阿巴卡韦是一种具有口服活性和竞争性的核苷类逆转录酶抑制剂。
| Cas No. | 136470-78-5 |
| 别名 | 阿巴卡韦 |
| 化学名 | [(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methanol |
| Canonical SMILES | C1CC1NC2=NC(=NC3=C2N=CN3C4CC(C=C4)CO)N |
| 分子式 | C14H18N6O |
| 分子量 | 286.33 |
| 溶解度 | ≥ 30.7 mg/mL in DMSO with gentle warming, ≥ 39.3 mg/mL in EtOH with gentle warming, ≥ 7.16 mg/mL in Water |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50 Value: 0.26 microM for HIV-1[1] Abacavir,(-)-(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol, is a novel purine carbocyclic nucleoside analogue that has been approved by the FDA for the treatment of HIV (as Ziagen trade mark [abacavir sulfate]) [2]. in vitro: In erythrocytes, abacavir influx was rapid, nonsaturable (rate constant=200 pmol/s/mM/microl cell water), and unaffected by inhibitors of nucleoside or nucleobase transport[2]. in vivo: pharmacokinetic, distribution, and toxicological profiles of 1592U89 were distinct from and improved over those of CBV, probably because CBV itself was not appreciably formed from 1592U89 in cells or animals (<2%). The 5'-triphosphate of CBV was a potent, selective inhibitor of HIV-1 RT, with Ki values for DNA polymerases (alpha, beta, gamma, and epsilon which were 90-, 2,900-, 1,200-, and 1,900-fold greater, respectively, than for RT (Ki, 21 nM). 1592U89 was relatively nontoxic to human bone marrow progenitors erythroid burst-forming unit and granulocyte-macrophage CFU (IC50s, 110 microM) and human leukemic and liver tumor cell lines[1]. Clinical trial: Estimate The Effect Of Lersivirine On The Pharmacokinetics Of Abacavir + Lamivudine In Healthy Subjects. Phage1 |
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