a-cgrp

Endogenous calcitonin gene-related peptide receptor (CGRP) agonist.

α-CGRP (human) acetate is a regulatory neuropeptide of 37 amino acids. It is the most potent vasodilator known to date and has inotropic and chronotropic effects.

Tyr-α-CGRP is an N-terminal extended tyrosinated analogue of α-calcitonin gene-related peptide . It binds to amylin receptors AMY1 and AMY3 in COS-7 cells expressing the human receptors (IC50s = 141 and 1.86 nM, respectively). Tyr-α-CGRP also binds to and stimulates cAMP accumulation in rat L6 myocytes (IC50 = 4 nM; EC50 = 12 nM). It also binds to rat brain and spleen membrane preparations (IC50s = 0.2 and 0.5 nM, respectively), induces positive chronotropic and inotropic effects in isolated right and left guinea pig atria (EC50s = 282 and 74 nM, respectively), and inhibits the twitch response in rat vas deferens (EC50 = 1.9 nM).

β-CGRP, human ,a 37-amino acid peptide,is the beta form of Calcitonin-gene-related peptide (β-CGRP), involved extensively in regulation of the cardiovascular and nervous systems. β-CGRP contains a disulphide bridge at the N-terminus, a C-terminal phenylal

Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist

Endogenous neuropeptide, potent vasodilator

Telcagepant (MK-0974) is an oral calcitonin gene-related peptide receptor (CGRP) antagonist that blocks CGRP receptors and reduces neurotransmission in the central nervous system and is used in the study of migraines and for pain relief.

β-CGRP,human tissue is one of the calcitonin peptide, through complex behavior of calcitonin receptor like receptor (CRLR) - and receptor activity - modifying proteins (increased), and 1 and 300 - nM CRLR IC50s/RAMP1 and CRLR/RAMP2 cells.

β-CGRP, human acetate is one of calcitonin peptides and acts via the complex of receptor-activity-modifying protein (RAMP) and calcitonin-receptor-like receptor (CRLR) (IC50s: 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells).

Rimegepant (BMS 927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.

CGRP antagonist 1 is a potent CGRP receptor antagonist with Ki values of 35 nM and IC50 values of 57 nM, respectively.CGRP antagonist 1 can be used for the study of cardiovascular and neurovascular diseases.

BMS-694153 is a potent and selective CGRP receptor antagonist.This compound is unstable in powder form and other related salt forms are recommended.

α-CGRP (rat) acetate is a calcitonin gene-related peptide (CGRP). CGRP (rat) acetate is a potent vasodilator.

Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a selective calcitonin gene-related peptide 1 (CGRP1) receptor antagonist with an IC50=0.03 nM and Ki=14.4 pM.

CGRP Antagonist 6 (Compound 23) is a potent CGRP receptor antagonist (Ki: 0.84 nM). It is utilized in the study of migraines.

CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a Ki value of 0.029 nM. It effectively inhibits CGRP receptor-mediated cyclic adenosine monophosphate (cAMP) production, with an IC50 value of 1.5 nM. This compound is useful in migraine research.

Rimegepant (BMS-927711) hemisulfate is a potent, orally active selective competitive antagonist of the calcitonin gene-related peptide (CGRP) receptor, with a Ki of 0.027 nM and an IC50 of 0.14 nM for the hCGRP receptor. Rimegepant hemisulfate is utilized in migraine research.

PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and 5-HT1F Receptor partial agonist (EC50 = 77.91 nM). It demonstrates significant efficacy in rat models of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins while inhibiting the phosphorylation levels of ERK and CREB. This compound is useful for migraine research.

Desfluoro-BMS-694153 (Compound 3) is an antagonist of the calcitonin gene-related peptide receptor (CGRP receptor) with a Ki of 0.01 nM. It exhibits a significantly reduced risk of CYP3A4 inhibition, with IC50 values of 36 μM for CYP3A4-BFC and 6 μM for CYP3A4-BZR. Desfluoro-BMS-694153 is useful for migraine research.

MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K(i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively.

AC 187 Acetate is a potent antagonist of amylin receptor .AC 187 shows more selective for amylin receptor than calcitonin and CGRP receptors.

BI-44370, a CGRP (calcitonin gene-related peptide) receptor antagonist, can be used to treat migraines and other chronic pain.

Cizolirtine is a calcitonin gene-related peptide antagonist. Cizolirtine may be useful for alleviating some neuropathic somatosensory disorders, in particular cold allodynia, with a reduced risk of undesirable side effects. Cizolirtine inhibits the spinal

Cyclo(L-Phe-L-Val) is a metabolite of the sponge bacterium Pseudoalteromonas sp. NJ6-3-1, capable of autoinducing the production of antibacterial substances active against S. aureus at low cell density. It induces neurite outgrowth and branching of chick cortical neurons in vitro at concentrations of 16 and 32 μM, increases phosphorylation of the PI3K substrate Akt, and this induction can be blocked by the PI3K inhibitor LY294002. Additionally, it enhances axon sprouting of calcitonin gene-related protein positive (CGRP+) primary afferents in the spinal cord post-crush injury and of serotonin neurons in the uninjured spinal cord. Cyclo(L-Phe-L-Val) is also a bitter taste component of cocoa and roasted coffee.