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Results for "

CGRP antagonists

" in MedChemExpress (MCE) Product Catalog:

By Targets:	CGRP Receptor (36) 5-HT Receptor (1) Amylin Receptor (2) Cytochrome P450 (1) Epigenetic Reader Domain (1) ERK (1) Isotope-Labeled Compounds (3) Reference Standards (4) TRP Channel (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (10) Endocrinology (2) Infection (1) Inflammation/Immunology (2) Neurological Disease (31)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Targets Recommended: CGRP Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10095

Olcegepant Maximum Cited Publications 42 Publications Verification BIBN-4096; BIBN 4096BS	CGRP Receptor	Neurological Disease
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the *calcitonin gene-related peptide 1 (CGRP1) receptor* with IC₅₀ of 0.03 nM and K_i of 14.4 pM for human CGRP .

HY-15498

Rimegepant 5+ Cited Publications BMS-927711; BHV-3000	CGRP Receptor	Neurological Disease
Rimegepant (BMS-927711) is an orally bioavailable and blood-brain barrier permeable antagonist of *CGRP* and AMY1 receptors, with a pIC₅₀ of 8.01 and a K_i of 0.027 nM for human *CGRP* receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at *CGRP* and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .

HY-12366

Ubrogepant MK-1602	CGRP Receptor	Cardiovascular Disease Neurological Disease
Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for *CGRP* receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by *α-CGRP*. Ubrogepant can be used in the study of acute migraine .

HY-109022

Atogepant MK-8031; AGN-241689	CGRP Receptor	Neurological Disease
Atogepant (MK-8031) is an orally active and selective calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine .

HY-10301

MK-3207 5 Publications Verification	CGRP Receptor	Neurological Disease
MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC₅₀=0.12 nM; K_i=0.024 nM). MK-3207 can be used for migraine studies .

HY-P1393

AC 187	Amylin Receptor	Endocrinology
AC 187 is a potent and orally active amylin receptor antagonist with an IC₅₀ of 0.48 nM and a K_i of 0.275 nM. AC 187 shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 has neuroprotective effects .

HY-P1471

Adrenomedullin (AM) (22-52), human 4 Publications Verification 22-52-Adrenomedullin (human)	CGRP Receptor	Cardiovascular Disease
Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .

HY-P0209

Rat CGRP-(8-37) Maximum Cited Publications 9 Publications Verification	CGRP Receptor	Cardiovascular Disease Neurological Disease
Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist.

HY-32709

Telcagepant 2 Publications Verification MK-0974	CGRP Receptor	Neurological Disease
Telcagepant (MK-0974) is an orally active *calcitonin gene-related peptide (CGRP) receptor* antagonist with K_is of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.

HY-10095A

Olcegepant hydrochloride Maximum Cited Publications 42 Publications Verification BIBN-4096 hydrochloride; BIBN4096BS hydrochloride	CGRP Receptor	Neurological Disease
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the *calcitonin gene-related peptide 1 (CGRP1) receptor* with IC₅₀ of 0.03 nM and with a K_i of 14.4 pM for human CGRP .

HY-134992

Vazegepant Zavegepant; BHV-3500	CGRP Receptor	Neurological Disease
Vazegepant (Zavegepant) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist. Vazegepant can be used in the study of migraine .

HY-P1014

HCGRP-(8-37) 2 Publications Verification Human α-CGRP (8-37)	CGRP Receptor	Cardiovascular Disease
HCGRP-(8-37) (Human α-CGRP (8-37)) is a fragment of human calcitonin gene-related peptide (hCGRP) and an antagonist of the *CGRP* receptor, with an IC₅₀ of 32.1 pM against the *CGRP* receptor. HCGRP-(8-37) blocks adenylate cyclase activation induced by *CGRP* receptor ligands and attenuates vascular responses triggered by *CGRP. HCGRP-(8-37) reduces capsaicin-induced vasodilation in porcine nasal mucosa and superficial skin. HCGRP-(8-37) serves as a research tool to distinguish effects mediated by CGRP* or calcitonin receptors, and to investigate *CGRP*-induced vascular effects .

