WS-12 (AR-15512) 是一种强效和选择性的TRPM8激动剂,是薄荷醇的衍生物,作为一种冷却剂。WS-12 显示出镇痛作用,可用于慢性神经性疼痛的研究。
生物活性 | WS-12 (AR-15512) is a potent and selectiveTRPM8agonist, the menthol derivative, as a cooling agent. WS-12 shows analgesic effect, and can be used in chronic neuropathic pain research[1][2]. |
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体外研究 (In Vitro) | WS-12 (10 μM) shows TRPM8 agonism in tests on heterologously expressed TRP ion channels[1]. WS-12 (1 or 10 μM; 0-250 s) shows highly potent and specific TRPM8 channel agonist in DRG neurons[1].
Cell Viability Assay[1] Cell Line: | HEK293T cells | Concentration: | 10 μM | Incubation Time: | | Result: | Activated mouse TRPM8 (mTRPM8), but neither activated nor inhibited mTRPA1. |
Cell Viability Assay[1] Cell Line: | Cultured mouse DRG neurons | Concentration: | 1 or 10 μM | Incubation Time: | 0-250 s | Result: | Showed approximately 10% to 14% of cultured wild-type neurons responsive to WS-12. |
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体内研究 (In Vivo) | WS-12 (intraperitoneal injection; 10 mg/kg; once) shows analgesic effect by selective TRPM8 activation in mice[1].
Animal Model: | Trpm8–/–mice and mice injected with Capsaicin[1] | Dosage: | 10 mg/kg | Administration: | Intraperitoneal injection; 10 mg/kg; once | Result: | Produced an obvious analgesic effect, and this effect abolished in Trpm8–/–mice. Showed no change falling latencies in mice in the rotarod test. Reduced Capsaicin-induced nocifensive behavior. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 20 mg/mL(69.11 mM;Need ultrasonic) 配制储备液 1 mM | 3.4553 mL | 17.2765 mL | 34.5531 mL | 5 mM | 0.6911 mL | 3.4553 mL | 6.9106 mL | 10 mM | 0.3455 mL | 1.7277 mL | 3.4553 mL |
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