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 a 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-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-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-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-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-115645
    R121919 hydrochloride
    		Antagonist
    R121919 (NBI30775) hydrochloride is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 hydrochloride has antidepressant and anxiolytic effects. R121919 hydrochloride alleviates defensive withdrawal in rats.
    R121919 hydrochloride
  • HY-120564
    BMS-763534
    		Antagonist
    BMS-763534 is a CRF1 antagonist that inhibits neurological disorders such as depression and anxiety..
    BMS-763534
  • HY-110056
    NBI 35965 hydrochloride
    		Antagonist
    NBI 35965 hydrochloride 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 hydrochloride does not inhibit CRF2. NBI 35965 hydrochloride reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 hydrochloride shows anxiolytic effects.
    NBI 35965 hydrochloride
  • 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-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-P1295
    Urocortin, human
    		Agonist 98.98%
    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-113603
    Tildacerfont
    		Inhibitor 98.25%
    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
  • 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-P1294
    α-Helical CRF(9-41)
    		Modulator 99.74%
    α-Helical CRF(9-41) is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) is also a partial agonist of CRF1 receptor with an EC50 of 140 nM.
    α-Helical CRF(9-41)
  • 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-P1296
    Urocortin, rat
    		Agonist 98.50%
    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
  • HY-P3684A
    [DPro5] Corticotropin Releasing Factor, human, rat TFA
    		Agonist 99.71%
    [DPro5] Corticotropin Releasing Factor, human, rat TFA is a selective corticotropin releasing factor/hormone R2 (CRH-R2)agonist. [DPro5] Corticotropin Releasing Factor, human, rat TFA fails to cause the typical anxiogenic effect, but modulates learning and memory processes in rat.
    [DPro5] Corticotropin Releasing Factor, human, rat TFA
  • HY-12131
    DMP 696
    		Antagonist 99.03%
    DMP 696 is a selective corticotropin-releasing hormone receptor 1 (CRHR1) antagonist, used for the treatment of anxiety and depression.
    DMP 696
CRFR Isoform Comparison

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