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.
CRFR Isoform Specific Products
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CRFR Related Products (90)
Related Products (90)
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CRFR Isoform Comparison
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NBI 35965 methanesulfonate
0 ImagesCat. No.: HY-103378CAS No.: 603151-83-3NBI 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.
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Emicerfont
0 ImagesSynonyms: GW876008Emicerfont is a corticotropin-releasing factor type 1 (CRF1) receptor antagonist with an IC50 of 66 nM.
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Urocortin III (human)
0 ImagesUrocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) potently binds to type 2 CRF receptors, specifically mCRF2β (Ki = 13.5 nM) and rCRF2α (Ki = 21.7 nM), while demonstrating negligible affinity for hCRF1 (Ki >100 nM). Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion[1][2].
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NVS-CRF38
0 ImagesCat. No.: HY-12339CAS No.: 1207258-55-6NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
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1,1′-Ethylidenebis[L-tryptophan]
![1,1′-Ethylidenebis[L-tryptophan]](https://file.medchemexpress.com/product_pic/hy-w585843.gif "Click to View 1,1′-Ethylidenebis[L-tryptophan] Product Detail")
0 ImagesCat. No.: HY-W585843CAS No.: 132685-02-01,1′-Ethylidenebis[L-tryptophan] is an orally active amino acid analog. 1,1′-Ethylidenebis[L-tryptophan] promotes the release of adrenocorticotropic hormone and corticosterone in rat plasma, and transiently inhibits CRH mRNA in the paraventricular nucleus of the hypothalamus via glucocorticoid negative feedback. 1,1′-Ethylidenebis[L-tryptophan] induces multi-tissue inflammation and fibrosis in rodents and human cells, increases the number of degranulated mast cells, and activates the IL-5 pathway in lymphocytes. 1,1′-Ethylidenebis[L-tryptophan] is activated by tryptophanyl-tRNA synthetase and replaces L-tryptophan during translation; it also interferes with tryptophan metabolism in mice via the kynurenine pathway and dynamically alters their plasma quinolinic acid levels. 1,1′-Ethylidenebis[L-tryptophan] can be used for studies on metabolism-related mechanisms.
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R121919 hydrochloride
0 ImagesCat. No.: HY-115645CAS No.: 195055-66-4Synonyms: NBI30775 hydrochlorideR121919 (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.
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CP 154526
0 ImagesCat. No.: HY-12130CAS No.: 157286-86-7CP 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.
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DMP 904
0 ImagesCat. No.: HY-12132CAS No.: 202579-74-6DMP 904 is a noncompetitive full corticotropin-releasing factor receptor (CRFR) antagonist. DMP 904 can inhibit CRF-stimulated adenylate cyclase activity and ACTH release. DMP 904 exhibits anti-depressant and anti-anxiety activity.
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CRF, bovine
0 ImagesCat. No.: HY-P1533CAS No.: 92307-52-3Synonyms: Corticotropin Releasing Factor bovineCRF, bovine is a potent agonist of CRF receptor, and displaces [125I-Tyr]ovine CRF with a Ki of 3.52 nM.
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CP 376395 hydrochloride
0 ImagesCat. No.: HY-103379CAS No.: 1013933-37-3CP 376395 hydrochloride is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist.
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BMS-665053
0 ImagesCat. No.: HY-14132CAS No.: 1173435-64-7BMS-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).
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NBI 30545
0 ImagesCat. No.: HY-119247CAS No.: 195054-99-0NBI 30545 is a blood-brain barrier permeable CRF1R antagonist with a Ki value of 3.4 nM for the human receptor. NBI 30545 inhibits CRF-stimulated intracellular cAMP accumulation and ACTH release. NBI 30545 can be used in the research of depression, anxiety disorders and stress-related diseases.
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NGD 98-2 hydrochloride
0 ImagesCat. No.: HY-110310CAS No.: 1780390-58-0NGD 98-2 hydrochloride is an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist
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Mepixanox
0 ImagesCat. No.: HY-100150CAS No.: 17854-59-0Synonyms: PimexoneMepixanox (Pimexone) is an analeptic agent used in respiratory and cardiorespiratory insufficiency.
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E-2508 free base
0 ImagesCat. No.: HY-119114CAS No.: 685885-75-0E-2508 free base is an orally active and highly selective corticotropin-releasing factor type 1 receptor (CRF1) antagonist with anxiolytic effects (Ki=11 nM). E-2508 free base blocks CRF-induced cAMP accumulation via CRF1 receptor inhibition. E-2508 free base is promising for research of stress-related psychiatric disorders, such as anxiety and depression.
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BMS-763534
0 ImagesCat. No.: HY-120564CAS No.: 1188407-40-0BMS-763534 is a CRF1 antagonist that inhibits neurological disorders such as depression and anxiety..
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BMS-764459
0 ImagesCat. No.: HY-14225CAS No.: 1188407-45-5BMS-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.
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a-Helical Corticotropin Releasing Factor (12-41)
0 ImagesCat. No.: HY-P3683CAS No.: 158535-55-8a-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.
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Neuropeptide SF (human) acetate
0 ImagesCat. No.: HY-P1245ACAS No.: 2924824-03-1Synonyms: Neuropeptide NPFF (human) acetateNeuropeptide 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.
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NBI 35965 hydrochloride
0 ImagesCat. No.: HY-110056CAS No.: 1782228-59-4NBI 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.
