1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. Pradigastat

Pradigastat (Synonyms: LCQ-908)

Cat. No.: HY-16278 Purity: 98.39%
Handling Instructions

Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.

For research use only. We do not sell to patients.

Pradigastat Chemical Structure

Pradigastat Chemical Structure

CAS No. : 956136-95-1

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 377 In-stock
Estimated Time of Arrival: December 31
5 mg USD 343 In-stock
Estimated Time of Arrival: December 31
10 mg USD 443 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1195 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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 IC50 value of 5 μM. Pradigastat inhibits OATP1B1, OATP1B3, and OAT3 activity in a concentration-dependent manner with estimated IC50 values of 1.66 μM, 3.34 μM, and 0.973 μM, respectively[2].

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].

Clinical Trial
Molecular Weight

455.47

Formula

C₂₅H₂₄F₃N₃O₂

CAS No.

956136-95-1

SMILES

O=C(O)C[[email protected]]1CC[[email protected]](C2=CC=C(C3=NC=C(NC4=CC=C(C(F)(F)F)N=C4)C=C3)C=C2)CC1

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
In Vitro: 

DMSO : 16.67 mg/mL (36.60 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (insoluble)

H2O : < 0.1 mg/mL (insoluble)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.39%

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Keywords:

PradigastatLCQ-908LCQ908LCQ 908AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseDGAT1anti-obesityanti-diabeticBCRPOATPOAT3chylomicronstriglycerideInhibitorinhibitorinhibit

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Product Name:
Pradigastat
Cat. No.:
HY-16278
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