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化學性質:
規格 | 10mM (in 1mL DMSO) 10mg 50mg |
CAS | 136470-78-5 |
別名 | Ziagen |
化學名 | [(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methanol |
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 H2O |
儲存條件 | Store at -20°C |
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 |
產品描述:
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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原創作者:上海莼試生物技術有限公司
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賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
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