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BMS303141

Cat. No. M3762
BMS303141 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 60  USD60 In stock
10mg USD 100  USD100 In stock
50mg USD 350  USD350 In stock
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Quality Control & Documentation
Biological Activity

BMS303141 blocks lipid synthesis (IC50 = 8 μM in HepG2 cells). Under identical incubation conditions, BMS-303141 showed no cytotoxicity up to 50 μM, indicating the observed inhibition of lipid synthesis was not a result of compound-induced cytotoxicity. BMS303141 Lowers plasma glucose and triglycerides in a mouse model of hyperlipidemia. BMS303141 is Orally bioavailable.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models BALB/c nude mice (4‐5 weeks old) injected HepG2 cells
Formulation saline
Dosages 5 mg/kg/d for 8 days
Administration gavage
Chemical Information
Molecular Weight 424.3
Formula C19H15Cl2NO4S
CAS Number 943962-47-8
Solubility (25°C) DMSO ≥ 20 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] Yihu Zheng, et al. J Cell Mol Med. ATP citrate lyase inhibitor triggers endoplasmic reticulum stress to induce hepatocellular carcinoma cell apoptosis via p-eIF2α/ATF4/CHOP axis

[2] Ma Z, et al. J Lipid Res. A novel direct homogeneous assay for ATP citrate lyase.

[3] Li JJ, et al. Bioorg Med Chem Lett. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.

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