Lamivudine-15N,d2
Lamivudine-15N,d2 is 15N and deuterated labeled Lamivudine (HY-B0250). Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS.
For research use only. We do not sell to patients.
- Formula: C8H10D2ClN215NO3S
- Molecular Weight:268.72
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Lamivudine (1 μM) is potent inhibitor of hepatitis B virus (HBV) replication, shows antiviral activity in primary duck hepatocyte (PDH) cultures derived from ducklings congenitally infected with the duck hepatitis B virus (DHBV)[2].
Lamivudine (0-20 μM; 2, 4, 9 d) inhibits DHBV replication with 50% inhibitory concentration of 0.55 μM[2].
Lamivudine, combinded with penciclovir (9-[2-hydroxy-1-(hydroxymethyl)ethoxymethyl]guanine [PCV]), (1 μM; 2, 4, 9 d) shows synergistic effect, acts potent function in reducing the normally recalcitrant viral covalently closed circular (CCC) DNA form of DHBV[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Lamivudine (50 mg/kg; i.p.; single dose) penetrates well in CNS and localizes in brain regions susceptible to HIV neurodegeneration in rat[4].
Pharmacokinetic Parameters of Lamivudine in HIV-infected Rats[4]
| Parameter | Cmax (μg/mL) | Tmax (h) | T1/2 (h) | AUC (h·ng/mL) |
| Plasma | 25,846 | 0.25 | 0.68 | 22,172 |
| Brain | 272 | 0.5 | 1.2 | 967 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 134678-17-4
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Molecular Weight 268.72
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Formula C8H10D2ClN215NO3S
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SMILES
OC([2H])([2H])[C@@H]1O[C@H](N2C=CC([15NH2])=NC2=O)CS1.Cl
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Synonyms
BCH-189-15N,d2
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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.
Purity & Documentation
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[2]. Colledge D, et al. Synergistic inhibition of hepadnaviral replication by lamivudine in combination with penciclovir in vitro. Hepatology. 1997 Jul;26(1):216-25. [Content Brief]
[3]. Olaniyan LW, et al. Lamivudine-Induced Liver Injury. Open Access Maced J Med Sci. 2015 Dec 15;3(4):545-50. [Content Brief]
[4]. Mdanda S, et al. Zidovudine and Lamivudine as Potential Agents to Combat HIV-Associated Neurocognitive Disorder. Assay Drug Dev Technol. 2019 Oct;17(7):322-329. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Lamivudine-15N,d2 Related Classifications
HY-B0250S Related Classifications
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