L-689502是一个有效的HIV-1蛋白酶(HIV-lprotease)抑制剂,其IC50值为1nM。
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L-689502 is a potent inhibitor of HIV-l protease with an IC50 of 1 nM.
Both L694746 and L-689502 inhibit HIV-l ptotease activity in a concentration-dependent manner. Pepstatin is much less potent than either compound exhibiting an IC50 of 2 μM. L694746 is as potent as L-689502 in inhibiting the HIV-l protease despite being structurally different from L-689502[1].
[1]. Lingham RB, et al. HIV-1 protease inhibitory activity of L-694,746, a novel metabolite of L-689,502. Biochem Biophys Res Commun. 1991 Dec 31;181(3):1456-61.
Cell experiment: | G689502 (3.3 pmoles in 1 mL of 100% DMSO) is added to cultures that have been growing for 48 hr. The final substrate and DMSO concentrations during the fermentation period are 65 pM and 2%, respectively. The fermentations containing L-689502 are carried out for an additional 72-96 hr prior to be harvested.The whole broth is sequenthdly extracted with methanol (0.5 vol) and acetone (0.5 vol). The supematant containing the derivatives of L-689502 is separated from the mycelia by filtration[1]. |
参考文献: [1]. Lingham RB, et al. HIV-1 protease inhibitory activity of L-694,746, a novel metabolite of L-689,502. Biochem Biophys Res Commun. 1991 Dec 31;181(3):1456-61. |
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