1. Signaling Pathways
  2. GPCR/G Protein
  3. CRFR

CRFR

Corticotropin-releasing Factor Receptor; CRHR

The CRFR (Corticotropin-releasing Factor Receptor, CRHR) belongs to the G-coupled receptor superfamily. Two receptor subtypes, CRF1 receptor and CRF2 receptor, and several splice variants for both receptor subtypes have been discovered. CRF itself has a greater affinity for CRF1 receptors while urocortin 1 (Ucn 1) binds with high affinity to both receptors and Ucn 2 and Ucn 3 both preferentially bind to CRF2 receptors.

Two CRF receptor subtypes are encoded by distinct genes which exhibit diverse alternative pre-mRNA splicing patterns resulting in multiple variants derived from partial or total exon deletions or insertions. With regard to the nine human CRF1 variants, CRF1a-i, described, CRF1a being the main wild type functional receptor while the other isoforms may modulate CRF signaling. For the CRF2, three functionally active splice variants, CRF2a-c, have been described in humans.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P3685
    [Met(O)21] Corticotropin Releasing Factor, ovine
    Modulator
    [Met(O)21] Corticotropin Releasing Factor, ovine is a corticotropin releasing factor isolated from ovine hypothalamic extracts. Corticotropin releasing factor (CRF) is a hypothalamic hormone, which stimulates the secretion of adrenocorticotrophic hormone (ACTH).
    [Met(O)21] Corticotropin Releasing Factor, ovine
  • HY-103378
    NBI 35965 methanesulfonate
    Antagonist
    NBI 35965 methanesulfonate is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 methanesulfonate does not inhibit CRF2. NBI 35965 methanesulfonate reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 methanesulfonate shows anxiolytic effects.
    NBI 35965 methanesulfonate
  • HY-P1858
    Urocortin III, mouse
    Activator
    Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2. Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics.
    Urocortin III, mouse
  • HY-P1297A
    CRF(6-33)(human) TFA
    Inhibitor
    CRF(6-33)(human) TFA is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) TFA competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) TFA has anti-obesity effect.
    CRF(6-33)(human) TFA
  • HY-P1298
    Sauvagine
    Agonist
    Sauvagine, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine is effective at releasing ACTH from rat pituitary cells. Sauvagine possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
    Sauvagine
  • HY-P3130
    Stresscopin-related peptide (human)
    Stresscopin-related peptide (human) is a specific ligand for the type 2 CRH receptor. Stresscopin-related peptide (human) suppresses food intake, delayed gastric emptying and decreases heat-induced edema. Stresscopin-related peptide (human) maintains homeostasis after stress, and can be used in the research of stress-related diseases.
    Stresscopin-related peptide (human)
  • HY-P2829
    Stresscopin (human)
    Ligand
    Stresscopin (human) is a selective ligand of type 2 adrenocorticotropin-releasing hormone (CRH) receptors and can be used in the research of stress-related diseases.
    Stresscopin (human)
  • HY-113603S
    Tildacerfont-d8
    Tildacerfont-d8 (SPR001-d8) is a deuterium labeled Tildacerfont (HY-113603). Tildacerfont is a potent and orally active corticotrophin-releasing factor type 1 (CRF1) receptort antagonis. Tildacerfont effectively reduces adrenocorticotropic hormone (ACTH) and adrenal androgen levels. Tildacerfont has favourable safety profile. Tildacerfont can be used for researching congenital adrenal hyperplasia.
    Tildacerfont-d<sub>8</sub>
  • HY-P3019
    Urocortin III (human)
    Activator
    Urocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) selectively binds to type 2 CRF receptors with Ki values of 13.5, 21.7, and >100 nM for mCRF2β, rCRF2α, and hCRF1, respectively. Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion.
    Urocortin III (human)
  • HY-14127R
    R121919 (Standard)
    Antagonist
    R121919 (Standard) is the analytical standard of R121919. This product is intended for research and analytical applications. R121919 (NBI30775) is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 has antidepressant and anxiolytic effects. R121919 alleviates defensive withdrawal in rats.
    R121919 (Standard)
  • HY-103377R
    Antalarmin hydrochloride (Standard)
    Antagonist
    Antalarmin (hydrochloride) (Standard) is the analytical standard of Antalarmin (hydrochloride). This product is intended for research and analytical applications. Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome.
    Antalarmin hydrochloride (Standard)
  • HY-139035
    CRHR1 antagonist 1
    Antagonist
    CRHR1 antagonist 1 (compound 10a) is a non-peptide corticotropin-releasing hormone type 1 receptor (CRHR1) antagonist. CRHR1 antagonist 1 can be utilized in mental disorders research.
    CRHR1 antagonist 1
  • HY-12127R
    Pexacerfont (Standard)
    Antagonist
    Pexacerfont (Standard) is the analytical standard of Pexacerfont. This product is intended for research and analytical applications. Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1±0.6 nM for human CRF1 receptor.
    Pexacerfont (Standard)
  • HY-105332
    CRA1000
    Antagonist
    CRA1000 is an orally active, selective and competitive CRF1 receptor antagonist with anxiolytic- and antidepressant-like properties.
    CRA1000
  • HY-14128
    NBI-34041
    Antagonist
    NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC50 of 58.9 nM and a Ki of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.
    NBI-34041
  • HY-135542R
    NBI-27914 (Standard)
    Antagonist
    NBI-27914 (Standard) is the analytical standard of NBI-27914. This product is intended for research and analytical applications. NBI-27914 is a potent and selective antagonist of CRFR1. The CRF receptors, CRFR1 and CRFR2, are members of the G protein-coupled receptor superfamily.
    NBI-27914 (Standard)
  • HY-162872
    NBI-35965
    Antagonist
    NBI-35965 is an antagonist of corticotropin-releasing factor receptor 1 (CRF-R1). NBI-35965 can be used in nervous system related research.
    NBI-35965
  • HY-103375
    SN003
    Antagonist
    SN003 is a reversible antagonist of corticotropin releasing factor receptor 1 (CRFR 1) (IC50 = 241 nM) that displays more than 1000-fold selectivity over CRFR 2. SN003 suppresses CRF-induced ACTH release in vitro. SN003 attenuates depressive-like behavior in rat.
    SN003
  • HY-124475R
    Antalarmin (Standard)
    Antagonist
    Antalarmin (Standard) is the analytical standard of Antalarmin. This product is intended for research and analytical applications. Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier.
    Antalarmin (Standard)
  • HY-118821
    JTC-017
    Antagonist
    JTC-017, a specific corticotropin-releasing hormone receptor 1 antagonist, attenuates hippocampal noradrenaline release, visceral perception, adrenocorticotropic hormone release, and anxiety after acute colorectal distention in rats. JTC-017 blocks stress-induced changes in colonic motility after chronic colorectal distention in rats.
    JTC-017

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