CCR5 antagonist 2
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.
For research use only. We do not sell to patients.
- CAS No.: 1800570-93-7
- Formula: C32H45F2N5O2S
- Molecular Weight:601.79
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CCR5 8.34 nM (IC50) |
HIV-1 11 nM (EC50, TZM-bl cell) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HOS | CC50 |
>200 μM
Compound: 25
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Cytotoxicity against human HOS-CD4-CCR5 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human HOS-CD4-CCR5 cells incubated for 48 hrs by MTT assay
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[PMID: 36472561] |
| PBMC | CC50 |
81.7 μM
Compound: 25
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Cytotoxicity against human PBMC cells incubated for 48 hrs by MTT assay
Cytotoxicity against human PBMC cells incubated for 48 hrs by MTT assay
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[PMID: 36472561] |
| TZM | CC50 |
>200 μM
Compound: 25
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Cytotoxicity against human TZM-bl cells incubated for 48 hrs by MTT assay
Cytotoxicity against human TZM-bl cells incubated for 48 hrs by MTT assay
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[PMID: 36472561] |
CCR5 antagonist 2 (Compound 25) (48 h) shows excellent HIV-1 inhibitory activity with an EC50 of 0.011 ± 0.002 μM in TZM-bl cells[1].
CCR5 antagonist 2 (48 h) shows antiviral activities with an EC50 of 4.34 ± 1.61 nM against CCR5-tropic integrase inhibitor resistant strain HIV-1YU-2(G140S/Q148H) in TZM-bl cells[1].
CCR5 antagonist 2 shows HIV-1 inhibitory activity with EC50s of 7.82, 8.73, 12.61, 15.99 and 16.93 nM against HIV-1 strains KIZ001, YU-2, KIZ006, SF162 and Ba-L, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| 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 |
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 No. 1800570-93-7
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Molecular Weight 601.79
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Formula C32H45F2N5O2S
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SMILES
CC1=NC2=C(N1[C@H]3C[C@H]4N(CC[C@@H](C5=CSC=C5)NC(C6CCC(F)(CC6)F)=O)[C@@H](C3)CC4)CCN(C2)C(C(C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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