1800570-92-6
1800570-92-6 structure
- Name: CCR5 antagonist 3
- Chemical Name: CCR5 antagonist 3
- CAS Number: 1800570-92-6
- Molecular Formula: C30H41F2N5O2S
- Molecular Weight: 573.74
- Catalog: Signaling Pathways Anti-infection HIV
- Create Date: 2023-01-26 17:51:50
- Modify Date: 2024-04-05 21:52:38
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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].
| Name | CCR5 antagonist 3 |
|---|
| 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]. |
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| 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 |
| Molecular Formula | C30H41F2N5O2S |
|---|---|
| Molecular Weight | 573.74 |