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GPCR/G Protein

Melanin-concentrating Hormone Receptor (MCHR)

(10)

Melanocortin Receptor

Neuropeptide Y Receptor

Prostaglandin Receptor

(181)

Protease-activated Receptor

Neuroscience

AAK1 (AP2 associated kinase 1)

Melanocortin Receptor

Neuropeptide Y Receptor

Serotonin Transporter

(46)

iGluR

(113)

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 Signaling 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.
- $50
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Cited
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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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.
- $96
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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.
- $221
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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.
- $286
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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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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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α-CGRP (mouse, rat) TFA
T78540
α-CGRP (mouse, rat) TFA, a neuropeptide belonging to the calcitonin gene-related peptide (CGRP) family, is predominantly located at neuromuscular junctions and functions as a potent vasodilator. Peripheral administration of α-CGRP (mouse, rat) TFA may result in decreased blood pressure and elevated heart rate, in addition to the relaxation of colonic smooth muscle. This compound shows promising utility in the investigation of cardiovascular, pro-inflammatory, migraine, and metabolic conditions [1] [2] [3].
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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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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.
7-10 days
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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.
- $98
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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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Ubrogepant
T171941374248-77-7
Ubrogepant (MK-1602) is an antagonist of calcitonin gene-related peptide receptor that can be used in the acute treatment of migraine studies.
- $155
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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.
- $288
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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.
- $198
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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).
- $31
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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).
- $890
35 days
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