[CAS NO. 956136-95-1] Pradigastat
PRODUCTS SPECIFICATIONS [956136-95-1]
DESCRIPTION [956136-95-1]
Overview
| MDL | MFCD25562905 |
|---|---|
| Molecular Weight | 455.47 |
| Molecular Formula | C25H24F3N3O2 |
| SMILES | O=C(O)C[C@H]1CC[C@H](C2=CC=C(C3=NC=C(NC4=CC=C(C(F)(F)F)N=C4)C=C3)C=C2)CC1 |
2 Publications Citing Use of MCE
Summary
Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects [1] [2] .
IC50 & Target
Diacylglycerol acyltransferase 1 (DGAT1) [1]
In Vitro
Pradigastat inhibits breast cancer resistance protein (BCRP)-mediated efflux activity in a dose-dependent fashion in a BCRP over-expressing human ovarian cancer cell line with an IC 50 value of 5 μM. Pradigastat inhibits OATP1B1, OATP1B3, and OAT3 activity in a concentration-dependent manner with estimated IC 50 values of 1.66 μM, 3.34 μM, and 0.973 μM, respectively [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pradigastat (LCQ-908) inhibits the postprandial triglyceride levels in rats, dogs and monkeys. In rats whose lipoprotein lipase (LPL) activity has been abolished, Pradigastat reduces the postprandial accumulation of plasma triglyceride. Pradigastat decreases the postprandial rate of chylomicron triglyceride (CM-TG) secretion into the lymphatic duct and reduces the size of chylomicrons [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01558323 | Novartis Pharmaceuticals|Novartis |
Renal Impairment
|
May 2012 | Phase 1 |
| NCT01387958 | Novartis Pharmaceuticals|Novartis |
Hepatitis C
|
July 2011 | Phase 2 |
| NCT01514461 | Novartis Pharmaceuticals|Novartis |
Familial Chylomicronemia Syndrome (FCS)
|
July 2012 | Phase 3 |
| NCT01594957 | Novartis Pharmaceuticals|Novartis |
Hepatic Impairment
|
April 2012 | Phase 1 |
| NCT01146522 | Novartis Pharmaceuticals|Novartis |
Hyperlipoproteinemia
|
May 2010 | Phase 1|Phase 2 |
| NCT01594983 | Novartis Pharmaceuticals|Novartis |
Non Familial Chylocmicronemia Syndrome (Non-FCS)
|
June 2012 | Phase 2 |
| NCT01474434 | Novartis Pharmaceuticals|Novartis |
Coronary Artery Disease|Hypertriglyceridemia
|
December 2011 | Phase 2 |
| NCT01589237 | Novartis Pharmaceuticals|Novartis |
Familial Chylomicronemia Syndrome (FCS) (HLP Type I)
|
February 2013 | Phase 3 |
| NCT01811472 | Novartis Pharmaceuticals|Novartis |
Non-alcoholic Fatty Liver Disease (NAFLD)
|
June 2013 | Phase 2 |
| NCT04620161 | Anji Pharma|Covance |
Functional Constipation
|
September 22, 2020 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 62.5 mg/mL ( 137.22 mM ; ultrasonic and warming and heat to 60°C)
H 2 O : < 0.1 mg/mL (insoluble)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1955 mL | 10.9777 mL | 21.9553 mL |
| 5 mM | 0.4391 mL | 2.1955 mL | 4.3911 mL |
| 10 mM | 0.2196 mL | 1.0978 mL | 2.1955 mL |
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Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.49 mM); Suspended solution; Need ultrasonic
References
- [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] 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.
- [3] 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.