urocortin, human

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)。

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。

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.

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.

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。

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。

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

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).