CCR5 antagonist 2
Names
[ CAS No. ]:
1800570-93-7
[ Name ]:
CCR5 antagonist 2
Biological Activity
[Description]:
CCR5 antagonist 2 (Compound 25) is a CCR5 antagonist with an IC50 of 8.34 nM. CCR5 antagonist 2 shows broad-spectrum anti-HIV-1 activities[1].
[Related Catalog]:
[Target]
CCR5:8.34 nM (IC50)
HIV-1:11 nM (EC50, TZM-bl cell)
[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]。
[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.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C32H45F2N5O2S
[ Molecular Weight ]:
601.79