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-P1368
    Stressin I
    		Agonist 98.20%
    Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) is a potent CRF1 receptor-selective agonist with a Ki of 1.7 nM. Stressin I induces increases in adrenocorticotropic hormone (ACTH) levels in rats.
    Stressin I
  • 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-P2847
    Urocortin II, mouse
    		Agonist 98.63%
    Urocortin II, mouse is a potent and selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor with Ki values of 0.66 nM and ﹥100 nM for CRFR2 and CRFR1, respectively. Urocortin II, mouse activates CRF2 receptors in a cAMP/PKA- and Ca2+/CaMKII-dependent manner.Urocortin II, mouse is expressed in discrete areas of the central nervous system, and activates central neurons involved in the processing of visceral sensory information, and in modulating autonomic outflow.
    Urocortin II, mouse
  • 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-P1294
    α-Helical CRF(9-41)
    		Modulator 99.44%
    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-P1752
    Urocortin II, human
    		Agonist 99.61%
    Urocortin II (human) is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. For investigating the role of the CRF (2) receptor in ingestive behavior.
    Urocortin II, human
  • HY-P1542B
    Urotensin I TFA
    		Agonist
    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 CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively.
    Urotensin I TFA
  • HY-14367
    Emicerfont
    		Antagonist 98.03%
    Emicerfont is a corticotropin-releasing factor type 1 (CRF1) receptor antagonist with an IC50 of 66 nM.
    Emicerfont
  • 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
  • HY-P1294A
    α-Helical CRF(9-41) TFA
    		Modulator 99.90%
    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.
    α-Helical CRF(9-41) TFA
  • 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.
    CRF(6-33)(human)
  • HY-P0060A
    Tetracosactide acetate
    		99.53%
    Tetracosactide acetate (Tetracosactrin acetate ) is the acetate salt form of Tetracosactide (HY-P0060). Tetracosactide acetate is an analogue of adrenocorticotrophic hormone (ACTH). Tetracosactide acetate is the agonist for melanocortin-4 receptor (MC4R) that activates human MC4R with an EC50 of 0.65 nM. Tetracosactide acetate can stimulate the release of corticosteroids such as cortisol from the adrenal gland. Tetracosactide acetate is currently used for the research of ulcerative colitis and Crohn's disease, juvenile/adult rheumatoid arthritis and osteoarthrosis.
    Tetracosactide acetate
  • 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.
    Urotensin I
  • HY-P1107
    Antisauvagine-30
    		Antagonist 99.74%
    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.
    Antisauvagine-30
  • HY-103376
    NBI-27914 hydrochloride
    		Antagonist
    NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with a Ki value of 1.7 nM.
    NBI-27914 hydrochloride
  • HY-P1245
    Neuropeptide SF (human)
    		Activator 99.53%
    Neuropeptide SF human augments paraventricular corticotrophin-releasing hormone (CRH) release and increases adrenocorticotropic hormone (ACTH) and corticosterone levels in the plasma. Neuropeptide SF human 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)
  • HY-12339
    NVS-CRF38
    		Antagonist
    NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
    NVS-CRF38
  • 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-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.
    K41498
  • HY-12130
    CP 154526
    		Antagonist
    CP 154526 is a potent, brain-penetrant and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki of 2.7 nM. CP 154526 shows selective for CRF1 over CRF2 (Ki = >10 μM). CP 154526 has anxiolytic activities.
    CP 154526
CRFR Isoform Comparison

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