CRFR2

CRFR2 (corticotropin-releasing factor receptor 2, CRHR2) is a class B G protein-coupled receptor that mediates adaptive responses to physiological and psychological stress through selective interactions with the urocortin peptide family^[1]^[2]. Mechanistically, CRFR2 regulates stress-recovery signaling, autonomic function, emotional processing, and neuroendocrine homeostasis through downstream G protein-dependent pathways that influence CREB phosphorylation and cellular stress responses^[3]^[4]. In experimental models, genetic deletion of Crhr2 produces enhanced anxiety-like behavior, stress hypersensitivity, and impaired adaptation to environmental challenges, establishing CRFR2 as a key regulator of stress resilience rather than stress initiation^[3]^[4]^[5]. Compared with the closely related isoform CRFR1, which predominantly promotes anxiogenic and hypothalamic-pituitary-adrenal axis activation, CRFR2 exerts counter-regulatory functions that facilitate recovery from stress exposure and restoration of homeostasis^[2]^[3]^[5]. The receptor also displays distinct isoform diversity, including CRFR2α, CRFR2β, and CRFR2γ, which differ in N-terminal structure, tissue distribution, and ligand responsiveness, providing additional regulatory specificity for experimental studies of receptor signaling^[6]^[7]. For research applications, the endogenous agonists urocortin II and urocortin III exhibit high selectivity for CRFR2 and are widely used to investigate receptor-dependent stress, cardiovascular, metabolic, and behavioral pathways in vivo and in vitro^[1]^[2].

References:

[1]. Vuppaladhadiam L, et al. Corticotropin-Releasing Factor Family: A Stress Hormone-Receptor System's Emerging Role in Mediating Sex-Specific Signaling. Cells. 2020 Mar 31;9(4):839. [Content Brief]

[2]. Database: Guide to pharmacology.

[3]. Kishimoto T, et al. Deletion of crhr2 reveals an anxiolytic role for corticotropin-releasing hormone receptor-2. Nat Genet. 2000 Apr;24(4):415-9. [Content Brief]

[4]. Bale TL, et al. Mice deficient for corticotropin-releasing hormone receptor-2 display anxiety-like behaviour and are hypersensitive to stress. Nat Genet. 2000 Apr;24(4):410-4. [Content Brief]

[5]. Bale TL, et al. Mice deficient for both corticotropin-releasing factor receptor 1 (CRFR1) and CRFR2 have an impaired stress response and display sexually dichotomous anxiety-like behavior. J Neurosci. 2002 Jan 1;22(1):193-9. [Content Brief]

[6]. Uniprotkb.

[7]. Sztainberg Y, et al. A novel corticotropin-releasing factor receptor splice variant exhibits dominant negative activity: a putative link to stress-induced heart disease. FASEB J. 2009 Jul;23(7):2186-96. [Content Brief]

CRFR2 Related Products (13):

By Type:	Pan (3) Selective (1)
By Effects:	Agonists (6) Antagonists (6) Modulator (1)

Cat. No.	Product Name	Effect	Purity

HY-P1752

Urocortin II, human	Agonist	99.95%
Urocortin 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.

HY-P2847

Urocortin II, mouse	Agonist	99.94%
Urocortin II, mouse is a potent and selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor with K_i 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.

HY-P1108A

Astressin 2B TFA	Antagonist	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.

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-14130

CP 376395	Antagonist	99.59%
CP 376395 is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist.

HY-P1296

Urocortin, rat	Agonist	99.23%
Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with K_is of 13 nM, 1.5 nM, and 0.97 nM for human CRF₁, rat CRF_2α and mouse CRF_2β, respectively.

HY-P1752B

Urocortin II, human acetate	Agonist	99.61%
Urocortin II, human acetate is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. Urocortin II, human acetate has an effect of promoting satiet and neuroprotective effect. Urocortin II, human acetate also has bactericidal, antiparasitic and pro-inflammation activity. Urocortin II, human acetate can activate NF-κB pathway and ERK1/2 MAP kinase. Urocortin II, human acetate can reduce pulmonary arterial hypertension and shows cardiac protection effect. Urocortin II, human acetate can be used for the researches of infection, inflammation, metabolic, neurological and cardiovascular disease.

HY-P1294A

α-Helical CRF(9-41) TFA	Modulator	99.91%
α-Helical CRF(9-41) TFA is a competitive CRF2 receptor antagonist with K_B of ~100 nM. α-Helical CRF(9-41) TFA is also a partial agonist of CRF1 receptor with an EC₅₀ of 140 nM.

HY-P1106

K41498	Antagonist	99.66%
K41498 is a highly selective CRF 2 receptor antagonist, with a K_i of 0.66 nM for human CRF2α receptor and a K_i 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-103379

CP 376395 hydrochloride	Antagonist
CP 376395 hydrochloride is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist.

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. Urocortin II, human TFA has an effect of promoting satiet and neuroprotective effect. Urocortin II, human TFA also has bactericidal, antiparasitic and pro-inflammation activity. Urocortin II, human TFA can activate NF-κB pathway and ERK1/2 MAP kinase. Urocortin II, human TFA can reduce pulmonary arterial hypertension and shows cardiac protection effect. Urocortin II, human TFA can be used for the researches of infection, inflammation, metabolic, neurological and cardiovascular disease.

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.

HY-14128

NBI-34041	Antagonist
NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC₅₀ of 58.9 nM and a K_i of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.

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