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| 5mg |
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| 25mg |
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Purity: ≥98%
Pradigastat (formerly also known as LCQ-908; LCQ908) is a novel, potent and orally bioavailable diacylglycerol acyltransferase 1 (DGAT1) inhibitor being developed for the treatment of familial chylomicronemia syndrome. It is also being studied in phase II clinical trials as an anti-obesity and anti-diabetic agent. Familial chylomicronemia syndrome (FCS) is a rare lipid disease caused by complete lipoprotein lipase (LPL) deficiency resulting in fasting chylomicronemia and severe hypertriglyceridemia. Inhibition of diacylglycerol acyltransferase 1 (DGAT1), which mediates chylomicron triglyceride (TG) synthesis, is an attractive strategy to reduce TG levels in FCS .
| ln Vitro |
In human ovarian cancer cell lines that overexpress BCRP, prediastat suppresses the protein's dose-dependent efflux activity, with an IC50 value of 5 μM. Estimated IC50 values for pradigastat's concentration-dependent inhibition of OATP1B1, OATP1B3, and OAT3 are 1.66 μM, 3.34 μM, and 0.973 μM, respectively [2].
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| ln Vivo |
In rats, dogs, and monkeys, digastat (LCQ-908) lowers their postprandial triglyceride levels. Rats with no longer having lipoprotein lipase (LPL) activity have less postprandial plasma triglyceride buildup when given pradigastat. Pradigastat reduces the size of chylomicrons and the postprandial rate of chylomicron triglyceride (CM -TG) secretion into the lymphatic duct[3].
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| 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. |
| Molecular Formula |
C25H24F3N3O2
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|---|---|
| Molecular Weight |
455.4722
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| CAS # |
956136-95-1
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| Related CAS # |
956136-95-1 (free acid);956136-98-4 (sodium);
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| SMILES |
FC(F)(C1=NC=C(NC2=CN=C(C3=CC=C([C@H](CC4)CC[C@H]4CC(O)=O)C=C3)C=C2)C=C1)F
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| InChi Key |
GXALXAKNHIROPE-CALCHBBNSA-N
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| InChi Code |
InChI=1S/C25H24F3N3O2/c26-25(27,28)23-12-10-21(15-30-23)31-20-9-11-22(29-14-20)19-7-5-18(6-8-19)17-3-1-16(2-4-17)13-24(32)33/h5-12,14-17,31H,1-4,13H2,(H,32,33)/t16-,17+
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| Chemical Name |
2-((1s,4s)-4-(4-(5-((6-(trifluoromethyl)pyridin-3-yl)amino)pyridin-2-yl)phenyl)cyclohexyl)acetic acid
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| Synonyms |
LCQ908; LCQ-908; LCQ 908
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~137.22 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.49 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.49 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (5.49 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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