CCR5 antagonist 3 (Compound 26) 是一种CCR5拮抗剂，其IC50为 15.90 nM。CCR5 antagonist 3 显示广谱抗HIV-1活性。
| 生物活性 | CCR5 antagonist3 (Compound 26) is aCCR5antagonist with anIC50of 15.90 nM.CCR5 antagonist3 shows broad-spectrum anti-HIV-1activities[1]. |
| IC50& Target[1] | CCR5 15.90 nM (IC50) | HIV-1 0.010 μM (EC50, In TZM-bl cells) |
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体外研究
(In Vitro) | CCR5 antagonist 3 (Compound 26) (48 h) shows excellent HIV-1 inhibitory activity with an EC50of 0.010 ± 0.004 μM in TZM-bl cells[1].
CCR5 antagonist 3 (48 h) shows antiviral activities with an EC50of 2.71 ± 0.34 nM against CCR5-tropic integrase inhibitor resistant strain HIV-1YU-2(G140S/Q148H)in TZM-bl cells[1].
CCR5 antagonist 3 shows HIV-1 inhibitory activity with EC50s of 2.89, 5.26, 7.64, 9.96 and 19.01 nM against HIV-1 strains YU-2, KIZ001, SF162, Ba-L and KIZ006 respectively[1].
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体内研究
(In Vivo) | PK Properties of CCR5 antagonist 3 (Compound 26) 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 3 | p.o. | 10 | 66.4 ± 64.0 | 2.67 ± 1.15 | 6.44 ± 2.10 | 249 ± 149 | 270 ± 145 | 9.16 ± 4.17 | – | 11.9 | | i.v. | 2 | – | – | 3.34 ± 1.55 | 420 ± 36 | 426 ± 34 | 2.43 ± 0.74 | 78.7 ± 6.6 | |
| 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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