CCR5 antagonist 2 (Compound 25) 是一种CCR5拮抗剂，其IC50为 8.34 nM。CCR5 antagonist 2 显示广谱抗HIV-1活性。
| 生物活性 | CCR5 antagonist2 (Compound 25) is aCCR5antagonist with anIC50of 8.34 nM.CCR5 antagonist2 shows broad-spectrum anti-HIV-1activities[1]. |
| IC50& Target[1] | CCR5 8.34 nM (IC50) | HIV-1 11 nM (EC50, TZM-bl cell) |
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体外研究
(In Vitro) | CCR5 antagonist 2 (Compound 25) (48 h) 在 TZM-bl 细胞中表现出优异的 HIV-1 抑制活性，EC50为 0.011 ± 0.002 μM[1]。
CCR5 antagonist 2 (48 h) 对 TZM-bl 细胞中亲 CCR5 整合酶抑制剂耐药株 HIV-1YU-2(G140S/Q148H)具有抗病毒活性，EC50为 4.34 ± 1.61 nM[1]。
CCR5 antagonist 2 对 HIV-1 菌株 KIZ001、YU-2、KIZ006、SF162 和 Ba-L 有抑制作用，EC50分别为 7.82、8.73、12.61、15.99 和 16.93 nM[1]。
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体内研究
(In Vivo) | PK Properties of CCR5 antagonist 2 (Compound 25) in SD Rats[1]
| compd | admin | dose (mg/kg) | Cmax(ng/mL) | Tmax(h) | T1/2(h) | AUC0–last(ng·h/mL) | AUC0–∞(ng·h/mL) | MRT (h) | CL (mL/min/kg) | F (%) | | CCR5 antagonist 2 | p.o. | 10 | 49.5 ± 18.6 | 2.0 ± 0.0 | 10.3 ± 2.5 | 229 ± 92 | 283 ± 105 | 13.2 ± 4.2 | – | 15.7 | | i.v. | 2 | – | – | 1.60 ± 0.03 | 291 ± 75 | 298 ± 76 | 1.81 ± 0.04 | 117 ± 29 | |
| Animal Model: | SD rats[1] | | Dosage: | 2 mg/kg and 10 mg/kg | | Administration: | Intravenous and oral administration (Pharmacokinetic Analysis) | | Result: | Displayed good PK profiles. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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