CGRP Receptor

CGRP receptor antagonists block the receptor for calcitonin gene-related peptide (CGRP), a neuropeptide. In 1982 alternative RNA processing of the calcitonin gene was shown to produce CGRP in neural tissue. The receptor is formed by calcitonin receptor-like receptor (CALCRL) together with receptor activity-modifying protein 1 (RAMP1), as described in 1998. CGRP release from trigeminal neurons is studied in migraine models and in neurogenic vasodilation. Olcegepant, telcagepant, MK-3207 and ubrogepant are small-molecule antagonists of this receptor complex. CGRP 8-37 (human) is a truncated peptide antagonist, and α-CGRP(human) serves as the native agonist.

Items 26-50 of 52

  • CTR/AMYR agonist-1 enantiomer
    Cat. No.
    A58891

    CTR/AMYR agonist-1 enantiomer

    CTR/AMYR agonist-1 enantiomer is a potent agonist of the calcitonin receptor (CTR) and amylin receptor (AMYR), exhibiting EC50 values between 0.56 and 6.9 nM. This compound plays a crucial role in the study of metabolic diseases, facilitating research into the regulation of energy metabolism and glucose homeostasis. Its high specificity and efficacy make it an essential tool for investigating therapeutic targets within the CTR/AMYR signaling pathways.

    Out of stock

    All 3 sizes
  • CTR/AMYR activator-1
    Cat. No.
    A58892

    CTR/AMYR activator-1

    CTR/AMYR activator-1 is a potent activator of the CTR and AMYR pathways. This compound plays a significant role in modulating physiological processes related to bone health, metabolism, cardiovascular function, and neurodegeneration. It is a valuable tool for researchers investigating the underlying mechanisms of these diseases and for potential therapeutic development.

    Out of stock

    All 3 sizes
  • CTR/AMYR agonist-1
    Cat. No.
    A58893

    CTR/AMYR agonist-1

    CTR/AMYR agonist-1 is a selective agonist for the Calcitonin Receptor (CTR) and Amylin Receptor (AMYR), exhibiting EC50 values ranging from 0.56 to 6.9 nM. This compound is instrumental in studying metabolic diseases, particularly in understanding the receptor-mediated pathways involved in energy homeostasis and glucose metabolism. Its high potency makes it a valuable tool for elucidating the physiological roles of CTR and AMYR in various biological contexts.

    Out of stock

    All 3 sizes
  • α-CGRP (mouse, rat)
    Cat. No.
    A59606

    α-CGRP (mouse, rat)

    Synonyms: CGRP (83-119); mouse; rat

    α-CGRP (mouse, rat) is a neuropeptide that primarily targets the neuromuscular junction and functions as a potent vasodilator. It is known to induce a decrease in blood pressure and an increase in heart rate upon peripheral administration, and it also promotes relaxation of colonic smooth muscle. This peptide is valuable for research applications in cardiovascular studies, pro-inflammatory responses, migraine pathophysiology, and metabolic processes.

    0.1 mg
    $20.00
    1 mg
    $130.00
    All 3 sizes
  • Vazegepant hydrochloride
    Cat. No.
    A59607

    Vazegepant hydrochloride

    Synonyms: Zavegepant (hydrochloride); BHV-3500 (hydrochloride)

    Vazegepant hydrochloride is a potent antagonist of the calcitonin gene-related peptide (CGRP) receptor, exhibiting a high binding affinity with a Ki value of 0.023 nM. This compound represents the first intranasal formulation in the gepant class, specifically developed for the acute management of migraine. Additionally, Vazegepant hydrochloride shows potential in addressing pulmonary inflammation associated with COVID-19, enabling further research into its therapeutic applications in these areas.

    1 mg
    $85.00
    5 mg
    $160.00
    All 6 sizes
  • β-CGRP, human
    Cat. No.
    A59609

    β-CGRP, human

    Synonyms: Human β-CGRP; CGRP-II (Human)

    β-CGRP, human is a member of the calcitonin peptide family and functions through binding to the calcitonin-receptor-like receptor (CRLR) in conjunction with receptor-activity-modifying proteins (RAMPs). It exhibits high affinity, with IC50 values of 1 nM for the CRLR/RAMP1 complex and 300 nM for the CRLR/RAMP2 complex in cellular assays. This peptide is crucial for research in pain modulation, migraine mechanisms, and neurobiological studies.

    0.5 mg
    $120.00
    1 mg
    $175.00
    All 3 sizes
  • Atogepant
    Cat. No.
    A59610

    Atogepant

    Synonyms: MK-8031; AGN-241689

    Atogepant is a selective antagonist of the calcitonin gene-related peptide (CGRP) receptor, exhibiting potent oral bioavailability. It is primarily utilized in research related to migraine pathophysiology and therapeutic interventions, contributing to the understanding of CGRP’s role in migraine mechanisms. This compound enables detailed investigations into migraine relief strategies targeting CGRP signaling pathways.

