| Chemical Properties | Back Directory | [Boiling point ]
526.1±50.0 °C(predicted) | [density ]
1.307±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [pka]
3.54±0.28(predicted) |
| Hazard Information | Back Directory | [Uses]
LBA-3 is a selective, orally active inhibitor for sodium-coupled citrate transporter SLC13A5, with an IC50 of 67 nM. LBA-3 decreases levels of triglyceride and total cholesterol in oleic and palmitic acid (OPA)-stimulated AML12 cells, PCN-stimulated primary mouse hepatocytes and in mouse models, without detectable toxicity. LBA-3 is blood-brain barrier permeable[1]. | [in vivo]
LBA-3 (50 mg/kg, po, single dose) exhibits a pharmacokinetic profil in Sprague Dawley rats, with peak plasma concentration Cmax of 288?262.00 μg/L, AUC of 704?570.43 h/μg–1·L and an oral bioavailability of 48.67%[1]. | [References]
[1] Zhang L, et al., Discovery of Highly Potent Solute Carrier 13 Member 5 (SLC13A5) Inhibitors for the Treatment of Hyperlipidemia. J Med Chem. 2024 Apr 25;67(8):6687-6704. DOI:10.1021/acs.jmedchem.4c00260 |
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