, resulting in decreased phosphorylation and activity of downstream targets, potentially leading to a reduction in CGRP1 expression.

Apocynin

498-02-2sc-203321
sc-203321A
sc-203321B
sc-203321C
1 g
10 g
100 g
500 g
$26.00
$67.00
$114.00
$353.00
74
(2)

Apocynin may suppress the activity of NADPH oxidase, leading to a decrease in reactive oxygen species (ROS) that could otherwise enhance the transcription of genes such as CGRP1.