Saroglitazar

For research use only.

Catalog No.S9674 Synonyms: Lipaglyn, ZYH1

Saroglitazar Chemical Structure

CAS No. 495399-09-2

Saroglitazar (Lipaglyn, ZYH1) is an agonist of peroxisome proliferator-activated receptor (PPAR) with EC50 of 0.65 pM and 3 nM for hPPARα and hPPARγ in HepG2 cells, respectively.

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Biological Activity

Description Saroglitazar (Lipaglyn, ZYH1) is an agonist of peroxisome proliferator-activated receptor (PPAR) with EC50 of 0.65 pM and 3 nM for hPPARα and hPPARγ in HepG2 cells, respectively.
Targets
hPPARα [1]
(Cell-free assay)
hPPARγ [1]
(Cell-free assay)
0.65 pM(EC50) 3 nM(EC50)
In vitro

Saroglitazar is a novel nonthiazolidinediones (TZD) and nonfibric acid derivative designed to act as dual regulator of lipids and glucose metabolism by activating peroxisome proliferator-activated receptors (PPAR). The EC50 values of Saroglitazar assessed in HepG2 cells using PPAR transactivation assay for hPPARa and hPPARc are 0.65 pmol/L and 3 nmol/L, respectively.[1]

In vivo

In db/db mice, 12-day treatment with Saroglitazar (0.01–3 mg/kg per day, orally) causes dose-dependent reductions in serum triglycerides (TG), free fatty acids (FFA), and glucose. The ED50 for these effects is found to be 0.05, 0.19, and 0.19 mg/kg, respectively with highly significant (91%) reduction in serum insulin and AUC-glucose following oral glucose administration (59%) at 1 mg/kg dose. Significant reduction in serum TG (upto 90%) is also observed in Zucker fa/fa rats, Swiss albino mice, and in high fat -high cholesterol (HF-HC)-fed Golden Syrian hamsters. LDL cholesterol is significantly lowered in hApoB100/hCETP double transgenic mice and HF-HC diet fed Golden Syrian Hamsters. Hyperinsulinemic-Euglycemic clamp study in Zucker fa/fa rats demonstrates potent insulin-sensitizing activity. Saroglitazar also shows a significant decrease in SBP (22 mmHg) and increase (62.1%) in serum adiponectin levels in Zucker fa/fa rats. A 90-day repeated dose comparative study in Wistar rats and marmosets confirms efficacy (TG lowering) potential of Saroglitazar and has indicated low risk of PPAR-associated side effects in humans.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: HepG2 cells
  • Concentrations: --
  • Incubation Time: 20-22 h
  • Method:

    HepG2 cells are seeded in 12-well plates at a density of 400,000 cells/well in 1 mL of medium per well. Cells are transfected with PPRE3-TK-luc and 0.08 μg of the pCDNA expression vector containing the cDNA of PPARa or 0.08 μg of the pSG5 expression vector containing the cDNA of PPARc using Superfect. Cells are incubated at 37 ℃, 5% CO2: 95% O2 and after 3 h 1.0 mL of the medium containing Saroglitazar are added to the respective wells. After the incubation for 20–22 h at 37 ℃ under 5% CO2, cells are first washed with Phosphate Buffer Saline (pH 7.3- 7.4), lysed and supernatant collected for luciferase and bgalactosidase activity. The luciferase activity is determined using commercial firefly luciferase assay according to the suppliers’ instructions in white 96-well plate. The bgalactosidase activity is determined in ELISA reader at 415 nm.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: B6.BKS(D)-Leprdb/J(db/db) mice
  • Dosages: 0.01 mg/kg, 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

Chemical Information

Molecular Weight 439.57
Formula

C25H29NO4S

Density 1.15 g/mL
CAS No. 495399-09-2
Storage 2 years 4°C liquid
Synonyms Lipaglyn, ZYH1
Smiles CCOC(CC1=CC=C(C=C1)OCCN2C(=CC=C2C3=CC=C(C=C3)SC)C)C(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04112446 Completed Drug: Saroglitazar magnesium Healthy Zydus Therapeutics Inc. September 20 2019 Phase 1

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PPAR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID