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WS 12 (Synonyms: WS-12; AR-15512; AVX-012)
目录号: PC12315 纯度: ≥98%
CAS No. :68489-09-8
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中文名称
WS 12
中文别名
凉味剂WS-12
英文名称
WS 12
英文别名
Cyclohexanecarboxamide,N-(4-methoxyphenyl)-5-methyl-2-(1-methylethyl)-, (1R,2S,5R)-;(1R*,2S*)-N-(4-METHOXYPHENYL)-5-METHYL-2-(1-METHYLETHYL)CYCLOHEXANECARBOXAMIDE;(1R,2S,5R)-N-(4-methoxyphenyl)-5-methyl-2-propan-2-ylcyclohexane-1-carboxamide;WS 12;7-Hydroxy-DPAT hydrobromide;cooling agent;WS-12
Cas No.
68489-09-8
分子式
C18H27NO2
分子量
289.41
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

WS-12 (AR-15512) is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. WS-12 shows analgesic effect, and can be used in chronic neuropathic pain research.

性状

Solid

IC50 & Target[1][2]

EC50: 39 nM (TRPM8)

体外研究(In Vitro)

WS-12 (10 μM) shows TRPM8 agonism in tests on heterologously expressed TRP ion channels.
WS-12 (1 or 10 μM; 0-250 s) shows highly potent and specific TRPM8 channel agonist in DRG neurons.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: HEK293T cells
Concentration: 10 μM
Incubation Time:
Result: Activated mouse TRPM8 (mTRPM8), but neither activated nor inhibited mTRPA1.

Cell Viability Assay

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Trpm8 mice and mice injected with Capsaicin
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.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 20 mg/mL (69.11 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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°C, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: 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。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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