Linerixibat

製品コードS3529 バッチS352901

印刷

化学情報

Chemical Structure Synonyms GSK2330672 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C28H38N2O7S
分子量 546.68 CAS No. 1345982-69-5
Solubility (25°C)* 体外 DMSO 50 mg/mL (91.46 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Linerixibat (GSK 2330672, GSK 672), a highly potent, nonabsorbable inhibitor of apical sodium dependent bile acid transporter (ABST), also known as the ileal bile acid transporter (IBAT), is used to the treatment of cholestatic pruritus in primary biliary Cholangitis. The IC50 of human ASBT is 42 nM.
in vitro

The zwitterionic, nonhygroscopic, crystalline salt form of Linerixibat shows good aqueous solubility at pH 7.4 (>7 mg/mL), excellent thermal stability, and does not generate reactive or humanspecific metabolite, characteristics.[3]
in vivo

Linerixibat (twice daily; for 14 days) treatment lowers glucose in an animal model of type 2 diabetes.[3]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human Multi-Drug Resistance 1-Madin-Darby Canine Kidney (HMDR1-) cells
濃度 3 μM
反応時間 30 min
実験の流れ

HMDR1-MDCK cells are seeded at 6.6 × 105 cells/well onto 12-well polycarbonate Transwells filter membranes with 0.4 μm pore size. After three days, media is removed from both the apical and basolateral chambers and replaced with transport buffer (HBSS containing 25 mM glucose and 25 mM HEPES) containing the P-gp inhibitor GF120918A at a final concentration of 2 μM. After a 30 min equilibration, the transport buffer is removed from the apical chambers and replaced with fastedstate simulated intestinal fluid containing 3 μM Linerixibat, 2 μM GF120918A, 25 mM glucose, and 250 μM Lucifer Yellow CH. Next, the transport buffer is removed from the basolateral chambers and replaced with transport buffer containing 1% (w/v) human serum albumin and 2 μM GF120918A. After 60 min incubation at 37 °C, samples are collected from the apical (donor) and basolateral (receiver) compartments and added to acetonitrile (1:1 and 1:2 (v/v), respectively). Receiver samples are then centrifuged and the supernatants are removed and analyzed by LC-MS/MS.
動物実験 動物モデル Male Zucker Diabetic Fatty (ZDF) rat
投薬量 0.05-10 mg/kg
投与方法 o.g.

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。