BI01383298, Citrate transporter inhibitor

Product Details

Formal Name: 1-(3,5-Dichlorophenylsulfonyl)-N-(4-fluorobenzyl)piperidine-4-carboxamide

Molecular Formula: C₁₉H₁₉Cl₂FN₂O₃S

Formula Weight: 445.3

CAS Number: 2227549-00-8

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to at least 35 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

Citrate transporter inhibitor

Functions

Potent, non-competitive, irreversible inhibitor of the human Na⁺-coupled citrate transporter (NaCT/SLC13A5/mINDY).  IC₅₀ = 49 nM in the presence of Li⁺ with preincubation and 118 nM without Li⁺.  BI01393298 is inactive in mouse NaCT for citrate transport.  NaCT delivers citrate, a key metabolite and regulator of multiple biochemical pathways, from the blood to hepatocytes and neurons. Reduced expression of NaCT has been linked to longevity and increased expression has been linked to type 2 diabetes and non-alcoholic fatty liver disease.  BI01383298 also blocked transport of arginine, dimethylarginine, and L-homoarginine in both human and mouse NaCT.

Application Procedures

First dissolved in DMSO (35 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored under an inert atmosphere at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)