human cgrp

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.

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.

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].

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.

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

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 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).

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

Adrenomedullin (AM) (22-52), human acetate is an antagonist of calcitonin generelated peptide receptor in the hindlimb vascular bed of the cat and an adrenomedullin receptor.

Eptinezumab, a human monoclonal antibody, specifically binds to and blocks the calcitonin gene-related peptide (CGRP) from binding to its receptor, thus acting as a preventive treatment for migraine in adults [1].

Vazegepant hydrochloride (Vazegepant HCl) is the first intranasal gepant for the acute treatment of migraine and has announced a positive phase II III study.

Atogepant (MK-8031) is an orally available, selective and potent calcitonin gene-related peptide receptor (CGRP) antagonist for the study of migraine.

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.

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].

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.

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

MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC 50 = 0.12 nM; K i = 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3. IC50 Value: 0.024 nM (Ki, Human CGRP) [1] As other CGRP receptor antagonists, MK-3207 shows a lower affinity for human CGRP receptors from other species, including canine and rodent. in vitro: MK-3207 is a potent antagonist of the human and rhesus monkey CGRP receptors (K(i) = 0.024 nM). in vivo: MK-3207 produced a concentration-dependent inhibition of dermal vasodilation, with plasma concentrations of 0.8 and 7 nM required to block 50 and 90% of the blood flow increase, respectively. The tritiated analog [3H]MK-3207 was used to study the binding characteristics on the human CGRP receptor. [3H]MK-3207 displayed reversible and saturable binding (K(D) = 0.06 nM), and the off-rate was determined to be 0.012 min(-1), with a t(1 2) value of 59 min [1]. After the first interim analysis, the two lowest MK-3207 doses (2.5, 5 mg) were identified as showing insufficient efficacy. Per the pre-specified adaptive design decision rule, only the 2.5-mg group was discontinued and the five highest doses (5, 10, 20, 50, 100 mg) were continued into the second stage [2]. Clinical trial: MK-3207 for the treatment of acute migraines. Phase 2b

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

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

Olcegepant (BIBN-4096) is an effective and selective non-peptide calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP).