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 (88)
Related Products (88)
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CRFR Isoform Comparison
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Antalarmin hydrochloride
0 ImagesAntalarmin (hydrochloride) is an oral active 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.
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Corticotropin-releasing factor (human)
0 ImagesSynonyms: Human CRF; Human corticotropin-releasing factorCorticotropin-releasing factor human (Human CRF) stimulates the synthesis and secretion of adrenocorticotropin in the anterior pituitary.
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Urocortin, human
0 ImagesSynonyms: Urocortin (human); Human urocortin; Human urocortin 1; Human urocortin IUrocortin, human, a 40-aa neuropeptide, acts as an agonist of endogenous CRF receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively.
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Urocortin II, human
0 ImagesUrocortin II, human is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. Urocortin II, human has an effect of promoting satiet and neuroprotective effect. Urocortin II, human also has bactericidal, antiparasitic and pro-inflammation activity. Urocortin II, human can activate NF-κB pathway and ERK1/2 MAP kinase. Urocortin II, human can reduce pulmonary arterial hypertension and shows cardiac protection effect. Urocortin II, human can be used for the researches of infection, inflammation, metabolic, neurological and cardiovascular disease.
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R121919
0 ImagesSynonyms: NBI30775R121919 (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.
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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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CRF1 receptor antagonist-2
0 ImagesCat. No.: HY-182645CAS No.: 441060-02-2CRF1 receptor antagonist-2 is an orally active, blood-brain barrier permeable CRF1 receptor antagonist, with an IC50 of 4 nM in CHO-K1 cell membranes and an IC50 of 7 nM in rat brain cell membranes. CRF1 receptor antagonist-2 exerts anxiolytic effects in swim stress-loaded rats. CRF1 receptor antagonist-2 can be used in studies related to stress-induced anxiety.
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Urocortin II, mouse
0 ImagesUrocortin 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.
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Sauvagine TFA
0 ImagesCat. No.: HY-P1298APurity: 99.96%Sauvagine TFA is a corticotropin-releasing factor receptor (CRFR) agonist. Sauvagine TFA activates HM-CRF receptors to stimulate intracellular cAMP accumulation, activates PC-CRF receptors to trigger associated signaling pathways, and stimulates the hypothalamic-pituitary-adrenal axis. Sauvagine TFA can be used for research on central nervous system and blood diseases.
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Antalarmin
0 ImagesAntalarmin 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.
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Astressin 2B TFA
0 ImagesCat. No.: HY-P1108APurity: 99.75%Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2.
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Tetracosactide
0 ImagesSynonyms: Tetracosactrin; ACTH(1–24)Tetracosactide (Tetracosactrin) is an analogue of adrenocorticotrophic hormone (ACTH). Tetracosactide is the agonist for melanocortin-4 receptor (MC4R) that activates human MC4R with an EC50 of 0.65 nM. Tetracosactide can stimulate the release of corticosteroids such as cortisol from the adrenal gland. Tetracosactide is currently used for the research of ulcerative colitis and Crohn's disease, juvenile/adult rheumatoid arthritis and osteoarthrosis.
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Urocortin III, mouse TFA
0 ImagesCat. No.: HY-P1858APurity: 98.06%Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2. 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.
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Stressin I
0 ImagesCat. No.: HY-P1368Purity: 98.85%Synonyms: Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)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.
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Astressin 2B
0 ImagesCat. No.: HY-P1108CAS No.: 681260-70-8Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2.
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Pexacerfont
0 ImagesSynonyms: BMS-562086Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1±0.6 nM for human CRF1 receptor.
