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UFP101是一种合成肽类物质,作为nociceptin受体的拮抗剂(Ki为0.06 nM,测试于表达人类受体的CHO细胞中)。它对nociceptin受体的选择性高于κ-opioid受体(Ki为204 nM,测试于表达大鼠受体的CHO细胞中)。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS(EC50为1.86 nM)。通过脑室内给药,UFP101(10 nmol/每只动物)能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中,UFP101(0.003、0.03及0.3 mg/kg)能提高生存率。
UFP101是一种合成肽类物质,作为nociceptin受体的拮抗剂(Ki为0.06 nM,测试于表达人类受体的CHO细胞中)。它对nociceptin受体的选择性高于κ-opioid受体(Ki为204 nM,测试于表达大鼠受体的CHO细胞中)。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS(EC50为1.86 nM)。通过脑室内给药,UFP101(10 nmol/每只动物)能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中,UFP101(0.003、0.03及0.3 mg/kg)能提高生存率。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 μg | ¥ 2,380 | 期货 | |
1 mg | ¥ 4,510 | 期货 | |
5 mg | ¥ 11,800 | 期货 |
产品描述 | UFP101 is a synthetic peptide that functions as an antagonist of the nociceptin receptor, demonstrating high affinity with a Ki of 0.06 nM in CHO cells expressing the human receptor. It exhibits selectivity for the nociceptin receptor over the κ-opioid receptor, with a Ki of 204 nM in CHO cells expressing the rat receptor. The compound effectively inhibits GTPγS release from the nociceptin receptor in CHO cell membranes, with an EC50 of 1.86 nM. When administered intracerebroventricularly at a dose of 10 nmol/animal, UFP101 prolongs the latency to tail withdrawal in the tail-flick test in mice, indicating its potential as an analgesic. Additionally, at doses of 0.003, 0.03, and 0.3 mg/kg, UFP101 enhances survival in a sepsis mouse model induced by cecal ligation and puncture, suggesting potential therapeutic applications in sepsis management. |
分子量 | 1908.18 |
分子式 | C82H138N32O21.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 | PBS pH 7.2: 10 mg/ml DMF: 5 mg/ml DMSO: 10 mg/ml |
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