CCR5 antagonist 3
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.
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- CAS. Nr.: 1800570-92-6
- Formel: C30H41F2N5O2S
- Molecular Weight:573.74
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
| 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD rats[1]
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Dosage:2 mg/kg and 10 mg/kg
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Administration:Intravenous and oral administration (Pharmacokinetic Analysis)
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Result:Displayed good PK profiles.
Chemical Information
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CAS. Nr. 1800570-92-6
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Molecular Weight 573.74
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Formel C30H41F2N5O2S
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SMILES
CC(N(C1)CCC2=C1N=C(C)N2[C@@H]3C[C@H]4N(CC[C@@H](C5=CSC=C5)NC(C6CCC(F)(CC6)F)=O)[C@@H](C3)CC4)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
CCR5 antagonist 3 Related Classifications
HY-152132 Related Classifications
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