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GSK-2330672, also known as linerixibat, is a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (IC50 = 42 nM) for the research of type 2 diabetes. In vivo, Linerixibat (0.05-10 mg/kg; oral gavage; twice daily for 14 days) treatment on male ZDF rat lowers glucose in an animal model of type 2 diabetes.
Fecal Collection in Rat.
Male ZDF rats arrived at seven weeks of age (±3 days). After a one-week acclimation period, rats were assigned to different treatment groups (n =6−8/group) based upon baseline glucose/vehicle (0.5% hydroxypropyl methylcellulose (HPMC), 0.1% Tween80); one vehicle group for each compound) and six doses (0.05, 0.1, 0.5, 1, 5, and 10 mg/kg) of compounds 20, 45, and GSK2330672 (56). All treatments were given via oral gavage twice a day. Fecal samples were collected for 24 h on day 7 of treatment.
Metabolic Effects in ZDF Rats.
Male ZDF rats arrived at seven weeks of age (±3 days). After a one-week acclimation period, rats were anesthetized with isoflurane and tail-vein blood samples were collected at 0900 without fasting. To ensure balanced treatment groups, ZDF rats were assigned to six treatment groups based upon baseline glucose/vehicle (0.5% hydroxypropyl methylcellulose (HPMC), 0.1%Tween80) and selected doses of compounds (0.05, 0.1, 0.5, 1, 5, and 10 mg/kg or 0.001, 0.01, 0.1, 1, and 10 mg/kg for compounds 20 and 45 or GSK2330672 (56), respectively). All treatments were given via oral gavage twice a day, and animals were followed for two weeks with blood samples collected from tail vein on day 14 at 0900 without fasting. Plasma samples were stored at −80 °C for further analyses.
https://pubmed.ncbi.nlm.nih.gov/23678871/
| Cell Experiment | |
|---|---|
| Cell lines | Caco2 cells |
| Preparation method | After pretreatment with 100 μM of CDCA for 6 h, Caco2 cells were treated with 50 μM TUDCA and 50 nM Linerixibat for 12 h. |
| Concentrations | 50 nM |
| Incubation time | 12 h |
| Animal Experiment | |
|---|---|
| Animal models | Wild-type male C57Bl6J/OlaHsd mice |
| Formulation | Not mentioned |
| Dosages | 10 mg/kg |
| Administration | Oral gavage |
| Molecular Weight | 546.68 |
| Formula | C28H38N2O7S |
| CAS Number | 1345982-69-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 37 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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