HY-15498A

Rimegepant sulfate hydrate 5+ Cited Publications BMS-927711 sulfate hydrate; BHV-3000 sulfate hydrate	CGRP Receptor	Neurological Disease
Rimegepant (BMS-927711) sulfate hydrate is a potent, orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a K_i of 0.027 nM and an IC₅₀ of 0.14 nM for hCGRP receptor. Rimegepant sulfate hydrate can be used for migraine research .

HY-112262

CGRP antagonist 1	CGRP Receptor	Cardiovascular Disease Neurological Disease
CGRP antagonist 1 (compound 21) is a highly potent CGRP receptor antagonist with a K_i and an IC₅₀ of 1.7 nM and 5.7 nM, respectively .

HY-10302

MK-3207 Hydrochloride 5 Publications Verification	CGRP Receptor	Neurological Disease
MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC₅₀ of 0.12 nM and K_i of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.

HY-P1393A

AC 187 TFA	Amylin Receptor	Endocrinology
AC 187 TFA is a potent and orally active amylin receptor antagonist with an IC₅₀ of 0.48 nM and a K_i of 0.275 nM. AC 187 TFA shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 TFA has neuroprotective effects .

HY-117694

MK-8825	CGRP Receptor	Neurological Disease Inflammation/Immunology
MK-8825 is an orally active, selective *CGRP* receptor antagonist with a K_i value of 47 pM for human *CGRP* receptors and 17 nM for rat *CGRP* receptors. MK-8825 blocks *CGRP*-stimulated cAMP responses and exhibits competitive-like antagonism. MK-8825 can be used in the research of migraine and temporomandibular joint disorders .

HY-103304

SB 268262	Others	Neurological Disease
CGRP antagonist 4 is an antagonist of calcitonin gene-related peptide (CGRP) receptor. CGRP antagonist 4 shows the highest affinity for CGRP receptors in the human brain. CGRP antagonist 4 can be used to study the binding properties of non-peptide calcitonin gene-related peptide (CGRP) receptor antagonist (gepants) in rat, pig and human menes .

HY-124277

ADM 12	TRP Channel	Neurological Disease
ADM 12 is a highly selective transient receptor potential ankyrin 1 (TRPA1) channel antagonist. ADM 12 blocks nitroglycerin (NTG)-induced trigeminal hyperalgesia in animal models, reducing expression of pain-related genes (c-Fos, TRPA1) and neuropeptides (CGRP, SP). ADM_12 is promising for research of migraine and neuropathic pain .

HY-12367

BMS-846372	CGRP Receptor	Cardiovascular Disease
BMS-846372 (Compound 5) is an orally active *CGRP* antagonist (K_i = 0.07 nM). BMS-846372 may be used in migraine research .

HY-114945

CGRP antagonist 2	CGRP Receptor	Neurological Disease
CGRP antagonist 2 is a CGRP receptor antagonist. CGRP antagonist 2 can be used for pain relief .

HY-174986

CGRP antagonist 7	CGRP Receptor	Cardiovascular Disease
CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a K_i of 0.029 nM. CGRP antagonist 7 Inhibit the production of cyclic adenosine monophosphate (cAMP) with an IC₅₀ of 1.5 nM. CGRP antagonist 7 can be used for the study of migraine .

HY-145353

HTL22562	CGRP Receptor	Neurological Disease
HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist for acute research of migraine.

HY-12366R

Ubrogepant (Standard) MK-1602 (Standard)	CGRP Receptor Reference Standards	Cardiovascular Disease Neurological Disease
Ubrogepant (Standard) is the analytical standard of Ubrogepant. This product is intended for research and analytical applications. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for *CGRP* receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by *α-CGRP*. Ubrogepant can be used in the study of acute migraine .

HY-109022A

(3R,5R,6S)-Atogepant (3R,5R,6S)-MK-8031; (3R,5R,6S)-AGN-241689	CGRP Receptor	Neurological Disease
(3R,5R,6S)-Atogepant ((3R,5R,6S)-MK-8031) is the enantiomer of Atogepant (HY-109022). Atogepant is a calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.

HY-162925

CGRP antagonist 6	CGRP Receptor	Neurological Disease
CGRP antagonist 6 (Compound 23) is a CGRP receptor antagonist (K_i: 0.84 nM). CGRP antagonist 6 can be used for research of migraine .

