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ARN19702 是一种选择性,具有口服活性的,可逆的,可透过血脑屏障的 N-乙酰乙醇胺酸酰胺酶 (NAAA) 抑制剂,对人 NAAA 的 IC50为 230 nM。ARN19702 具有广泛的镇痛作用。


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ARN19702 是一种选择性,具有口服活性的,可逆的,可透过血脑屏障的 N-乙酰乙醇胺酸酰胺酶 (NAAA) 抑制剂,对人 NAAA 的 IC50为 230 nM。ARN19702 具有广泛的镇痛作用。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 563 | 现货 | |
| 5 mg | ¥ 1,230 | 现货 | |
| 10 mg | ¥ 1,990 | 现货 | |
| 25 mg | ¥ 3,890 | 现货 | |
| 50 mg | ¥ 5,550 | 现货 | |
| 100 mg | ¥ 7,550 | 现货 | |
| 200 mg | ¥ 9,870 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 1,220 | 现货 |
| 产品描述 | ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC 50 of 230 nM for human NAAA. ARN19702 exhibits a broad analgesic profile [1] [2]. |
| 靶点活性 | NAAA:230 nM |
| 体内活性 | ARN19702 (3-10 mg/kg; po; daily; for 7 consecutive days) reduces nociception associated with Paclitaxel-induced neuropathy without development of subacute antinociceptive tolerance in male rats [1]. In male mice, ARN19702 (0.1-30 mg/kg; po) dose-dependently reduces the spontaneous nocifensive response elicited by intraplantar formalin injection and the hypersensitivity caused by intraplantar carrageenan injection, paw incision, or sciatic nerve ligation [1].. ARN19702 (3-10 mg/kg; po) produces remarkable protective effects against multiple sclerosis in mice [2]. Pharmacokinetic properties of ARN19702 in mice 3 mg/kg,i.v 3 mg/kg, p.o. C max (ng/mL) 1660±166 613±68 T max (min) (5.0) 30 CL (mL/min/Kg) 33.2±1.6 49±8 t 1/2 (min) 73.9±3.7 104±16 AUC plasma (h×ng/mL) 1366.8±68.3 988±157 AUC brain (h×ng/mL) 404.3±109.1 181±28 F (%) - 72±11 |
| 分子量 | 447.55 |
| 分子式 | C21H22FN3O3S2 |
| CAS No. | 1971937-18-4 |
| Smiles | CCS(=O)(=O)c1ccccc1C(=O)N1CCN(C[C@@H]1C)c1nc2ccc(F)cc2s1 |
| 密度 | 1.359 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 50 mg/mL (111.72 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.47 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
对于不同动物的给药剂量换算,您也可以参考 更多