



| 货号 | 包装规格 | 操作 |
|---|---|---|
| SML2985-5MG | 5 mg | |
| SML2985-25MG | 25 mg |
≥98%(HPLC)
AM-0902 (AMG0902) is a potent and selective transient receptor potential A1 (TRPA1) antagonist (rat/human TRPA1 IC50 = 71/131 nM against AITC-induced 45Ca2+ influx in respective CHO transfectants with [AITC] = EC90 = 3 μM/hTRPA1 or 35 μM/rTRPA1; human/rat IC50 = 24/20 nM by FLIPR) with little potency against human TRPV1/4, human CYP3A4/2D6, rat TRPV1/3, rat TRPM8, or mouse NaV1.7. AM-0902 effectively reduces AITC-induced flinching in a rat pain model (by 65% and 85%, respectively, with 10 or 30 mg/kg AM-0902 p.o. 1 hr prior to AITC injection) with good pharmacokinetic properties, oral availability and brain exposure (F = 60%, B/P = 0.2; 30 mg/kg p.o. in rats) in vivo.
脑渗透剂、口服活性、强效和选择性瞬时受体电位A1(TRPA 1)拮抗剂,在体内对大鼠AITC诱导的退缩有效。
| 英文名称 | AM-0902 |
| CAS 号 | 1883711-97-4 |
| 经验分子式 | C17H15ClN6O2 |
| 分子量 | 370.79 |
| UNSPSC | 51111800 |
| NACRES | NA.77 |
| SMILES字符串 | Clc1ccc(cc1)CCc2n[o]c(n2)C[n]3[c](c4[n](cnc4nc3)C)=O |
| InChI key | 联合国开发计划署 |
| InChI | 1S/C17H15ClN6O2/10 - 20 -16-15(23)17(25)24(10-20-16)8-14- 2,1 -13(22-26-14)7-4-11-2-5-12(18)6-3-11/h2- 3,5 - 6,9 -10H,4,7-8H2,1H3 |
| 含量测定 | ≥98%(HPLC) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| 溶解性 | DMSO: 2 mg/mL,清澈 |
| 储存温度 | 2-8°C |
| 质量等级 | 100 |
| 包装规格(货号 SML2985-5MG) | 5 mg |
| 包装规格(货号 SML2985-25MG) | 25 mg |