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]. |
| IC50& Target | |
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. |
|
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. |
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 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 |
|
| 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2 mg/mL (6.91 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (6.91 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
m.cnreagent.com