HY-32709S

Telcagepant-d8 MK-0974-d₈	Isotope-Labeled Compounds CGRP Receptor	Neurological Disease
Telcagepant-d₈ (MK-0974-d₈) is deuterium labeled Telcagepant. Telcagepant (MK-0974) is an orally active *calcitonin gene-related peptide (CGRP) receptor* antagonist with K_is of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.

HY-12366S

Ubrogepant-d5 MK-1602-d₅	Isotope-Labeled Compounds CGRP Receptor	Cardiovascular Disease Neurological Disease
Ubrogepant-d₅ (MK-1602-d₅) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for *CGRP* receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by *α-CGRP*. Ubrogepant can be used in the study of acute migraine .

HY-114574

BMS-694153	CGRP Receptor	Neurological Disease
BMS-694153 is a potent antagonist of the human calcitonin gene-related peptide receptor (CGRP Receptor). BMS-694153 can be used for migraine with rapid and efficient intranasal exposure .

HY-134992S

(Rac)-Vazegepant-13C,d3	Isotope-Labeled Compounds	Others
(Rac)-Vazegepant- ¹³C,d₃ is the C13 and deuterium labeled (Rac)-Vazegepant. Vazegepant (HY-134992) is the first intranasal CGRP receptor antagonist for the study the acute research of migraine .

HY-P1471A

Adrenomedullin (AM) (22-52), human TFA 22-52-Adrenomedullin (human) TFA	CGRP Receptor	Cardiovascular Disease
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH₂ terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide *(CGRP)* receptor in the hindlimb vascular bed of the cat .

HY-179684

PCC0105005	CGRP Receptor 5-HT Receptor ERK Epigenetic Reader Domain	Neurological Disease
PCC0105005 is a dual-target CGRP Receptor antagonist (IC₅₀ = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC₅₀ = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine .

HY-183180

CGRP antagonist-8	CGRP Receptor	Neurological Disease
CGRP antagonist-8 is a CGRP receptor antagonist with an IC₅₀ of 2.7 nM. CGRP antagonist-8 can be used for the research of migraine .

HY-180955

Desfluoro-BMS-694153	CGRP Receptor Cytochrome P450	Neurological Disease
Desfluoro-BMS-694153 (Compound 3) is a calcitonin gene-related peptide receptor (CGRP receptor) antagonist, with a K_i value of 0.01 nM. Desfluoro-BMS-694153 has a significantly reduced risk of CYP3A4 inhibition, and its IC₅₀ values for CYP3A4-BFC and CYP3A4-BZR are 36 and 6 μM respectively. Desfluoro-BMS-694153 can be used for research on migraines .

HY-183181

CGRP antagonist-9	CGRP Receptor	Neurological Disease
CGRP antagonist-9 is a CGRP receptor antagonist with an IC₅₀ of 25 nM. It regulates the cAMP signaling pathway and can be used in migraine-related studies .

HY-10095R

Olcegepant (Standard) BIBN-4096 (Standard); BIBN 4096BS (Standard)	CGRP Receptor Reference Standards	Neurological Disease
Olcegepant (Standard) is the analytical standard of Olcegepant (HY-10095). This product is intended for research and analytical applications. Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP .

HY-132131

Vazegepant hydrochloride Zavegepant hydrochloride; BHV-3500 hydrochloride	CGRP Receptor	Infection Inflammation/Immunology
Vazegepant (BHV-3500) hydrochloride is a highly affinity *CGRP* receptor antagonist (hCGRP K_i= 0.023 nM). Vazegepant hydrochloride is the first intranasal gepant for migraine. Vazegepant hydrochloride may be helpful in effective management of COVID-19 associated pulmonary inflammation .

HY-15498B

Rimegepant hemisulfate BMS-927711 hemisulfate; BHV-3000 hemisulfate	CGRP Receptor	Neurological Disease
Rimegepant (BMS-927711) hemisulfate is a potent, orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a K_i of 0.027 nM and an IC₅₀ of 0.14 nM for hCGRP receptor. Rimegepant hemisulfate can be used for migraine research .

