cgrp receptor

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

CGRP (83-119), rat TFA (Calcitonin Gene Related Peptide(83-119), rat TFA) is a 37 amino acid calcitonin family of neuropeptide, acts through calcitonin receptor-like receptor.

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.

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.

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).

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

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

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

Calcitonin Gene Related Peptide (CGRP) (83-119), rat is a 37 amino acid calcitonin family of neuropeptide, acts through calcitonin receptor-like receptor.

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

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

AC 187 TFA, a potent and orally active amylin receptor antagonist, exhibits an IC50 of 0.48 nM and a Ki of 0.275 nM. It demonstrates greater selectivity for the amylin receptor over calcitonin and CGRP receptors and has been shown to possess neuroprotective effects [1] [2].

Atogepant ((3R,5R,6S)-MK-8031) is the enantiomer of itself and serves as a calcitonin gene-related peptide (CGRP) receptor antagonist, primarily utilized in migraine research.

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].

Olcegepant hydrochloride is a potent and selective non-peptidethe calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (with IC50 of 0.03 nM for human CGRP).

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

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.

MK-8825 is a CGRP receptor antagonist.

Telcagepant is an orally active antagonist of calcitonin gene-related peptide (CGRP) receptor (Kis: 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively).

Calcitonin (salmon), a calcium regulating hormone, is used to treat osteoporosis in women who are at least 5 years past menopause.

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.

Vazegepant (Zavegepant) is an orally available and selective antagonist of the calcitonin gene-related peptide CGRP receptor for pain relief and may be used in the study of migraine.

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

[Tyr22] Calcitonin Gene Related Peptide (22-37), rat, refers to a fragment (amino acids 22-37) of the rat calcitonin gene-related peptide (CGRP) that targets the CGRP receptor and adenylate cyclase. While calcitonin is primarily produced by thyroid C cells, CGRP is predominantly secreted and stored within the nervous system [1].

HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist for acute treatment of migraine.

CGRP 8-37 (rat) is a CGRP receptor antagonist, a CGRP fragment with potential anti-injury effects that induces arterial relaxation.

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).

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

Human β-CGRP TFA (β-CGRP, human TFA) is a calcitonin peptide that functions through interaction with the calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP) complex, demonstrating IC50 values of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2, respectively, in cellular assays [1].

Ubrogepant (MK-1602) is an antagonist of calcitonin gene-related peptide receptor that can be used in the acute treatment of migraine studies.

Endogenous central calcitonin (CT) receptor agonist that stimulates cAMP formation at a potency 350-fold greater than CT (ED50 values are 0.2 and 71 nM respectively). Displays no activity at calcitonin-gene related peptide (CGRP) and adrenomedullin recept