human a-cgrp

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

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.

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.

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).

MK-3207 Hydrochloride (MK-3207 HCl) is a potent CGRP receptor antagonist with IC50 and Kiof 0.12 nM and 0.022 nM, highly selective versus human AM1, AM2, CTR, and AMY3. Phase 2.

α-CGRP (human) TFA is a 37-amino acid regulatory neuropeptide extensively located within the central and peripheral nervous systems, functioning as a potent vasodilator [1].

Adrenotensin (human) (Pro-ADM-153-185 (human)), a 153-185 fragment of the Adrenomedullin precursor peptide, is a 52-amino acid peptide from the CGRP superfamily that plays a diverse role in vasodilation [1].

Eptinezumab is a humanised monoclonal antibody targeting CGRP (calcitonin gene-related peptide), which prevents CGRP binding to its receptor and may be used for migraine prevention.

Fremanezumab (TEV-48125) is a humanised monoclonal antibody targeting CGRP, capable of neutralising human (IC50=7.94 nM), mouse (IC50=19.6 nM) and rat CGRP, and is indicated for the prevention of migraine. Fremanezumab inhibits CGRP's vasodilatory effects in the basilar artery constriction segment and suppresses activation of A-δ and high-threshold (HT) neurons in the meningeal nociceptive system triggered by cortical spreading depression (CSD) in rats. In vitro, Fremanezumab counteracts CGRP's immunosuppressive effects on microglia and lymphocytes.

Erenumab is a whole-human monoclonal antibody. Erenumab inhibits calcitonin gene-related peptide (CGRP) receptors. Erenumab can be used to prevent migraine attacks.

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

HCGRP-(8-37) acetate is a human calcitonin gene-related peptide (hCGRP) fragment acetate and also an antagonist of CGRP receptor.

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.

Biotinyl-α-CGRP (human) TFA is a peptide identified through peptide screening, which serves as a research tool primarily utilizing immunoassays to gather active peptides. This method is applicable in studying protein interactions, conducting functional analyses, and screening antigen epitopes, particularly useful in the research and development of active molecules.