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GPCR/G Protein

Cholecystokinin Receptor

Melanin-concentrating Hormone Receptor (MCHR)

(11)

Melanocortin Receptor

Neuropeptide Y Receptor

Prostaglandin Receptor

(199)

Protease-activated Receptor

Neuroscience

Melanocortin Receptor

Neuropeptide Y Receptor

Serotonin Transporter

(54)

iGluR

(143)

CGRP Receptor

CGRP receptor is found in myelinated A-fibers axon which is required for ligand specificity and function of the receptor. The CGRP receptor has three subunits: receptor activity-modifying protein 1 (RAMP1), calcitonin-like receptor (CLR) and receptor component protein (RCP).[17] The complex central receptor is the G protein-coupled receptor calcitonin receptor-like receptor (CALCRL) which is necessary for CGRP and adrenomedullin (AM receptors). For function CGRP, CALCRL must coincide with RAMP1 where the ligand-binding domain of CGRP is located.

Filter HomeSignaling PathwaysNeuroscience-GPCR/G ProteinCGRP Receptor

Rimegepant

T46101289023-67-1

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

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Ubrogepant

T171941374248-77-7

Ubrogepant (MK-1602) is a calcitonin gene-related peptide receptor antagonist used in acute migraine treatment studies.

$155

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Olcegepant

T12293L204697-65-4

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).

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Calcitonin (salmon)

TP104047931-85-1

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

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HCGRP-(8-37) acetate

TP1134L

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

$172

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CGRP antagonist 1

T134531123757-49-2In house

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.

$342

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Cagrilintide acetate

T76262L

Cagrilintide acetate is the salt form of Cagrilintide.Cagrilintide is a long-acting amylin analog that is used to treat type 2 diabetes and obesity by reducing appetite through activation of the amylin receptor AMY3R and calcitonin receptor CTR.

$129

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Erenumab

T768741582205-90-0

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

$213

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Galcanezumab

T766821578199-75-3

Galcanezumab is a humanized IgG4 monoclonal antibody targeting the CGRP ligand, which binds to the ligand calcitonin gene-related peptide. Galcanezumab can be used to prevent and treat migraines or cluster headaches.

$129

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Atogepant

T266821374248-81-3

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

$158

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Vazegepant hydrochloride

T86821414976-20-7

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

$109

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Vazegepant

T387341337918-83-8

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.

$106

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Telcagepant

T16093781649-09-0

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.

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β-CGRP, human acetate

TP2167

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).

$382

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CGRP 8-37 (rat)

TP1323129121-73-9

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

$287

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Calcitonin(salmon) Acetate(47931-85-1(free base))

TP1040L

Calcitonin(salmon)Acetate(47931-85-1(free base))(Salmon calcitonin) , a calcium regulating hormone, is used to treat osteoporosis in women who are at least 5 years past menopause.

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SUN B8155

T23406345893-91-6

SUN B8155 is a calcitonin (CT) receptor agonist that selectively mimics the biological effects of calcitonin and induces cAMP formation in cells expressing recombinant human CT receptor.

$142

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Adrenomedullin (AM) (22-52), human acetate

TP1257L

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.

$133

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MK-3207 Hydrochloride

T6590957116-20-0

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.

$153

10-14 weeks

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Olcegepant hydrochloride

T12293586368-06-1

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.

$107

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PHM-27 (human) acetate

TP1954L

PHM-27 (human) acetate is the endogenous peptide product of prepro-VIP (human), an agonist of the calcitonin receptor (EC 50 = 11 nM). Transgenic mice overexpressing PHM-27 (human) acetate in pancreatic β-islets exhibited enhanced glucose-induced insulin secretion.

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Calcitonin-13C6,15N4 TFA

T201476

Calcitonin-13CIC6,15NIC4(salmon) (Salmon calcitonin-13CIC6,15NIC4) TFA is a version of calcitonin(salmon) labeled with carbon-13 and nitrogen-15. This hormone regulates calcium and acts dualistically as an agonist to both amylin and calcitonin receptors, promoting bone formation while inhibiting bone resorption.

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CGRP antagonist 6

T200460

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

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ML230

T161071776055-05-0

ML230 is a selective ATP-binding cassette (ABC) transporter ABCG2 inhibitor. It 36-fold selective for ABCG2 over ABCB1 (EC50s: 0.13 μM and 4.65 μM, respectively).

35 days

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