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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 μg | ¥ 2,280 | 期货 | |
1 mg | ¥ 4,330 | 期货 | |
5 mg | ¥ 19,800 | 期货 |
产品描述 | K 41498 is a selective peptide antagonist targeting both corticotropin-releasing factor receptor 2α (CRF2α) and CRF2β, demonstrating high affinity with Kis of 0.66 and 0.62 nM, respectively, in HEK293 cells expressing these human receptors. Its selectivity is evident as it exhibits a significantly reduced affinity for CRF1 receptor (Ki = 425 nM in HEK293 cells expressing the human CRF1 receptor). Additionally, K 41498, when administered intravenously at 1.84 µg/animal, effectively mitigates urocortin-induced hypotension in rats. Furthermore, its intrathecal delivery ranging from 0.075 to 0.5 µmol/animal significantly lowers the mechanical paw withdrawal threshold in a rat model, indicating its potential utility in managing nociception triggered by complete Freund's adjuvant. |
分子量 | 3632.22 |
分子式 | C162H276N48O46.XCF3COOH |
存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | H2O: Soluble |
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