CRFR

R121919 is a potent small-molecule CRF1 receptor antagonist.

Emicerfont, also known as GW876008, is a CRF-1 antagonist. Emicerfont blocks the CRH-1 receptor, and so reduces ACTH release.

Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1??0.6 nM for human CRF1 receptor.

Corticotropin Releasing Factor, bovine, neurotransmitter and CRF receptor antagonist.

Verucerfont, also known as GSK561679 and NBI77860, is a CRF-1 antagonist. Verucerfont blocks the CRH-1 receptor, and so reduces ACTH release following chronic stress.

DMP 696 is a selective corticotropin-releasing hormone receptor 1 (CRHR1) antagonist, used for the treatment of anxiety and depression.

NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.

CP 376395 is a potent and selective Corticotropin releasing factor 1 (CRF1) receptor antagonist.

CP 316311 is a potent and selective CRF1 receptor antagonist with an IC50 value of 6.8 nM.

Urocortin, rat (Urocortin (Rattus norvegicus)) 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 CRF2α and mouse CRF2β, respectively.

CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) has anti-obesity effect.

Urocortin 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) selectively binds to type 2 CRF receptors with Ki values of 13.5, 21.7, and >100 nM for mCRF2β, rCRF2α, and hCRF1, respectively. Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) secretion.

Antalarmin hydrochloride is an orally active, non-peptide antagonist of corticotropin-releasing hormone receptor 1 (CRHR1) with a Ki of 1 nM. It effectively suppresses CRH-induced adrenocorticotropic hormone (ACTH) secretion and blocks both CRH- and novelty-induced anxiety-like behaviors in animal models. Antalarmin hydrochloride also exhibits anti-inflammatory activity in arthritis models and alleviates stress-induced gastric ulceration, supporting its potential in research related to irritable bowel syndrome and stress-related inflammatory conditions.

NBI-27914 is a potent and selective antagonist of corticotropin-releasing factor receptor 1 (CRFR1), a member of the G protein-coupled receptor (GPCR) superfamily. By selectively blocking CRFR1, NBI-27914 is useful for studying stress-related pathways and disorders mediated by CRF signaling, such as anxiety and depression.

Urocortin, human, is a 40-amino acid neuropeptide that functions as a selective agonist of the endogenous corticotropin-releasing factor receptor 2 (CRF₂). It exhibits high binding affinity with Kᵢ values of 0.4 nM for human CRF₁, 0.3 nM for rat CRF₂α, and 0.5 nM for mouse CRF₂β. Urocortin plays a role in modulating stress responses, cardiovascular function, and feeding behavior.

JNJ19567470 (R317573) is a selective, non-peptidergic corticotropin-releasing factor type 1 (CRF₁) receptor antagonist. It effectively blocks sodium lactate (NaLac)-induced panic-like behavior and associated cardiovascular responses. JNJ19567470 also reduces regional glucose utilization in the amygdala and attenuates anxiety-related responses

Antalarmin is a selective, nonpeptide antagonist of corticotropin-releasing factor receptor 1 (CRHR1), with a Ki of 2.7 nM. It is capable of crossing the blood–brain barrier, making it a valuable compound for investigating CRHR1-mediated central nervous system functions and stress-related disorders.

α-Helical CRF(9-41) is a competitive antagonist of the corticotropin-releasing factor receptor 2 (CRF₂) with a K\_B of approximately 100 nM. It also acts as a partial agonist at the CRF₁ receptor, with an EC₅₀ of 140 nM. This dual activity makes it a useful tool for studying CRF receptor signaling and stress-related physiological responses.

Tildacerfont is a potent and orally active corticotropin-releasing factor type 1 (CRF1) receptor antagonist. It effectively reduces levels of adrenocorticotropic hormone (ACTH) and adrenal androgens, demonstrating a favorable safety profile. Tildacerfont is being investigated for the treatment of congenital adrenal hyperplasia (CAH) and holds promise for research into disorders of the hypothalamic-pituitary-adrenal (HPA) axis.

Tetracosactide is a potent agonist of the melanocortin-4 receptor (MC4R), activating human MC4R with an EC50 of 0.65 nM. This synthetic analogue of adrenocorticotrophic hormone (ACTH) is known to stimulate the release of corticosteroids, including cortisol, from the adrenal gland. Tetracosactide is utilized in research investigating conditions such as ulcerative colitis, Crohn's disease, and various forms of arthritis, including juvenile and adult rheumatoid arthritis and osteoarthrosis.

Urocortin II, human is a selective agonist of the type-2 corticotropin-releasing factor (CRF2) receptor, exhibiting key biological activities that include promoting satiety and providing neuroprotective effects. This peptide also demonstrates bactericidal and antiparasitic properties, as well as pro-inflammatory activity. Additionally, Urocortin II, human can activate the NF-κB pathway and ERK1/2 MAP kinase, making it relevant for research in pulmonary arterial hypertension and cardiac protection. Its diverse applications extend to studies in infection, inflammation, metabolic disorders, neurological conditions, and cardiovascular diseases.

