1. Vías de señalización
  2. GPCR/G Protein
    Neuronal Signaling
  3. CGRP Receptor

CGRP Receptor

Calcitonin gene-related peptide receptor

CGRP receptor is a heterodimer formed by calcitonin-receptor-like receptor (CRLR), a type II (family B) G-protein-coupled receptor, and receptor-activity-modifying protein 1 (RAMP1), a single-membrane-pass protein. RAMP1 is needed for CGRP binding and also cell-surface expression of CLR. CLR is an example of a family B GPCR.

CGRP is a neuropeptide abundant in the trigeminal system and widely expressed in both the peripheral and central nervous systems. CGRP has several functions including vasodilation, the perception of painful stimuli, and inflammation. CGRP exerts its biological action by interacting with its receptors. There are two types of CGRP receptors, CGRP-A and CGRP-B.

Cat. No. Nombre del producto Efecto Pureza Chemical Structure
  • HY-127141
    Cizolirtine citrate
    Agonist
    Cizolirtine citrate (E-4018) is an analgesic agent. Cizolirtine citrate has significant analgesic and anti-hyperalgesic action in neuropathic pain models.
    Cizolirtine citrate
  • HY-P1471A
    Adrenomedullin (AM) (22-52), human TFA
    Antagonist
    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.
    Adrenomedullin (AM) (22-52), human TFA
  • HY-P2601A
    Tyr-α-CGRP (human) TFA
    Tyr-α-CGRP (human) TFA is an N-terminally extended human α-CGRP analog. Tyr-α-CGRP (human) TFA can bind to membrane preparations from rat brain and spleen with IC50 values of 0.2 nM and 0.5 nM, respectively, and induce positive chronotropic and inotropic effects in isolated guinea pig right and left atria with EC50 values of 282 nM and 74 nM, respectively. Tyr-α-CGRP (human) TFA also inhibits contractile responses in rat vas deferens with an EC50 value of 1.9 nM.
    Tyr-α-CGRP (human) TFA
  • HY-180955
    Desfluoro-BMS-694153
    Antagonist
    Desfluoro-BMS-694153 (Compound 3) is a calcitonin gene-related peptide receptor (CGRP receptor) antagonist, with a Ki 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.
    Desfluoro-BMS-694153
  • HY-114613
    D-Trp-Aib
    D-Trp-Aib is a dipeptide and amyloid-β inhibitor with a Kd of 29.6 nM. D-Trp-Aib triggers formation of non-toxic, non-β-sheet, amorphous amyloid β clusters from misfolded amyloid β monomers and toxic amyloid β oligomers, and reduces toxic amyloid β1-42 deposits. D-Trp-Aib inhibits amyloid fibril formation of α‑synuclein, IAPP and calcitonin. D-Trp-Aib can be used for the research of Alzheimer's disease.
    D-Trp-Aib
  • HY-P1548B
    β-CGRP, human acetate
    β-CGRP, human acetate (Human β-CGRP acetate) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells.
    β-CGRP, human acetate
  • HY-103303
    CRSP-1
    Activator
    CRSP-1 is short for calcitonin receptor-stimulating peptide-1. CRSP-1 inhibits osteoclast formation by inhibiting the formation and activity of multinucleated osteoclast.
    CRSP-1
  • HY-P3919
    Adrenotensin (human)
    Adrenotensin (human) (Pro-ADM-153-185 (human)) is a 153-185 fragment of precursor peptide of Adrenomedullin. Adrenomedullin (ADM) is a 52-amino acid multifunctional peptide, which belongs to the CGRP superfamily of vasoactive peptide hormones.
    Adrenotensin (human)
  • HY-109022A
    (3R,5R,6S)-Atogepant
    Antagonist 99.55%
    (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.
    (3R,5R,6S)-Atogepant
  • HY-12367
    BMS-846372
    Antagonist
    BMS-846372 (Compound 5) is an orally active CGRP antagonist (Ki = 0.07 nM). BMS-846372 may be used in migraine research.
    BMS-846372
  • HY-P11843
    TPM004
    Agonist
    TPM004 is an ultralong-acting, nonaggregating dual amylin (AMY3R) and calcitonin receptor (CTR) agonist with EC50 values of 0.5 and 0.7 pM. TPM004 induces weight loss, attenuates adiposity rebound, lowers glucose, and improves glucose homeostasis. TPM004 can be used for the research of obesity, diabetes.
    TPM004
  • HY-120657R
