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CCR5 antagonist 3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CCR5 antagonist 3图片
CAS NO:1800570-92-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)

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].

体内研究
(In Vivo)

PK Properties of CCR5 antagonist 3 (Compound 26) in SD Rats[1]

compdadmindose (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 ± 4.1711.9
i.v.23.34 ± 1.55420 ± 36426 ± 342.43 ± 0.7478.7 ± 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.
分子量

573.74

Formula

C30H41F2N5O2S

CAS 号

1800570-92-6

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.