Corticotropin-releasing factor (human) acts as a modulator of corticotropin-releasing factor receptors (CRFR). It plays a crucial role in the hypothalamic-pituitary-adrenal (HPA) axis by stimulating the synthesis and secretion of adrenocorticotropin (ACTH) in the anterior pituitary. This reagent is essential for research in stress response, neuroendocrine regulation, and related pathophysiological conditions. Its applications extend to studies in anxiety, depression, and other mood disorders, providing insight into the molecular mechanisms of HPA axis regulation.

Urocortin II, mouse is a selective agonist of the type-2 corticotropin-releasing factor (CRF2) receptor, exhibiting a high affinity with a Ki value of 0.66 nM for CRFR2 and over 100 nM for CRFR1. It activates CRF2 receptors via cAMP/PKA and Ca2+/CaMKII signaling pathways. This peptide is predominantly expressed in specific regions of the central nervous system and plays a crucial role in processing visceral sensory information while modulating autonomic functions, making it valuable for research in neurobiology and stress response.

Astressin 2B is a selective antagonist of the corticotropin-releasing factor receptor 2 (CRFR2) with an IC50 of 0.57 nM. This compound disrupts the protective effects mediated by CRFR2, leading to increased intestinal damage in models of hemorrhagic injury and suggesting potential roles in studying inflammatory responses. Astressin 2B also reverses the protective effects of Urocortin 1 against intestinal complications and mitigates the anxiogenic effects of Urocortin 2, demonstrating its utility in research related to stress-induced anxiety and gastrointestinal pathology. This reagent is an effective tool for investigating CRFR2's role in intestinal protection and inflammatory processes.

Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide that primarily targets and activates CRF receptor type 2 (CRF-R2). It plays a significant role in the behavioral stress response system and is known to modulate social dynamics through its action in the medial amygdala. Urocortin III is valuable for research applications focused on stress responses and neurobehavioral studies.

BMS-665053 is a potent corticotropin-releasing factor-1 (CRF1) receptor antagonist, exhibiting an IC50 of 1.0 nM. This compound effectively inhibits CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells, with an IC50 of 4.9 nM. BMS-665053 is valuable for research in neuroendocrine regulation and stress response pathways.

[DPro5] Corticotropin Releasing Factor, human, rat is a selective agonist for the CRFR2 receptor, primarily involved in neuroendocrine response regulation. This molecule stimulates the release of adrenocorticotropic hormone (ACTH) and β-endorphin, contributing to various physiological responses. Notably, unlike traditional CRF peptides, [DPro5] does not induce anxiogenic effects, instead demonstrating potential to influence learning and memory processes in rat models. It serves as a valuable tool for investigating the role of CRFR2 in stress response and cognitive function.

BMS-561388 benzenesulfonate is a selective antagonist of the corticotropin-releasing factor receptor (CRFR). This compound exhibits significant potential in modulating stress-related responses, making it a valuable tool for research into neurological disorders such as anxiety and depression. Its ability to inhibit CRFR activity underscores its relevance in the study of stress-related pathologies and therapeutic interventions.

(Tyr0)-Urocortin, rat is a high-affinity agonist for both corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2). Exhibiting inhibitory binding constants (Ki) in the range of 1-2 nM, it is a key reagent for studying the role of CRF receptors in stress response and neuroendocrine signaling. This compound is particularly valuable for research into anxiety, depression, and related disorders, facilitating investigations into receptor-mediated pathways and therapeutic interventions.

Sauvagine, a 40-amino-acid neuropeptide and a potent corticotropin-releasing factor (CRF) agonist, is derived from the skin of the frog. It effectively stimulates the release of adrenocorticotropic hormone (ACTH) from rat pituitary cells. Additionally, sauvagine exhibits various pharmacological effects, influencing diuresis, cardiovascular function, and endocrine activity, making it a valuable tool for research in neurobiology and endocrinology.

NBI-35965 is a selective antagonist of corticotropin-releasing factor receptor 1 (CRF-R1). This compound is utilized in research applications focusing on the nervous system, particularly in studies exploring stress response, anxiety, and depression. By inhibiting CRF-R1 activity, NBI-35965 provides valuable insights into the mechanisms underlying these neuropsychiatric disorders.

SN003 is a reversible antagonist of corticotropin-releasing factor receptor 1 (CRFR 1), exhibiting an IC50 of 241 nM and over 1000-fold selectivity for CRFR 1 compared to CRFR 2. This compound effectively suppresses corticotropin-releasing factor-induced adrenocorticotropic hormone (ACTH) release in vitro. Additionally, SN003 demonstrates the potential to mitigate depressive-like behavior in rat models, making it a valuable tool for research in neuropsychiatric disorders.

DMP 904 is a noncompetitive antagonist of the corticotropin-releasing factor receptor (CRFR), effectively inhibiting CRF-stimulated adenylate cyclase activity and adrenocorticotropic hormone (ACTH) release. This compound demonstrates significant antidepressant and anxiolytic properties, making it a valuable tool for research in stress-related disorders and neuropsychiatric conditions. Its mechanism of action can provide insights into the therapeutic potential for anxiety and depression treatments.