INCB9471
Based on 1 publication(s) in Google Scholar
INCB9471 is a potent, selective and orally active CCR5 antagonist. INCB9471 shows anti-HIV-1 activity.
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- CAS. Nr.: 869769-98-2
- Formel: C30H40F3N5O2
- Molecular Weight:559.67
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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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Publications Citing Use of MedChemExpress (MCE) INCB9471
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Biologische Aktivität
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CCR5 |
HIV-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
0.16 nM
Compound: 22a, INCB9471, diastereomer1
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Antiviral activity against HIV-1 BaL infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA
Antiviral activity against HIV-1 BaL infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA
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[PMID: 24900235] |
| PBMC | IC50 |
0.36 nM
Compound: 22a, INCB9471, diastereomer1
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Antiviral activity against HIV-1 ADA infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA
Antiviral activity against HIV-1 ADA infected in PHA-stimulated human PBMC cells assessed as viral p24 core protein level after 7 days by ELISA
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[PMID: 24900235] |
| PBMC | IC50 |
3 nM
Compound: 22a, INCB9471, diastereomer1
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Antagonist activity at CCR5 in IL-10 stimulated human PBMC cells assessed as MIP-1beta induced chemotaxis
Antagonist activity at CCR5 in IL-10 stimulated human PBMC cells assessed as MIP-1beta induced chemotaxis
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[PMID: 24900235] |
INCB9471 (0-1 µM) inhibits MIP-1 induced chemotaxis of rhIL-10-treated human monocytes with an IC50 value of 4.8 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| rats | dogs | ||
| i.v. | dose iv/po (mg/kg) | 1/20 | 1/20 |
| CL (L/h/kg) | 0.62 | 0.2 | |
| Vdss (L/h) | 4.1 | 3.8 | |
| T1/2 (h) | 6 | 11 | |
| AUC (nM h) | 2898 | 7854 | |
| p.o. | Tmax (h) | 3 | 0.5 |
| Cmax(ng/mL) | 4071 | 14007 | |
| C24h (nM) | 1088 | ||
| T1/2 (h) | 12 | 17 | |
| AUC (nM h) | 55160 | 149779 | |
| F (%) | 100 | 95 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 869769-98-2
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Molecular Weight 559.67
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Formel C30H40F3N5O2
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SMILES
CCO[C@H]1[C@H](N2[C@H](CN(C3(CCN(CC3)C(C4=C(C)N=CN=C4C)=O)C)CC2)C)C5=CC=C(C(F)(F)F)C=C5C1
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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.
Publications (1)
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Journal Impact Factor
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Most Recent
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APL Bioeng
Quercetin targets the Ccl4-Ccr5 axis to relieve neuropathic pain after spinal cord injury. [Abstract]2025 Jul 24;9(3):036108. PMID: 40717840
Reinheit & Dokumentation
Verweise
[1]. Shin N, et al. Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection. J Pharmacol Exp Ther. 2011 Jul;338(1):228-39. [Content Brief]
[2]. Xue CB, et al. Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity. ACS Med Chem Lett. 2010 Aug 25;1(9):483-7. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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