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Pradigastat

Catalog No. T11827   CAS 956136-95-1
Synonyms: ANJ908, LCQ908-NXA, LCQ908A, LCQ-908

Pradigastat (LCQ-908) is an orally active, potent and selective diacylglycerol acyltransferase 1 (DGAT1) inhibitor for the treatment of constipation, which may be used in the study of obesity and diabetes.

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Pradigastat Chemical Structure
Pradigastat, CAS 956136-95-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 113.00
2 mg 5 days $ 163.00
5 mg In stock $ 283.00
1 mL * 10 mM (in DMSO) 5 days $ 297.00
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Purity: 95.21%
Purity: 95.21%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Pradigastat (LCQ-908) is an orally active, potent and selective diacylglycerol acyltransferase 1 (DGAT1) inhibitor for the treatment of constipation, which may be used in the study of obesity and diabetes.
Targets&IC50 bovine 5-HT1D:6.6 (pKi), Rat hippocampus 5-HT1A receptor:6.3 (pKi), H1:6.5 (Rat, pKi), rat 5-HT2A:6.5 (pKi), Ca2+ channel:5.6 (Rat, pKi), Histamine H2:6.6 (guinea-pig, pKi)
In vitro Pradigastat inhibits BCRP-mediated efflux activity in BCRP-overexpressing human ovarian cancer cell lines in a dose-dependent manner, with an IC50 value of 5 μM. Similarly, pradigastat demonstrates concentration-dependent inhibition of OATP1B1, OATP1B3 (estradiol 17β-glucuronide transport), and OAT3 (sulfated estrone-3-sulfate transport), with estimated IC50 values of 1.66 ± 0.95 μM, 3.34 ± 0.64 μM, and 0.973 ± 0.11 μM, respectively.3].
In vivo Research indicates that Pradigastat (LCQ-908) can inhibit postprandial triglyceride levels in rats, dogs, and monkeys. In rats with eliminated lipoprotein lipase (LPL) activity, Pradigastat reduces postprandial plasma triglyceride accumulation. Additionally, Pradigastat lowers the rate of postprandial chylomicron triglyceride (CM-TG) secretion into the lymphatic system and decreases chylomicron particle size[2].
Synonyms ANJ908, LCQ908-NXA, LCQ908A, LCQ-908
Molecular Weight 455.47
Formula C25H24F3N3O2
CAS No. 956136-95-1

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: <0.1 mg/mL (Insoluble)

DMSO: 50 mg/mL (109.78 mM), Sonification is recommended.

TargetMolReferences and Literature

1. Meyers CD, et al. Effect of the DGAT1 inhibitor pradigastat on triglyceride and apoB48 levels in patients with familial chylomicronemia syndrome. Lipids Health Dis. 2015 Feb 18;14:8. 2. Charles DanielMeyersMD, et al. The DGAT1 inhibitor pradigastat decreases chylomicron secretion and prevents postprandial triglyceride elevation in humans. Journal of Clinical Lipidology. Volume 7, Issue 3, May-June 2013, Page 285. 3. Kulmatycki K, et al. Evaluation of a potential transporter-mediated drug interaction between ZD 4522 and pradigastat, a novel DGAT-1 inhibitor. Int J Clin Pharmacol Ther. 2015 May;53(5):345-55.

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Keywords

Pradigastat 956136-95-1 Metabolism Transferase ANJ908 LCQ908 LCQ908-NXA LCQ908A LCQ 908 LCQ-908 inhibitor inhibit

 

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