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

CRFR

Corticotropin-releasing Factor Receptor; CRHR

CRFR

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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.

CRFR Isoform Specific Products:

CRFR Isoform Comparison
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, rCRF2α and mCRF2β, respectively.
    Urocortin, human
  • HY-P1245A
    Neuropeptide SF (human) acetate
    		Activator
    Neuropeptide SF (human) acetate augments paraventricular corticotrophin-releasing hormone (CRH) release and increases adrenocorticotropic hormone (ACTH) and corticosterone levels in the plasma. Neuropeptide SF (human) acetate play a physiologic role in the regulation of such circadian functions as the activity of motor centers and the HPA axis, through the release of CRH.
    Neuropeptide SF (human) acetate
  • 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-105332
    CRA1000
    		Antagonist
    CRA1000 is an orally active, selective and competitive CRF1 receptor antagonist with anxiolytic- and antidepressant-like properties.
    CRA1000
  • 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-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-124475
    Antalarmin
    		Antagonist 99.95%
    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
  • 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-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-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 CRF2α and mouse CRF2β, respectively.
    Urocortin, rat
CRFR Isoform Comparison

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