crf2

α-helical CRF 9-41 acetate 是 CRF2 的竞争性拮抗剂 (KB = 100 nM) 和 CRF1 的部分激动剂 (EC50 = 140 nM)。

Urocortin, human (Human urocortin I) 是由 40 个氨基酸组成的神经多肽，是选择性 CRF2受体激动剂，作用于 hCRF1(Ki:0.4 nM)、rCRF2α(Ki:0.3 nM)、 mCRF2β(Ki:0.5 nM)。

K41498 acetate 是 antisauvagine-30 的类似物，可抑制 suvagine 刺激的 cAMP 在表达 hCRF2α 和 hCRF2β 的细胞中的积累。 K41498 acetate 是一种有效且高度选择性的 CRF2 受体拮抗剂，对人 CRF2α、CRF2β 和 CRF1 受体的 Ki 值分别为 0.66 nM、0.62 nM 和 425 nM。

R121919 (NBI30775) 是一种高效的促肾上腺皮质激素释放因子受体 1 （CRF1）小分子受体拮抗剂，具有抗抑郁和抗焦虑活性，抑制 CRF1 受体、 CRF2 受体和 CRF 结合蛋白。

Urotensin I acetate 是一种 CRF 样神经肽，可作为 CRF 受体激动剂，对 CHO 细胞中的人 CRF1、人 CRF2 和大鼠 CRF2α 受体的 pEC50 分别为 11.46、9.36 和 9.85，对 CHO 细胞的 Kis 分别为 0.4、1.8 和 5.7 nM hCRF1、rCRF2α 和 mCRF2β 受体。

Urocortin (rat) acetate 是一种内源性 CRFR 激动剂，对人 CRF1、大鼠 CRF2α 和小鼠 CRF2β 的 Ki 分别为 13 nM、1.5 nM 和 0.97 nM。 Urocortin (rat) acetate 是一种神经肽。

Antisauvagine-30 TFA (aSvg-30 TFA) is a highly selective and competitive antagonist of CRF2 receptor peptidic. It shows a Kd of 1.4 nM and 150 nM for mCRFR2β and CRFR1, respectively.

Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011). Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively). It stimulates cAMP production in CHO cells expressing rat CRF2α and mouse CRF2β (EC50s = 0.16 and 0.12 nM, respectively) as well as cultured anterior pituitary cells expressing endogenous CRF2β. Urocortin III is co-released with insulin to potentiate glucose-stimulated somatostatin release in vitro in human pancreatic β-cells.2 In vivo, urocortin III reduces food intake in a dose- and time-dependent manner in mice with a minimum effective dose (MED) of 0.3 nmol/animal.3 It increases swimming time in a forced swim test in mice, indicating antidepressant-like activity.4 References1. Lewis, K., Li, C., Perrin, M.H., et al. Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. U.S.A. 98(13), 7570-7575 (2001).2. van der Meulen, T., Donaldson, C.J., Cáceres, E., et al. Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion. Nat. Med. 21(7), 769-776 (2015).3. Pelleymounter, M.A., Joppa, M., Ling, N., et al. Behavioral and neuroendocrine effects of the selective CRF2 receptor agonists urocortin II and urocortin III. Peptides 25(4), 659-666 (2004).4. Tanaka, M., Kádár, K., Tóth, G., et al. Antidepressant-like effects of urocortin 3 fragments. Brain Res. Bull. 84(6), 414-418 (2011).

Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004). Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2 References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004).

Verucerfont (NBI77860) 是促肾上腺皮质激素释放因子受体 1 (CRF1) 拮抗剂，作用于 CRF1(IC50:6.1 nM)，CRF2 (IC50>1000 nM)和 CRF-BP (IC50>1000 nM)。

K41498 TFA 是一种强选择性的CRF2 receptor 拮抗剂，其对人 CRF2α、CRF2β和 CRF1受体的Ki 值分别为 0.66 nM、0.62 nM 和425 nM。K41498 TFA 是 antisauvagine-30 (aSvg-30) 的类似物，可抑制 sauvagine 刺激的 cAMP 在 hCRF2α hCRF2β表达细胞中的积累。K41498 可用于低血压研究。