    1 mg
    $125.00
    5 mg
    $230.00
    All 7 sizes
  • Vazegepant
    Cat. No.
    A59611

    Vazegepant

    Synonyms: Zavegepant; BHV-3500

    Vazegepant is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist. It selectively inhibits the CGRP receptor, thereby modulating pain pathways associated with migraine. This compound is valuable for research on migraine treatments and the role of CGRP in nociceptive signaling.

    1 mg
    $80.00
    5 mg
    $195.00
    All 6 sizes
  • Adrenomedullin (1-50), rat
    Cat. No.
    A59614

    Adrenomedullin (1-50), rat

    Synonyms: Adrenomedullin (rat)

    Adrenomedullin (1-50), rat is a 50 amino acid peptide that functions as a CGRP receptor activator. It is known to induce selective arterial vasodilation, making it relevant for research in cardiovascular physiology and pathophysiology. This peptide is utilized in studies investigating the role of adrenomedullin in vascular regulation and its potential therapeutic applications in hypertension and related disorders.

    0.5 mg
    $200.00
    1 mg
    $280.00
    All 3 sizes
  • Rimegepant sulfate hydrate
    Cat. No.
    A59616

    Rimegepant sulfate hydrate

    Synonyms: BMS-927711 sulfate hydrate; BHV-3000 sulfate hydrate

    Rimegepant sulfate hydrate is a potent, orally active, selective antagonist of the calcitonin gene-related peptide (CGRP) receptor. It exhibits a binding affinity with a Ki of 0.027 nM and an IC50 of 0.14 nM for the human CGRP receptor. This compound is primarily utilized in migraine research, contributing to studies focused on novel therapeutic approaches for migraine management.

    5 mg
    $100.00
    10 mg
    $150.00
    All 5 sizes
  • Adrenomedullin (16-31), human
    Cat. No.
    A59618

    Adrenomedullin (16-31), human

    Adrenomedullin (16-31), human is a peptide fragment comprising amino acid residues 16-31 of human adrenomedullin (hADM). This analog exhibits significant affinity for the CGRP1 receptor, influencing cardiovascular regulation. It has been shown to elicit pressor activity in the systemic vascular bed of rats, making it a valuable tool for exploring vascular responses and related research applications.

    5 mg
    $205.00
    10 mg
    $355.00
    All 2 sizes
  • HTL22562
    Cat. No.
    A59619

    HTL22562

    HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist that plays a significant role in the study of migraine pathology. It effectively inhibits CGRP receptor activity, which is critical for understanding migraine mechanisms and developing therapeutic strategies. HTL22562 is primarily used in acute research settings to explore the implications of CGRP signaling in headache disorders.

    25 mg
    $2,740.00
    All 1 sizes
  • CGRP antagonist 7
    Cat. No.
    A59620

    CGRP antagonist 7

    CGRP Antagonist 7 is a highly potent calcitonin gene-related peptide (CGRP) receptor antagonist, exhibiting a Ki value of 0.029 nM. This compound effectively inhibits the production of cyclic adenosine monophosphate (cAMP) with an IC50 of 1.5 nM. CGRP Antagonist 7 is primarily utilized in research focused on migraine pathophysiology and therapeutic interventions targeting CGRP signaling pathways.

    Out of stock

    All 3 sizes
  • MK-8825
    Cat. No.
    A59621

    MK-8825

    MK-8825 is a selective antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating a Ki value of 47 pM for human and 17 nM for rat receptors. It effectively inhibits CGRP-mediated cAMP responses, showcasing competitive antagonism. This compound is valuable for research into migraine and temporomandibular joint disorders, contributing to the understanding of therapeutic targets in these conditions.

    25 mg
    $2,535.00
    50 mg
    $3,265.00
    All 3 sizes
  • Rimegepant hemisulfate
    Cat. No.
    A59622

    Rimegepant hemisulfate

    Synonyms: BMS-927711 hemisulfate; BHV-3000 hemisulfate

    Rimegepant hemisulfate is a selective and competitive antagonist of the calcitonin gene-related peptide (CGRP) receptor, exhibiting a Ki value of 0.027 nM and an IC50 of 0.14 nM for the human CGRP receptor. This compound demonstrates potent biological activity in blocking CGRP signaling pathways, making it a valuable tool for migraine research and the investigation of related neurological conditions. Its oral bioavailability supports its application in in vivo studies focused on migraines and CGRP-mediated mechanisms.

    Out of stock

    All 3 sizes
  • Desfluoro-BMS-694153
    Cat. No.
    A59623

    Desfluoro-BMS-694153

    Desfluoro-BMS-694153 is a potent antagonist of the calcitonin gene-related peptide (CGRP) receptor, with a Ki value of 0.01 nM. This compound exhibits minimal risk of CYP3A4 inhibition, demonstrated by IC50 values of 36 μM for CYP3A4-BFC and 6 μM for CYP3A4-BZR. Desfluoro-BMS-694153 is primarily utilized in research focused on migraine pathophysiology and the exploration of therapeutic interventions targeting CGRP pathways.

