2. GPCR/G Protein
  3. CRFR

CRFR

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 Related Products (54):

Cat. No. Product Name Effect Purity
  • 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.
  • 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[1].
  • 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[1].
  • 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[1][2][3].
  • 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[1][2][3].
  • 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[1][2].
  • 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[1][2][3].
  • 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[1][2].
  • HY-P1106
    K41498 Antagonist
    K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 can be used for hypotension study[1].
  • 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[1][2][3].
  • HY-P1294A
    α-Helical CRF(9-41) TFA Modulator 99.72%
    α-Helical CRF(9-41) TFA is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) TFA is also a partial agonist of CRF1 receptor with an EC50 of 140 nM[1][2].
  • 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[1][1].
  • HY-P1533
    CRF, bovine Agonist
    CRF, bovine is a potent agonist of CRF receptor, and displaces [125I-Tyr]ovine CRF with a Ki of 3.52 nM.
  • HY-103379
    CP 376395 hydrochloride Antagonist
    CP 376395 hydrochloride is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist[1][2].
  • HY-12339
    NVS-CRF38 Antagonist
    NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
  • HY-14132
    BMS-665053 Antagonist
    BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM)[1].
  • HY-P1297
    CRF(6-33)(human) Inhibitor 99.54%
    CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) has anti-obesity effect[1][2].
  • HY-P1298A
    Sauvagine TFA Agonist
    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[1][2][3].
  • HY-P1542
    Urotensin I Agonist
    Urotensin I (Catostomus urotensin I), a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively[1][2].
  • HY-P1107
    Antisauvagine-30 Antagonist
    Antisauvagine-30 (aSvg-30) is a potent, competitive and selective CRF2 receptor antagonist with Kd values of 1.4 nM and 153.6 nM for mouse CRF2β and rat CRF1 receptors, respectively[1].