1. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  2. Acyltransferase BCRP OAT
  3. Pradigastat sodium

Pradigastat sodium (LCQ 908 sodium) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro.

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Pradigastat sodium Chemical Structure

Pradigastat sodium Chemical Structure

CAS No. : 956136-98-4

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Description

Pradigastat sodium (LCQ 908 sodium) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro[1][2][3][4].

IC50 & Target

Diacylglycerol acyltransferase 1 (DGAT1)[1]
IC50: 5 µM (BCRP); IC50: 1.66 µM (OATP1B1); IC50: 3.34 µM (OATP1B3); IC50: 0.973 µM (OAT3)[2]

In Vitro

Pradigastat (0-50 μM; 1 h) inhibits BCRP-mediated efflux activity in a dose-dependent manner in overexpressing human ovarian cancer cell lines with an IC50 of 5 µM[2].
Pradigastat (0-50 μM; 5 minutes) inhibits OATP1B1, OATP1B3, and OAT3 activities in a concentration-dependent manner with IC50 of 1.66µM, 3.34µM and 0.973µM, respectively[2].
Pradigastat (2-20 μM; 8 h) inhibits the replication and production of hepatitis C virus in vitro[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

477.45

Formula

C25H23F3N3NaO2

CAS No.
SMILES

O=C(O[Na])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

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Pradigastat sodium
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HY-16278A
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