产品
编 号：F747126
分子式：C30H41F2N5O2S
分子量：573.74
分子式：C30H41F2N5O2S
分子量：573.74
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CAS No: 1800570-92-6
产品详情
生物活性：
CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities.
体内研究：
PK Properties of CCR5 antagonist 3 (Compound 26) in SD Ratscompdadmin 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 3p.o.1066.4 ± 64.02.67 ± 1.156.44 ± 2.10249 ± 149270 ± 1459.16 ± 4.17–11.9
i.v.2––3.34 ± 1.55420 ± 36426 ± 342.43 ± 0.7478.7 ± 6.6
Animal Model:SD rats
Dosage:2 mg/kg and 10 mg/kg
Administration:Intravenous and oral administration (Pharmacokinetic Analysis)
Result:Displayed good PK profiles.
体外研究：
CCR5 antagonist 3 (Compound 26) (48 h) shows excellent HIV-1 inhibitory activity with an EC50 of 0.010 ± 0.004 μM in TZM-bl cells.CCR5 antagonist 3 (48 h) shows antiviral activities with an EC50 of 2.71 ± 0.34 nM against CCR5-tropic integrase inhibitor resistant strain HIV-1YU-2(G140S/Q148H) in TZM-bl cells.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.
CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities.
体内研究：
PK Properties of CCR5 antagonist 3 (Compound 26) in SD Ratscompdadmin 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 3p.o.1066.4 ± 64.02.67 ± 1.156.44 ± 2.10249 ± 149270 ± 1459.16 ± 4.17–11.9
i.v.2––3.34 ± 1.55420 ± 36426 ± 342.43 ± 0.7478.7 ± 6.6
Animal Model:SD rats
Dosage:2 mg/kg and 10 mg/kg
Administration:Intravenous and oral administration (Pharmacokinetic Analysis)
Result:Displayed good PK profiles.
体外研究：
CCR5 antagonist 3 (Compound 26) (48 h) shows excellent HIV-1 inhibitory activity with an EC50 of 0.010 ± 0.004 μM in TZM-bl cells.CCR5 antagonist 3 (48 h) shows antiviral activities with an EC50 of 2.71 ± 0.34 nM against CCR5-tropic integrase inhibitor resistant strain HIV-1YU-2(G140S/Q148H) in TZM-bl cells.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.
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