2. Signaling Pathways
  3. GPCR/G Protein
  4. CRFR
  5. CRFR Antagonist

CRFR Antagonist

CRFR Isoform Comparison

CRFR Antagonists (48):

Cat. No. Product Name Effect Purity
  • HY-103377
    Antalarmin hydrochloride
    		Antagonist 99.87%
    Antalarmin (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.
  • HY-14127
    R121919
    		Antagonist 99.66%
    R121919 (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.
  • HY-119247
    NBI 30545
    		Antagonist
    NBI 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.
  • HY-182645
    CRF1 receptor antagonist-2
    		Antagonist
    CRF1 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.
  • HY-P1108A
    Astressin 2B TFA
    		Antagonist 99.54%
    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.
  • HY-135542
    NBI-27914
    		Antagonist 99.94%
    NBI-27914 is a highly selective, high-affinity non-peptide competitive antagonist of human corticotropin-releasing factor receptor 1 (CRFR1). NBI-27914 primarily binds to the His199 and Met276 sites in the transmembrane domain of the receptor.
  • HY-P0257
    Astressin
    		Antagonist 98.93%
    Astressin is a potent corticotropin releasing factor (CRF) antagonist.
  • HY-124475
    Antalarmin
    		Antagonist 99.95%
    Antalarmin 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.
  • HY-12127
    Pexacerfont
    		Antagonist 99.87%
    Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1±0.6 nM for human CRF1 receptor.
  • HY-P1108
    Astressin 2B
    		Antagonist
    Astressin 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.
  • HY-14875
    Verucerfont
    		Antagonist 99.93%
    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-14130
    CP 376395
    		Antagonist 99.59%
    CP 376395 is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist.
  • 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.
  • HY-P1107A
    Antisauvagine-30 TFA
    		Antagonist 98.10%
    Antisauvagine-30 TFA (aSvg-30 TFA) is a potent, highly selective and competitive CRF2 receptor peptidic antagonist. Antisauvagine-30 TFA exhibits a Kd of 1.4 nM and 150 nM for mCRFR2β and CRFR1, respectively.
  • HY-P1106
    K41498
    		Antagonist 99.66%
    K41498 is a highly selective CRF 2 receptor antagonist, with a Ki of 0.66 nM for human CRF2α receptor and a Ki of 0.62 nM for human CRF2β receptor. K41498 inhibits cAMP accumulation in cells expressing CRF2. K41498 antagonizes the hypotensive response induced by systemic administration of urocortin in conscious rats. K41498 undergoes radioiodination without loss of activity and serves for autoradiographic studies of native CRF2 receptors in rat brain and peripheral tissues.
  • 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.
  • 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.
  • 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.
  • HY-14367
    Emicerfont
    		Antagonist 98.03%
    Emicerfont is a corticotropin-releasing factor type 1 (CRF1) receptor antagonist with an IC50 of 66 nM.
  • HY-12339
    NVS-CRF38
    		Antagonist
    NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.