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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  | In stock | |
| 5 mg | ¥ 1,230  | In stock | |
| 10 mg | ¥ 1,990  | In stock | |
| 25 mg | ¥ 3,890  | In stock | |
| 50 mg | ¥ 5,550  | In stock | |
| 100 mg | ¥ 7,550  | In stock | |
| 200 mg | ¥ 9,870  | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 1,220  | In stock | 
| 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.   | |||||||||||||||||||||||||||||||||||
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