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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CCR5 8.34 nM (IC50) |
HIV-1 11 nM (EC50, TZM-bl cell) |
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
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 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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CCR5 antagonist 2 Related Classifications
HY-152131 Related Classifications
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