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BMS-303141

Catalog No.
B1079
ATP-citrate lyase inhibitor,potent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$99.00
In stock
10mg
$94.00
In stock
25mg
$187.00
In stock
50mg
$330.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

BMS-303141 (CAS 943962-47-8) is a small molecule inhibitor targeting ATP-citrate lyase (ACL), a cytoplasmic enzyme involved in converting citrate to acetyl-CoA, the essential precursor for de novo fatty acid and cholesterol biosynthesis. It inhibits ACL activity with an IC50 of 0.13 μM (0.94 μM for human ACL). In vitro studies using HepG2 cells show suppression of lipid synthesis (IC50 ~8 μM) without cytotoxicity up to 50 μM. In mouse models, oral administration of BMS-303141 reduces plasma triglyceride, cholesterol, and glucose levels, and restricts weight gain, highlighting its relevance for studying dyslipidemia, obesity, and metabolic disorders.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt424.3
Cas No.943962-47-8
FormulaC19H15Cl2NO4S
Solubility≥21.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name3,5-dichloro-2-hydroxy-N-(4-methoxy-[1,1'-biphenyl]-3-yl)benzenesulfonamide
SDFDownload SDF
Canonical SMILESCOC1=C(NS(C2=CC(Cl)=CC(Cl)=C2O)(=O)=O)C=C(C3=CC=CC=C3)C=C1
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

HepG2 cells

Preparation method

The solubility of this compound in DMSO is > 21.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

8 μM; 6 hrs

Applications

In HepG2 cells, BMS-303141 inhibited total lipid synthesis with an IC50 value of 8 μM. Moreover, BMS-303141 showed no cytotoxicity up to 50 μM.

Animal experiment [1]:

Animal models

High-fat fed mice

Dosage form

10 and 100 mg/kg; p.o.

Applications

In high-fat fed mice, BMS-303141 modestly reduced both plasma cholesterol and triglyceride 20 days after treatment. In addition, fasting plasma glucose started to decrease from day 7 to completion of the study.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Li JJ, Wang H, Tino JA, et al. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett, 2007, 17(11): 3208-3211.

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