Name: Saroglitazar
Brand: Selleck Chemicals
SKU: S9674
Availability: InStock
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Quality Control

Batch: S967401 Purity: 98.62%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

98.62

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other PPAR Inhibitors	T0070907 GW9662 GW6471 WY-14643 (Pirinixic Acid) GSK3787 GW0742 AZ6102 GSK0660 Harmine Astaxanthin

Solubility

In vitro
Batch:

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.650mg/ml (3.75mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.710mg/ml (1.62mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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Average weight of animals: g

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	439.57	Formula	C₂₅H₂₉NO₄S	Storage (From the date of receipt)	2 years 4°C liquid
CAS No.	495399-09-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Lipaglyn, ZYH1			Smiles	CCOC(CC1=CC=C(C=C1)OCCN2C(=CC=C2C3=CC=C(C=C3)SC)C)C(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	hPPARα (Cell-free assay) 0.65 pM(EC50) hPPARγ (Cell-free assay) 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 this compound assessed in HepG2 cells using PPAR transactivation assay for hPPARa and hPPARc are 0.65 pmol/L and 3 nmol/L, respectively.
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. This compound 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 this chemical and has indicated low risk of PPAR-associated side effects in humans.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26171220/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05211284	Recruiting	Nonalcoholic Steatohepatitis	Zydus Therapeutics Inc.	September 26 2022	Phase 2
NCT04112446	Completed	Healthy	Zydus Therapeutics Inc.	September 20 2019	Phase 1

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Saroglitazar PPAR agonist

Chemical Structure

Molecular Weight: 439.57