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-103377
    Antalarmin hydrochloride
    Antagonist 99.87%
    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
  • HY-P0060
    Tetracosactide
    99.91%
    Tetracosactide (Tetracosactrin) is an analogue of adrenocorticotrophic hormone (ACTH), Tetracosactide can stimulate the release of corticosteroids such as cortisol from the adrenal gland. Tetracosactide is currently used for the research of ulcerative colitis and Crohn's disease, juvenile/adult rheumatoid arthritis and osteoarthrosis.
    Tetracosactide
  • HY-14127
    R121919
    Antagonist 99.53%
    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
  • HY-135542
    NBI-27914
    Antagonist 99.82%
    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
  • HY-P1295
    Urocortin, human
    Agonist 99.12%
    Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF and mCRF, respectively.
    Urocortin, human
  • HY-123677
    E2508
    Antagonist
    E2508 is an orally active corticotropin-releasing factor 1 (CRF1) receptor antagonist with a Ki value of 11 nM for hCRF1.
    E2508
  • HY-105332
    CRA1000
    Antagonist
    CRA1000 is an orally active, selective and competitive CRF1 receptor antagonist with anxiolytic- and antidepressant-like properties.
    CRA1000
  • 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-14875
    Verucerfont
    Antagonist 99.51%
    Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000?nM for CRF1, CRF2, and CRF-BP, respectively.
    Verucerfont
  • HY-P1533A
    CRF, bovine TFA
    Agonist 98.10%
    CRF, bovine (TFA) is a potent agonist of CRF receptor, and displaces [125I-Tyr]ovine CRF with a Ki of 3.52 nM.
    CRF, bovine TFA
  • HY-P2287
    Cortagine
    Agonist 99.53%
    Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an EC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive agent in the mouse model.
    Cortagine
  • HY-P0257
    Astressin
    Antagonist 98.93%
    Astressin is a potent corticotropin releasing factor (CRF) antagonist.
    Astressin
  • HY-P1107A
    Antisauvagine-30 TFA
    Antagonist 98.10%
    Antisauvagine-30 TFA (aSvg-30 TFA) is a potent, highly selective and competitive CRF2 receptor peptidic antagonist. Antisauvagine-30 TFA exhibits a Kd of 1.4 nM and 150 nM for mCRFR2β and CRFR1, respectively.
    Antisauvagine-30 TFA
  • HY-14130
    CP 376395
    Antagonist 99.68%
    CP 376395 is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist.
    CP 376395
  • HY-12127
    Pexacerfont
    Antagonist 99.97%
    Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1±0.6 nM for human CRF1 receptor.
    Pexacerfont
  • HY-P1368A
    Stressin I TFA
    Agonist 98.38%
    Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) TFA is a potent CRF1 receptor selective agonist, Ki is 1.7 nM. Stressin I induces an increase in adrenocorticotropic hormone (ACTH) levels in rats.
    Stressin I TFA
  • HY-P1858A
    Urocortin III, mouse TFA
    Activator
    Urocortin III, mouse TFA 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 TFA
  • HY-P1298A
    Sauvagine TFA
    Agonist 98.76%
    Sauvagine TFA, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine TFA is effective at releasing ACTH from rat pituitary cells. Sauvagine TFA possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
    Sauvagine TFA
  • HY-P1296
    Urocortin, rat
    Agonist
    Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF and mouse CRF, respectively.
    Urocortin, rat
  • HY-124475
    Antalarmin
    Antagonist
    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

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