(Rac)-Adibelivir
(Rac)-Adibelivir ((Rac)-IM-250) is a blood-brain barrier-penetrant HSV helicase-primase inhibitor and metabolic stabilizer with antiviral activity. (Rac)-Adibelivir is also effective against Acyclovir (HY-17422)-resistant strains, and its deuterated structure exhibits enhanced metabolic stability, reducing the formation of hydroxylated metabolites. (Rac)-Adibelivir prolongs in vivo half-life, reduces administration dosage, improves oral bioavailability, and achieves higher brain exposure in mice. (Rac)-Adibelivir can be used in the research of herpes simplex infection, herpes encephalitis and Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 2137928-83-5
- Formula: C20H19F2N3O2S2
- Molecular Weight:435.51
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Helicase |
(Rac)-Adibelivir (Example 7) inhibits wild-type HSV-1, HSV-2, and ACV-resistant HSV-1 replication in Vero cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Vero cells
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Concentration:IC50
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Incubation Time:/
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Result:Inhibited wild-type HSV-1, HSV-2, and ACV-resistant HSV-1 replication in Vero cells with IC50 values of 25-100 nM, 25-100 nM, and 25-100 nM, respectively.
(Rac)-Adibelivir (10 mg/kg; p.o.; single dose) enantiomer Example 4/2 achieves a brain-to-plasma ratio of 1.57 in mice after oral administration, with improved plasma and brain exposure relative to its non-deuterated matched pair[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6N Mice (male, 21-25 g)[1]
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Dosage:10 mg/kg (oral); 2 mg/kg (intravenous)
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Administration:p.o.; single dose; i.v.; single dose
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Result:Reached mean Cmax of 4607 ng/mL, mean AUC(0-tz) of 80231 ng*h/mL, and mean bioavailability of 201% after oral administration.
Reached mean C0 of 16.2 ng/mL, mean AUC(0-tz) of 7997 ng*h/mL, mean AUC(0-inf) of 10648 ng*h/mL, mean elimination half-life (t1/2z) of 11.3 h, mean clearance (CL) of 188 mL/(h*kg), and mean volume of distribution (Vz) of 3074 mL/kg after intravenous administration.
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Animal Model:C57Bl/6N Mice (21-26 g)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Achieved mean plasma concentration of 5474 ng/mL, mean brain concentration of 8609 ng/mL, and brain-to-plasma ratio of 1.57 at 4 hours post-dose.
Chemical Information
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CAS No. 2137928-83-5
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Appearance Powder
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Molecular Weight 435.51
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Formula C20H19F2N3O2S2
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SMILES
FC(C=CC(F)=C1)=C1C(C=C2)=CC=C2CC(N(C3=NC(C)=C(S(C)(=N)=O)S3)C)=O
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Synonyms
(Rac)-IM-250
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(Rac)-Adibelivir Related Classifications
HY-150306A Related Classifications
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