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.

7 Items

  • KBP-089
    Cat. No.
    A58867

    KBP-089

    KBP-089 is a dual agonist of Amylin and Calcitonin receptors. This compound demonstrates significant biological activity by promoting weight reduction, decreasing adipose tissue mass, and enhancing glucose tolerance in obese rat models. Additionally, KBP-089 reduces lipid accumulation in both liver and muscle tissues while improving glycemic homeostasis and insulin sensitivity. It is particularly relevant for research focused on obesity and type 2 diabetes.

    Out of stock

    All 3 sizes
  • Petrelintide
    Cat. No.
    A58870

    Petrelintide

    Synonyms: ZP8396

    Petrelintide is a dual amylin and calcitonin receptor agonist (DACRA) that effectively modulates energy intake by selectively reducing high-fat diet consumption in diet-induced obese (DIO) rats. This compound promotes fat mass loss while preserving lean body mass throughout weight reduction processes. Petrelintide is valuable for research in diabetes and obesity, providing insights into the regulation of metabolic pathways associated with these conditions.

    1 mg
    $465.00
    5 mg
    $1,190.00
    All 3 sizes
  • Davalintide
    Cat. No.
    A58878

    Davalintide

    Davalintide is a potent agonist of the amylin receptor, calcitonin receptor, and calcitonin gene-related peptide (CGRP) receptor, demonstrating high affinity with IC50 values of 0.04 nM, 0.06 nM, and 3.1 nM, respectively. It effectively stimulates cyclic AMP production via the calcitonin receptor, with an EC50 of 1.4 nM. Davalintide has been shown to regulate blood glucose levels and body weight through mechanisms such as delaying gastric emptying, inhibiting glucagon secretion, and suppressing food intake. This peptide is valuable for research applications focused on obesity and diabetes management.

    1 mg
    $80.00
    5 mg
    $205.00
    All 4 sizes
  • Lenbelintide
    Cat. No.
    A58883

    Lenbelintide

    Lenbelintide is a dual amylin and calcitonin receptor agonist, designed to engage both receptor pathways. This compound has demonstrated significant biological activity in modulating metabolic processes, making it valuable for research focused on obesity and related metabolic disorders. Its unique mechanism offers insights into appetite regulation and energy expenditure, providing a promising avenue for therapeutic exploration in weight management research.

    1 mg
    $130.00
    5 mg
    $335.00
    All 5 sizes
  • 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 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
  • 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

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