HLB-0532247
HLB-0532247 is a cell-permeable phosphoramidate prodrug of 3'-deoxy-3',4'-didehydrocytidine (ddhC). HLB-0532247 increases the intracellular level of the endogenous antiviral nucleotide ddhCTP (HY-128788). HLB-0532247 reduces the titers of Zika virus and West Nile virus in cell cultures. HLB-0532247 can be used in studies related to Zika virus infection, West Nile virus infection, and coronavirus infection.
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- CAS No.: 2850362-12-6
- Formule: C21H27N4O8P
- Masse moléculaire:494.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
HLB-0532247 (0.1-1.0 mM) potently reduces Zika virus levels by more than 1 log10 pfu/mL at a concentration of 0.1 mM in HUH7 and HUH7.5 cells after 4 days, while it shows weak activity in Vero cells[1].
HLB-0532247 (1.0 mM) potently reduces West Nile virus levels by more than 4 log10 pfu/mL in HUH7 and HUH7.5 cells, but shows no activity in Vero cells[1].
HLB-0532247 (1.0 mM; 2-5 days) shows no cytotoxicity in Vero and HUH7 cells after 2 days of treatment, and only exhibits mild toxicity (cell viability >60%) after 5 days of treatment at 1.0 mM, with its CC50 greater than 1 mM[1].
HLB-0532247 (2 μM; 0-120 min) is stable in plasma, with a remaining proportion of >87% after incubation at 37°C for 2 hours[1].
HLB-0532247 (2 μM; 0-360 min) shows stable properties in simulated gastric fluid, with approximately 76% remaining after incubation at 37°C for 6 hours[1].
HLB-0532247 (2-10 μM; 2 h) exhibits a mean apparent permeability coefficient of 0.3 nm/sec in Caco-2 cells, showing cellular permeability similar to that of sofosbuvir[1].
HLB-0532247 (100 μM; 24 h) is metabolized to ddhCTP in HUH7 cells. After treatment with 100 μM for 24 h, 3.8 nmol of ddhCTP is produced per 5×106 cells (intracellular concentration >1 mM), representing a 29-fold increase compared with cells treated with ddhC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Vero, HUH7
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Concentration:1.0 mM
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Incubation Time:2 day, 5 day
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Result:Showed no cytotoxicity in Vero or HUH7 cells after 2 days.
Caused only modest toxicity with >60% cell viability at 1.0 mM after 5 days.
Had a CC50 greater than 1 mM.
Chemical Information
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CAS No. 2850362-12-6
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Masse moléculaire 494.43
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Formule C21H27N4O8P
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SMILES
NC(C=CN1[C@H]2[C@H](O)C=C(CO[P@](OC3=CC=CC=C3)(N[C@@H](C)C(OC(C)C)=O)=O)O2)=NC1=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Passow KT, et al. A Chemical Strategy for Intracellular Arming of an Endogenous Broad-Spectrum Antiviral Nucleotide. J Med Chem. 2021;64(20):15429-15439. [Content Brief]
[2]. Zhu M, et al. CMPK2 is a host restriction factor that inhibits infection of multiple coronaviruses in a cell-intrinsic manner. PLoS Biol. 2023;21(3):e3002039. Published 2023 Mar 17. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)