crf2β

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。

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)。

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)。

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。

K 41498 是一种针对皮质酮释放因子受体2α（CRF2α）和CRF2β的肽拮抗剂，其在表达人类受体的HEK293细胞中的Ki值分别为0.66和0.62 nM。它对CRF2α和CRF2β具有选择性，与CRF1相比（在表达人类受体的HEK293细胞中Ki值为425 nM）。K 41498 (1.84 µg/动物, 静脉注射) 能够阻止大鼠由于尿催肾上腺皮质激素引发的低血压。通过脊髓内给药，K 41498 (0.075-0.5 µmol/动物) 能降低完全弗氏佐剂引起的大鼠模型中机械性爪撤回阈值。

Corticotropin-releasing factor receptor antagonist (Ki values are 17, 5 and 0.97 at human CRF1, rat CRF2α and mouse CRF2β receptors 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 III (human) 是一种促肾上腺皮质激素释放因子 (CRF) 相关肽。Urocortin III (human) 优先结合并激活CRF-R2，并且具有离散的中枢神经系统和外周分布。Urocortin III (human) 选择性结合 2 型 CRF 受体，mCRF2β、rCRF2α 和 hCRF1 的Ki 值分别为 13.5、21.7 和 >100 nM。Urocortin III (human) 介导Insulin(human) 分泌的生长抑素依赖性负反馈控制。

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

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

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。

Urocortin, rat TFA is a neuropeptide and a potent endogenous CRFR agonist (Kis: 0.97 nM, 1.5 nM, and 13 nM for mouse CRF2β, rat CRF2α, and human CRF1).