495399-09-2
495399-09-2 structure
- Name: saroglitazar
- Chemical Name: (2S)-2-ethoxy-3-[4-[2-[2-methyl-5-(4-methylsulfanylphenyl)pyrrol-1-yl]ethoxy]phenyl]propanoic acid
- CAS Number: 495399-09-2
- Molecular Formula: C25H29NO4S
- Molecular Weight: 439.56700
- Catalog: Research Areas Metabolic Disease
- Create Date: 2017-02-06 13:46:36
- Modify Date: 2025-08-27 12:04:19
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Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
| Name | (2S)-2-ethoxy-3-[4-[2-[2-methyl-5-(4-methylsulfanylphenyl)pyrrol-1-yl]ethoxy]phenyl]propanoic acid |
|---|---|
| Synonyms |
Saroglitazar
UNII-E0YMX3S4JD Lipaglyn |
| Description | Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively. |
|---|---|
| Related Catalog | |
| Target |
PPARα:0.65 pM (EC50, HepG2 cell) PPARγ:3 nM (EC50, HepG2 cell) |
| 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. 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. Based on efficacy and safety profile, Saroglitazar appears to have good potential as novel[1]. |
| Animal Admin | Rats: Rats randomize based on body weights and are divided into three equal groups and receives the daily administration of vehicle (50% w/v honey for marmoset and 0.1% carboxymethylcellulose for Wistar rats) or Saroglitazar (1.5 and 15 mg/kg per day) for 90 days by oral gavage[1]. Mice: Male C57BL/6J-db/db mice are bled on day 0 to determine pretreatment serum glucose and TG. During next 12 days, each animal is dosed (by oral gavage) with vehicle (0.5% sodium carboxymethyl cellulose) or Saroglitazar (0.01, 0.03, 0.1, 0.3,1, and 3 mg/kg per day) or pioglitazone (60 mg/kg per day) and on day 12 of the treatment, blood samples are collected (1 h after dosing) from orbital sinus under light ether anesthesia. The serum is isolated and analyzed for glucose, TG, free fatty acid (FFA), and insulin levels[1]. |
| References |
| Molecular Formula | C25H29NO4S |
|---|---|
| Molecular Weight | 439.56700 |
| Exact Mass | 439.18200 |
| PSA | 85.99000 |
| LogP | 5.29660 |
| Storage condition | 2-8℃ |