CCR5 antagonist 3
Names
[ CAS No. ]:
1800570-92-6
[ Name ]:
CCR5 antagonist 3
Biological Activity
[Description]:
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[1].
[Related Catalog]:
[Target]
CCR5:15.90 nM (IC50)
HIV-1:0.010 μM (EC50, In TZM-bl cells)
[In Vitro]
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[1]. 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[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].
[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.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C30H41F2N5O2S
[ Molecular Weight ]:
573.74