    9-PAHSA (Standard)
    Agonist
    Flumethrin (Standard) is the analytical standard of Flumethrin. This product is intended for research and analytical applications. 9-PAHSA is an orally active endogenous GPR120 agonist (EC50=18 μM). 9-PAHSA significantly inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway. 9-PAHSA induces adipocyte browning, enhances glucose uptake and reduces lipid accumulation, while improving mitochondrial function and the survival rate of steatotic hepatocytes. In terms of neuroprotection, 9-PAHSA regulates the expression of REST and BDNF in the prefrontal cortex of diabetic mice, and effectively prevents spatial working memory deficits and abnormal social behaviors. 9-PAHSA does not directly regulate insulin secretion or improve systemic insulin sensitivity, and possesses specific anti-inflammatory, metabolic regulatory and neuroprotective properties. 9-PAHSA can be used in the research of diabetes-related cognitive impairment, obesity and non-alcoholic fatty liver disease.
    9-PAHSA (Standard)
  • HY-P11584
    KBP-066A
    Agonist
    KBP-066A is a long-acting dual amylin and calcitonin receptor agonist. KBP-066A can activate the CTR and AMY-R potently, with no off-target activity. KBP-066A reduces fasting blood glucose levels, fasting insulin levels, and body weight in diabetic rat models. KBP-066A can be used for the research of type 2 diabetes mellitus, obesity.
    KBP-066A
  • HY-182539
    DD04107
    Modulator
    DD04107 is a neuronal exocytosis inhibitor with a rat Syt1-C2B domain binding Ka of 2.4 μM. DD04107 interferes with synaptobrevin-syntaxin-SNAP-25 complex formation and Syt1-SNARE complex interaction to block α-calcitonin gene-related peptide (α-CGRP) exocytotic release from primary sensory neurons. DD04107 blocks inflammatory ion channel recruitment to nociceptor plasma membranes. DD04107 can be used for the research of chronic inflammatory pain, neuropathic pain, osteosarcoma pain, chemotherapy-induced peripheral neuropathy, diabetic neuropathy, inflammatory pain.
    DD04107
  • HY-P4766
    Adrenomedullin (porcine)
    Adrenomedullin (porcine) is a peptide that regulates vasodilation. Adrenomedullin (porcine) induces endothelium-dependent relaxation in rat aorta with IC50 value of 2.4 nM. Adrenomedullin (porcine) induces endothelium-independent relaxation of porcine coronary arteries with an IC50 of 27.6 nM.
    Adrenomedullin (porcine)
  • HY-185234A
    (R)-CTR/AMYR activator-1
    Activator
    (R)-CTR/AMYR activator-1 (Compound 122) is a CTR/AMYR activator with EC50 values of 0.8 and 0.73 nM. (R)-CTR/AMYR activator-1 can used for the researches of bone diseases, metabolic diseases, cardiovascular diseases, and neurodegenerative diseases.
    (R)-CTR/AMYR activator-1
  • HY-P1770A
    Adrenomedullin (16-31), human TFA
    Adrenomedullin (16-31), human TFA is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human TFA possesses pressor activity in the systemic vascular bed of the rat, but not the cat.
    Adrenomedullin (16-31), human TFA
  • HY-P1913
    Calcitonin Gene Related Peptide II (rat)
    Activator
    Calcitonin Gene Related Peptide II rat, a CGRP receptor activator, is a potent and long-lasting vasodilator. Calcitonin Gene Related Peptide II rat can be used in the research of cardiovascular diseases.
    Calcitonin Gene Related Peptide II (rat)
  • HY-162925
    CGRP antagonist 6
    Antagonist
    CGRP antagonist 6 (Compound 23) is a CGRP receptor antagonist (Ki: 0.84 nM). CGRP antagonist 6 can be used for research of migraine.
    CGRP antagonist 6
  • HY-P0090A
    Calcitonin (salmon) acetate
    Agonist
    Calcitonin (salmon) (acetate) is a dual-action amylin and calcitonin receptor agonist, can stimulate bone formation and inhibit bone resorption.The acetate form can affect the absorption and efficacy of hormones.
    Calcitonin (salmon) acetate
Cat. No. Nombre del producto / Synonyms Application Reactivity