Antisauvagine-30 TFA (aSvg-30 TFA) 是有效的、高度选择性的、竞争性的CRF2受体的多肽拮抗剂。Antisauvagine-30 TFA 对 mCRFR2β 和CRFR1的Kd 值分别为1.4 nM 和150 nM。

α-Helical CRF(9-41) TFA 是一种竞争性 CRF2受体拮抗剂，KB 约为 100 nM。α-Helical CRF(9-41) TFA 也是一种 CRF1受体的部分激动剂，EC50为 140 nM。

Urotensin I (Catostomus urotensin I) TFA 是一种类 CRF 样肽，可作为 CRF 受体激动剂，在细胞实验中，对人 CRF1，CRF2和大鼠 CRF2α受体的 pEC50值分别为 11.46，9.36 和 9.85，对 hCRF1，rCRF2α和 mCRF2β受体的 Ki 值分别为 0.4，1.8 和 5.7 nM。

Urocortin II, mouse 是一种选择性的 2 型促肾上腺皮质激素释放因子 (CRF2) 受体内源性多肽激动剂，对CRFR2和CRFR1的Ki 值分别为 0.66 nM 和 ﹥100 nM。Urocortin II, mouse 通过以 cAMP PKA 和 Ca2+ CaMKII 依赖性方式激活 CRF2 受体。Urocortin II, mouse 在中枢神经系统的离散区域表达，并激活参与内脏感觉信息处理和调节自主神经外流的中枢神经元。

Urocortin III (mouse) (free acid) 是一种选择性的 CRF2受体激动剂 (对 CRF2受体具有高亲和力)。Urocortin III (mouse) (free acid) 可显著抑制胃排空而不改变结肠运输。

Urocortin II, a neuropeptide hormone within the corticotropin-releasing factor (CRF) family—which comprises mammalian CRF, urocortin I, urocortin III, frog sauvagine, and piscine urotensin I—displays 34, 43, and 37-40% sequence homology with rat and human CRF, human urocortin I, and human urocortin III, respectively. This compound enhances rabbit ventricular myocyte shortening and relaxation in both a time- and concentration-dependent manner. In vivo studies reveal that urocortin II lowers arterial blood pressure in both normotensive and spontaneously hypertensive rats through peripheral CRF2 receptor agonism, inducing dose-dependent tachycardia and hypotension at doses of 3 and 30 pmol/kg. Additionally, it mitigates the visceral pain response to colorectal distension at 10 and 20 μg/kg in conscious rats and delays gastric emptying in mice.

NBI 35965 hydrochloride 是一种选择性、口服活性、能穿过血脑屏障的促肾上腺皮质激素释放因子受体 1 (CRF1) 拮抗剂，Ki 值为 4 nM，pKi 值为 8.5，并且不抑制 CRF2。NBI 35965 hydrochloride 可减少体内 CRF 或应激诱导的促肾上腺皮质激素 (ACTH) 生成，pIC50 值分别为 7.1 和 6.9，具有抗焦虑作用。

CRF, bovine (TFA) is a potent agonist of CRF receptor, and displaces [125I-Tyr]ovine CRF with a Ki of 3.52 nM.CRF, bovine is a potent agonist of CRF receptor, and displaces [125I-Tyr]ovine CRF with a Ki of 3.52 nM[1]. CRF shows pEC50s of 11.16, 8.53 and 8

Urotensin I is, 41-aa neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectivel

Human urocortin (hUcn) II is a new member of the corticotropin-releasing-factor (CRF) family. It selectively binds to the CRF2 receptor. Human urocortin II exhibits mild motor-suppressive effects and delayed anxiolytic-like effects,suggesting a time-depen

Human urocortin (hUcn) II is a new member of the corticotropin-releasing-factor (CRF) family. It selectively binds to the CRF2 receptor.

Potent and highly selective CRF2 receptor antagonist (Ki values are 0.66, 0.62 and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. In rats in vivo, blo

Potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist (Kd values are 1.4 and 153.6 nM for binding to mouse CRF2β and rat CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in HEK-mCRF2β cells