Ciapavir
Ciapavir (SBI-0953294) is a HIV-1 latency-reversing agent. Ciapavir reverses latent HIV-1 reservoir in vitro and in vivo without inducing systemic T cell activation or broad cytokine release. Ciapavir degrades cIAP1 and activates non-canonical NF-κB pathway. Ciapavir can be used for the research of HIV-1 infection.
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- No. CAS: 2433895-70-4
- Fòrmula: C54H70N8O8S2
- Peso molecular:1023.31
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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HIV-1 |
cIAP |
Ciapavir (0.1-10000 nM; 48 h) mediates HIV-1 latency reversal in 2D10 Jurkat cells through activation of the non-canonical NF-κB pathway[1].
Ciapavir (1-10 μM; 24 h) does not trigger cytokine release or T cell activation in human PBMCs or resting CD4+ T cells at concentrations up to 10 μM[1].
Ciapavir (0.1-10000 nM; 48 h) synergizes with BET inhibitors JQ1 (HY-13030) and I-BET151 (HY-13235) to enhance HIV-1 latency reversal in 2D10 Jurkat cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ciapavir (10-20 mg/kg; i.p.; single dose) induces latent HIV-1 expression in antiretroviral therapy-treated BLT mice without overt immune activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B6.129S-Rag2tm1Fwa Cd47tm1Fpl Il2rgtm1Wjl/J (male and female, 3 months old)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:I.p., single dose
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Result:Caused three of nine treated mice to exhibit increases in plasma HIV RNA 48 hours post-administration.
caused four of six mice in the 20 mg/kg group to show a significant increase in bone marrow HIV RNA.
Did not cause significant upregulation of CD69 in blood CD45+ cells or CD4+ T cells, or in bone marrow CD45+ cells.
Induced modest CD69 upregulation in bone marrow CD4+ T cells at 10 mg/kg but not 20 mg/kg.
Chemical Information
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No. CAS 2433895-70-4
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Peso molecular 1023.31
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Fòrmula C54H70N8O8S2
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SMILES
O=C([C@H]1N2[C@](SCC[C@@H](C2=O)NC([C@H](C)NC)=O)([H])CC1(C)C)N[C@@H](C3=CC=CC=C3C4)[C@@H]4OCC#CC#CCO[C@@H]5CC6=CC=CC=C6[C@@H]5NC([C@H]7N8[C@](SCC[C@@H](C8=O)NC([C@H](C)NC)=O)([H])CC7(C)C)=O
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Synonyms
SBI-0953294
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ciapavir Related Classifications
HY-134844 Related Classifications
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