1. GPCR/G Protein
    Neuronal Signaling
  2. CGRP Receptor

CGRP Receptor

CGRP receptor is a heterotrimer: a large peptide with 7 transmembrane domains, named calcitonin receptor-like receptor (CLR or CRLR), is supplemented by a small single transmembrane peptide, named receptor activity-modifying protein (RAMP1) that forms the CGRP-specific ligand binding site. CGRP receptors are expressed by multiple different cell types within the nervous, cardiovascular and immune systems that are thought to play important roles in migraine pathology: on cerebral vascular smooth muscle, where they cause vasodilation, on dural mast cells triggering their degranulation, at the central terminals of the trigeminal nerve, where CGRP is a neuromodulator at second-order nociceptive neurons in the spinal trigeminal nucleus caudalis and in the dorsal horn of the spinal cord, where CGRP has a similar role in inducing central sensitisation to tactile stimuli. CGRP is produced in both peripheral and central neurons. It is a potent peptide vasodilator and can function in the transmission of pain.

CGRP Receptor 相关产品 (16):

Cat. No. Product Name Effect Purity
  • HY-10095
    Olcegepant Antagonist 99.32%
    Olcegepant是有效和选择性的降钙素基因相关肽1 (CGRP1) 受体 拮抗剂,IC50Ki 分别为0.03 nM,14.4 pM。
  • HY-15498
    Rimegepant Antagonist 99.08%
    Rimegepant (BMS-927711) 是一种有效的降钙素基因相关肽 (CGRP) 受体拮抗剂,Ki 为 0.027 nM。
  • HY-10302
    MK-3207 Hydrochloride Antagonist 98.07%
    MK-3207 Hydrochloride 是一种有效的,可口服的 CGRP receptor 拮抗剂,IC50 值为 0.12 nM,Ki 值为 0.024 nM。
  • HY-32709
    Telcagepant Antagonist 99.07%
    Telcagepant (MK-0974) 是降钙素基因相关肽 (CGRP) 受体拮抗剂,与人和恒河猴CGRP结合的Ki分别为0.77 nM 和 1.2 nM。
  • HY-10095A
    Olcegepant hydrochloride Antagonist
    Olcegepant hydrochloride (BIBN4096BS hydrochloride) 是高效选择性的降钙素基因相关肽 (CGRP) 的拮抗剂, 对人类CGRP的Ki值为14.4 pM。
  • HY-P1548A
    β-CGRP, human TFA
    β-CGRP, human TFA 是一种降钙素肽,通过降钙素受体样受体 CRLRRAMP 的复合物起作用,在细胞体系中,对 CRLR/RAMP1 和 CRLR/RAMP2 的 IC50 值分别为 1 nM 和 300 nM。
  • HY-P1014
    HCGRP-(8-37) Antagonist 98.28%
    HCGRP-(8-37) 是人降钙素基因相关肽 (hCGRP) 片段,也是 CGRP 受体的拮抗剂。
  • HY-P0209
    Rat CGRP-(8-37) Antagonist 98.29%
    Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) 是高度选择的 CGRP receptor 拮抗剂。
  • HY-P1548
    β-CGRP, human
    β-CGRP, human 是一种降钙素肽,通过降钙素受体样受体 CRLRRAMP 的复合物起作用,在细胞体系中,对 CRLR/RAMP1 和 CRLR/RAMP2 的 IC50 值分别为 1 nM 和 300 nM。
  • HY-P1462A
    Calcitonin Gene Related Peptide (CGRP) (83-119), rat TFA Modulator
    Calcitonin Gene Related Peptide (CGRP) (83-119), rat (TFA) 是一种由 37 个氨基酸组成的降钙素家族神经肽,通过 (CRLR) 起作用。
  • HY-10301
    MK-3207 Antagonist
    MK-3207是口服生物相容性的CGRP受体拮抗剂,IC50和Ki分别为0.12 nM和0.024 nM,对AM1,AM2,CTR和AMY3的抑制性较弱。
  • HY-112262
    CGRP antagonist 1 Antagonist
    CGRP antagonist 1是高效的 CGRP 受体拮抗剂,KiIC50 值分别为35 和 57 nM。
  • HY-P1534
    Adrenomedullin (1-50), rat Activator
    Adrenomedullin (1-50), rat 是由 50 个氨基酸组成的多肽,能够通过激活 CGRP1 受体来诱导动脉血管舒张。
  • HY-P1471
    Adrenomedullin (AM) (22-52), human Antagonist
    Adrenomedullin (AM) (22-52), human 为肾上腺髓质素 (adrenomedullin receptor) 受体拮抗剂,同时在猫后肢血管床中,对降钙素基因相关肽 (CGRP) 受体也具有拮抗作用。
  • HY-P1462
    Calcitonin Gene Related Peptide (CGRP) (83-119), rat Agonist
    Calcitonin Gene Related Peptide (CGRP) (83-119), rat 是一种由 37 个氨基酸组成的降钙素家族神经肽,通过 (CRLR) 起作用。
  • HY-12366
    Ubrogepant Antagonist
    Ubrogepant (MK-1602) 是一种新型口服降钙素基因相关肽受体 (CGRP) 拮抗剂,正在开发治疗急性偏头痛。
Isoform Specific Products

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