1. GPCR/G Protein
  2. 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 (25):

Cat. No. Product Name Effect Purity
  • HY-14127
    R121919 Antagonist 99.84%
    R121919 (NBI30775) is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types[1].
  • HY-P0086
    Corticotropin-releasing factor (human)
    Corticotropin-releasing factor human (Human CRF) stimulates the synthesis and secretion of adrenocorticotropin in the anterior pituitary.
  • HY-14130
    CP 376395 Antagonist 99.71%
    CP 376395 is a potent and selective Corticotropin releasing factor 1 (CRF1) receptor antagonist.
  • HY-12127
    Pexacerfont Antagonist 99.79%
    Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1±0.6 nM for human CRF1 receptor.
  • HY-P0086A
    Corticotropin-releasing factor (human) (acetate) 98.51%
    Corticotropin-releasing factor human acetate (Human CRF acetate) stimulates the synthesis and secretion of adrenocorticotropin in the anterior pituitary.
  • HY-P1542B
    Urotensin I TFA Agonist 98.29%
    Urotensin I (Catostomus urotensin I) TFA, 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 CRF receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF and mCRF receptors, respectively[1][2].
  • HY-P1533A
    CRF, bovine TFA Agonist
    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-14875
    Verucerfont Antagonist 98.67%
    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-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 CRF receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF and mCRF receptors, respectively[1][2].
  • HY-P1295
    Urocortin, human Agonist
    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.
  • 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 CRF, CRF and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 can be used for hypotension study[1].
  • HY-P1294A
    α-Helical CRF(9-41) TFA Modulator
    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-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-P1297
    CRF(6-33)(human) Inhibitor
    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-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 CRF and rat CRF1 receptors, respectively[1].
  • 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[1][2].
  • HY-P2287
    Cortagine Agonist
    Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model[1].
  • 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[1]. 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[2].
  • HY-P1294
    α-Helical CRF(9-41) Modulator
    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[1][2].