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Lamivudine (BCH-189)

Cat. No. M3352
Lamivudine (BCH-189) Structure
Synonym:

BCH-189

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
50mg USD 52  USD52 In stock
100mg USD 78  USD78 In stock
500mg USD 194  USD194 In stock
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Quality Control & Documentation
Biological Activity

Lamivudine (BCH-189) is a potent nucleoside analog reverse transcriptase inhibitor with an IC50 of 2.7 mM. The pH-driven uptake of TEA by BBMV (pHin = 6.0, pHout = 7.5) was inhibited by lamivudine. The IC50 value (concentration resulting in 50% inhibition) for the concentration-dependent effect of lamivudine on TEA uptake by BBMV after 30 s was 2668 uM whereas IC50 values for cimetidine and trimethoprim were < 2.5 uM and < 25 uM, respectively. The early uptake of TEA by BLMV was also reduced significantly by lamivudine. The IC50 value for the concentration-dependent effect of lamivudine on uptake of TEA by BLMV at 30 s was > 25 mM, whereas the IC50 values for cimetidine and trimethoprim were 2116 uM and 445uM, respectively.

Chemical Information
Molecular Weight 229.26
Formula C8H11N3O3S
CAS Number 134678-17-4
Solubility (25°C) Water 50 mg/mL
DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Lesley J Scott. Dolutegravir/Lamivudine Single-Tablet Regimen: A Review in HIV-1 Infection

[2] Pedro Cahn, et al. Durable Efficacy of Dolutegravir Plus Lamivudine in Antiretroviral Treatment-Naive Adults With HIV-1 Infection: 96-Week Results From the GEMINI-1 and GEMINI-2 Randomized Clinical Trials

[3] Princy N Kumar, et al. Lamivudine for the treatment of HIV

[4] Tim Ibbotson, et al. Lamivudine/zidovudine/abacavir: triple combination tablet

[5] D J Porche. Lamivudine

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