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

CRFR

Corticotropin-releasing Factor Receptor; CRHR

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    CRF, bovine
  • HY-103379
    CP 376395 hydrochloride
    Antagonist
    CP 376395 hydrochloride is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist.
    CP 376395 hydrochloride
  • 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).
    BMS-665053
  • HY-100150
    Mepixanox
    Activator
    Mepixanox (Pimexone) is an analeptic agent used in respiratory and cardiorespiratory insufficiency.
    Mepixanox
  • HY-120564
    BMS-763534
    Antagonist
    BMS-763534 is a CRF1 antagonist that inhibits neurological disorders such as depression and anxiety..
    BMS-763534
  • HY-14225
    BMS-764459
    Antagonist
    BMS-764459 is a CRF1 antagonist. BMS-764459 can be used for the research of neurological disorders such as depression and anxiety. BMS-764459 is also an atypical CYP1A1 inducer.
    BMS-764459
  • HY-P3683
    a-Helical Corticotropin Releasing Factor (12-41)
    Inhibitor
    a-Helical Corticotropin Releasing Factor (12-41) is a 30 amino acids long, α-helical analogue of corticotropin releasing factor/hormone. Corticotropin releasing factor (CRF) is a hypothalamic hormone, which stimulates the secretion of adrenocorticotrophic hormone (ACTH). a-Helical Corticotropin Releasing Factor (12-41) would suppress the stimulatory effect.
    a-Helical Corticotropin Releasing Factor (12-41)
  • 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-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-P3687
    [Tyr0] Corticotropin Releasing Factor, ovine
    Agonist
    [Tyr0] Corticotropin Releasing Factor, ovine is a corticotropin releasing factor/hormone isolated from ovine. Corticotropin releasing factor (CRF) is a hypothalamic hormone, stimulates the release of adrenocorticotropic hormone (ACTH) and of β-endorphin.
    [Tyr0] Corticotropin Releasing Factor, ovine
  • HY-P4542
    (D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat)
    Antagonist
    (D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) is a CRF antagonist. (D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) prevents the IL-1a induced Luteinizing hormone (LH) inhibition.
    (D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat)
  • HY-P3684
    [DPro5] Corticotropin Releasing Factor, human, rat
    Agonist
    [DPro5] Corticotropin Releasing Factor, human, rat is a selective R2 agonist of corticotropin releasing factor/hormone. Corticotropin releasing factor (CRF) is a hypothalamic hormone, stimulates the release of adrenocorticotropic hormone (ACTH) and of β-endorphin. [DPro5] Corticotropin Releasing Factor, human, rat fails to cause the typical anxiogenic effect, but modulates learning and memory processes in rat.
    [DPro5] Corticotropin Releasing Factor, human, rat
  • HY-P3169
    a-Helical Corticotropin Releasing Factor (9-41)
    Antagonist
    α-Helical Corticotropin Releasing Factor (9-41) is a corticotropin releasing factor (CRF) antagonist. α-Helical Corticotropin Releasing Factor (9-41) decreases plasma growth hormone (GH) values in vivo.
    a-Helical Corticotropin Releasing Factor (9-41)
  • HY-P1752A
    Urocortin II, human TFA
    Agonist
    Urocortin II, human (TFA) 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 TFA
  • HY-P1296A
    Urocortin, rat TFA
    Agonist
    Urocortin, rat TFA (Urocortin (Rattus norvegicus) TFA) 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.
    Urocortin, rat TFA
  • HY-123677
    E2508
    Antagonist
    E2508 is an orally active corticotropin-releasing factor 1 (CRF1) receptor antagonist with a Ki value of 11 nM for hCRF1.
    E2508
  • HY-P3959
    (Tyr0)-Urocortin, rat
    Agonist
    (Tyr0)-Urocortin, rat is a high-affinity agonist of corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2). (Tyr0)-Urocortin, rat shows inhibitory binding constants (Ki) of 1-2 nM.
    (Tyr0)-Urocortin, rat
  • HY-14129
    CP 316311
    Antagonist
    CP 316311 is a potent and selective CRF1 receptor antagonist with an IC50 value of 6.8 nM.
    CP 316311
  • HY-P3685
    [Met(O)21] Corticotropin Releasing Factor, ovine
    Modulator
    [Met(O)21] Corticotropin Releasing Factor, ovine is a corticotropin releasing factor isolated from ovine hypothalamic extracts. Corticotropin releasing factor (CRF) is a hypothalamic hormone, which stimulates the secretion of adrenocorticotrophic hormone (ACTH).
    [Met(O)21] Corticotropin Releasing Factor, ovine
  • 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.
    NBI 35965 methanesulfonate

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