    Out of stock

    All 3 sizes
  • Adrenotensin (human)
    Cat. No.
    A59625

    Adrenotensin (human)

    Synonyms: Pro-ADM-153-185 (human)

    Adrenotensin (human), a fragment of pro-adrenomedullin, corresponds to amino acids 153-185 of the precursor peptide. As a member of the calcitonin gene-related peptide (CGRP) superfamily, Adrenomedullin (ADM) functions as a multifunctional vasoactive hormone. This fragment is relevant for research applications targeting cardiovascular physiology, cellular signaling, and pathophysiological processes associated with ADM.

    Out of stock

    All 3 sizes
  • BMS-846372
    Cat. No.
    A59626

    BMS-846372

    BMS-846372 is a potent oral antagonist of the calcitonin gene-related peptide (CGRP), exhibiting a Ki value of 0.07 nM. This compound is primarily utilized in research studies focused on migraine pathophysiology and may aid in the development of therapeutic strategies for migraine management.

    Out of stock

    All 3 sizes
  • CGRP antagonist 2
    Cat. No.
    A59628

    CGRP antagonist 2

    CGRP Antagonist 2 is a competitive antagonist of the calcitonin gene-related peptide (CGRP) receptor. It effectively inhibits CGRP-mediated signaling, which is crucial for the modulation of nociceptive pathways associated with pain perception. This reagent is widely utilized in research focused on migraine mechanisms and pain management therapies.

    1 mg
    $290.00
    5 mg
    $1,065.00
    All 5 sizes
  • Calcitonin Gene Related Peptide II (rat)
    Cat. No.
    A59629

    Calcitonin Gene Related Peptide II (rat)

    Synonyms: CGRP II (rat)

    Calcitonin Gene Related Peptide II (rat) is a CGRP receptor activator that functions as a potent and enduring vasodilator. It plays a crucial role in the regulation of vascular tone and blood pressure. This peptide is utilized in research on cardiovascular diseases, aiding in the exploration of therapeutic strategies for conditions such as hypertension and vascular dysfunction.

    Out of stock

    All 3 sizes
  • Calcitonin (salmon) (acetate)
    Cat. No.
    A59630

    Calcitonin (salmon) (acetate)

    Synonyms: Salmon calcitonin acetate

    Calcitonin (salmon) (acetate) functions as a calcitonin gene-related peptide (CGRP) receptor agonist. This compound stimulates bone formation while inhibiting bone resorption, making it valuable for research in osteoporosis and other bone-related disorders. The acetate form enhances the absorption and bioactivity of the peptide, providing a more effective hormonal intervention for studies focusing on bone metabolism and calcium homeostasis.

    Out of stock

    All 3 sizes
  • Adrenomedullin (11-50), rat
    Cat. No.
    A59632

    Adrenomedullin (11-50), rat

    Adrenomedullin (11-50), rat is a bioactive peptide fragment that represents the C-terminal portion of rat adrenomedullin. This compound primarily targets CGRP1 receptors, effectively inducing selective arterial vasodilation. Its key biological activity makes it useful in cardiovascular research, particularly in studies focusing on vascular function and regulation.

    Out of stock

    All 3 sizes
  • BMS-694153
    Cat. No.
    A59633

    BMS-694153

    BMS-694153 is a potent antagonist of the human calcitonin gene-related peptide receptor (CGRP receptor). This compound exhibits significant biological activity in blocking CGRP-mediated signaling pathways, making it a valuable tool for migraine research. It is particularly effective in studies examining intranasal delivery methods for rapid therapeutic intervention in migraine treatment.

    25 mg
    $5,085.00
    50 mg
    $6,525.00
    All 3 sizes
  • Telcagepant-d8
    Cat. No.
    A59634

    Telcagepant-d8

    Synonyms: MK-0974-d8

    Telcagepant-d8 is a deuterium-labeled variant of Telcagepant, a potent orally active antagonist of the calcitonin gene-related peptide (CGRP) receptor. This compound exhibits binding affinities (Kis) of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively. Telcagepant-d8 is primarily utilized in pharmacokinetic studies and metabolic research, providing a valuable tool for investigating CGRP-related pathways and receptor interactions in various biological systems.

    Out of stock

    All 3 sizes
  • ω-Agatoxin IVA
    Cat. No.
    A66085

    ω-Agatoxin IVA

    ω-Agatoxin IVA is a highly selective blocker of P/Q type calcium channels (Cav2.1), with IC50 values of 2 nM and 90 nM. This compound effectively inhibits glutamate exocytosis and calcium influx triggered by elevated potassium levels. Additionally, ω-Agatoxin IVA suppresses capsaicin-induced CGRP release and associated vasodilation. It is valuable for investigations into neurological and cardiovascular diseases, contributing to the understanding of calcium channel modulation in these contexts.

    0.01 mg
    $20.00
    0.1 mg
    $150.00
    All 6 sizes

Items 26-50 of 52

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