HY-109022R

Atogepant (Standard) MK-8031 (Standard); AGN-241689 (Standard)	Reference Standards CGRP Receptor	Neurological Disease
Atogepant (Standard) is the analytical standard of Atogepant (HY-109022). This product is intended for research and analytical applications. Atogepant (MK-8031) is an orally active and selective calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine .

HY-10302R

MK-3207 hydrochloride (Standard)	Reference Standards CGRP Receptor	Neurological Disease
MK-3207 hydrochloride (Standard) is the analytical standard of MK-3207 hydrochloride (HY-10302). This product is intended for research and analytical applications. MK-3207 hydrochloride is a potent and orally bioavailable CGRP receptor antagonist with IC₅₀ of 0.12 nM and K_i of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.

HY-183142

CLR/RAMP3-receptor antagonist-1	CGRP Receptor	Cancer
CLR/RAMP3-receptor antagonist-1 is a selective antagonist of the CLR/RAMP3 receptor (CLR/RAMP3, AM₂ receptor), with pIC₅₀ values of 5.86, 9.21 and 9.07 against AM₁ (CLR/RAMP2), AM₂ (CLR/RAMP3) and CGRP (CLR/RAMP1) receptors, respectively. CLR/RAMP3-receptor antagonist-1 reduces the levels of pancreatic cancer progression markers, induces apoptosis in vitro, and prolongs survival in mouse models of pancreatic cancer. CLR/RAMP3-receptor antagonist-1 can be used in pancreatic cancer-related research .

Cat. No.	Product Name	Target	Research Area

HY-P1393

AC 187	Amylin Receptor	Endocrinology
AC 187 is a potent and orally active amylin receptor antagonist with an IC₅₀ of 0.48 nM and a K_i of 0.275 nM. AC 187 shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 has neuroprotective effects .

HY-P1471

Adrenomedullin (AM) (22-52), human 4 Publications Verification 22-52-Adrenomedullin (human)	CGRP Receptor	Cardiovascular Disease
Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat .

HY-P0209

Rat CGRP-(8-37) Maximum Cited Publications 9 Publications Verification	CGRP Receptor	Cardiovascular Disease Neurological Disease
Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist.

HY-P1014

HCGRP-(8-37) 2 Publications Verification Human α-CGRP (8-37)	CGRP Receptor	Cardiovascular Disease
HCGRP-(8-37) (Human α-CGRP (8-37)) is a fragment of human calcitonin gene-related peptide (hCGRP) and an antagonist of the *CGRP* receptor, with an IC₅₀ of 32.1 pM against the *CGRP* receptor. HCGRP-(8-37) blocks adenylate cyclase activation induced by *CGRP* receptor ligands and attenuates vascular responses triggered by *CGRP. HCGRP-(8-37) reduces capsaicin-induced vasodilation in porcine nasal mucosa and superficial skin. HCGRP-(8-37) serves as a research tool to distinguish effects mediated by CGRP* or calcitonin receptors, and to investigate *CGRP*-induced vascular effects .

HY-P1393A

AC 187 TFA	Amylin Receptor	Endocrinology
AC 187 TFA is a potent and orally active amylin receptor antagonist with an IC₅₀ of 0.48 nM and a K_i of 0.275 nM. AC 187 TFA shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 TFA has neuroprotective effects .

HY-P1471A

Adrenomedullin (AM) (22-52), human TFA 22-52-Adrenomedullin (human) TFA	CGRP Receptor	Cardiovascular Disease
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH₂ terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide *(CGRP)* receptor in the hindlimb vascular bed of the cat .

Cat. No.	Product Name	Chemical Structure

HY-32709S

Telcagepant-d8
Telcagepant-d₈ (MK-0974-d₈) is deuterium labeled Telcagepant. Telcagepant (MK-0974) is an orally active *calcitonin gene-related peptide (CGRP) receptor* antagonist with K_is of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.

HY-12366S

Ubrogepant-d5

Ubrogepant-d₅ (MK-1602-d₅) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .

HY-134992S

(Rac)-Vazegepant-13C,d3
(Rac)-Vazegepant- ¹³C,d₃ is the C13 and deuterium labeled (Rac)-Vazegepant. Vazegepant (HY-134992) is the first intranasal CGRP receptor antagonist for the study the acute research of migraine .

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