| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Saroglitazar targets peroxisome proliferator-activated receptors (PPARs), specifically PPARα and PPARγ. It is a potent PPARα agonist (EC50 = 0.65 pM) with moderate PPARγ activity (EC50 = 3 nM). By activating PPARα, it lowers triglyceride levels. Activation of PPARγ improves insulin resistance and contributes to lower blood sugar levels. Its dual agonism provides both lipid-lowering and insulin-sensitizing effects.
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| ln Vitro |
Saroglitazar has EC50 values of 0.65 pM for PPARα and 3 nM for PPARγ in HepG2 cells. It shows lipid-lowering and insulin-sensitizing effects in preclinical models. Its predominant PPARα activity reduces triglycerides, while its moderate PPARγ activity improves insulin sensitivity. It is a potent and selective PPAR agonist.
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| ln Vivo |
Treatment with Saroglitazar (0.01-3 mg/kg daily, po) for 12 days caused a dose-dependent reduction in blood glucose, free fatty acids (FFA), and triglycerides (TG) in db/db mice. After oral glucose delivery at a dose of 1 mg/kg (59%), serum insulin and AUC glucose were considerably lowered (91%) (ED50s for these effects were 0.05, 0.19, and 0.19 mg/kg, respectively). Saroglitazar's efficacy (TG-lowering capability) was validated in a 90-day repeated dosage comparison research conducted in Wistar rats and marmosets. The study also showed a low risk of PPAR-related side effects in people. Saroglitazar seems to have good potential as a novel medicine based on efficacy and safety [1].
Saroglitazar has demonstrated lipid-lowering and insulin-sensitizing effects in preclinical models. It has been developed for the treatment of dyslipidemia and has favorable effects on glycemic parameters in type 2 diabetes mellitus. It has been investigated in clinical trials for primary biliary cholangitis, non-alcoholic steatohepatitis, and nonalcoholic fatty liver disease. It is marketed as Lipaglyn in India. |
| Enzyme Assay |
In vitro enzyme or receptor binding assays for Saroglitazar measure its affinity and agonist activity at PPARα and PPARγ. The receptors are incubated with a radiolabeled ligand and varying concentrations of the compound, and displacement is measured. Functional assays assess PPAR activation using reporter gene assays, where cells expressing PPARs and a luciferase reporter are treated with the compound, and luciferase activity is measured.
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| Cell Assay |
In vitro cellular assays for Saroglitazar involve treating cells (e.g., HepG2) with the compound and measuring PPAR target gene expression by qPCR. Its effects on lipid metabolism and insulin signaling can be assessed in adipocytes or hepatocytes. Glucose uptake and triglyceride levels are measured to evaluate its metabolic effects. Cytotoxicity and cell viability assays are also performed.
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| Animal Protocol |
In vivo animal models for Saroglitazar include rodent models of dyslipidemia, type 2 diabetes, and non-alcoholic fatty liver disease to evaluate its lipid-lowering, insulin-sensitizing, and hepatoprotective effects. In these models, animals are treated with the compound, and parameters such as blood glucose, triglycerides, insulin sensitivity, and liver histology are measured.
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| ADME/Pharmacokinetics |
Saroglitazar is orally active. It is well-absorbed after oral administration and has good bioavailability. It is metabolized in the liver, and its metabolites are excreted in urine and feces. Its half-life is consistent with once-daily dosing. Its pharmacokinetics have been characterized in preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
The toxicological profile of Saroglitazar is characteristic of PPAR agonists. Common side effects may include weight gain, edema, and gastrointestinal disturbances. Long-term use may be associated with cardiovascular and hepatic effects. Its safety has been evaluated in clinical trials for the treatment of dyslipidemia and other conditions.
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| References | |
| Additional Infomation |
Saxagliptin is a monocarboxylic acid, chemically named (2S)-2-ethoxy-3-(p-ethoxyphenyl)propionic acid, in which a methyl hydrogen atom on the p-ethoxy substituent is replaced by a nitrogen atom of 2-methyl-5-[4-(methylthio)phenyl]-1H-pyrrole. It is an agonist of peroxisome proliferator-activated receptor (PPAR) α and γ subtypes, primarily exhibiting PPARα activity, and is used to treat type 2 diabetes. It has dual effects as a PPARγ agonist, hypoglycemic agent, and PPARα agonist. It belongs to the pyrrole class of compounds, monocarboxylic acids, methyl sulfides, and aromatic ethers. Saxagliptin has been investigated for the treatment of fatty liver.
Saroglitazar is a novel PPAR agonist with predominant PPARα and moderate PPARγ activity. It has EC50 values of 0.65 pM for PPARα and 3 nM for PPARγ. It is used for dyslipidemia and has favorable effects on glycemic parameters in type 2 diabetes. It has been investigated for primary biliary cholangitis, non-alcoholic steatohepatitis, and nonalcoholic fatty liver disease. |
| Molecular Formula |
C25H29NO4S
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|---|---|
| Molecular Weight |
439.56706
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| Exact Mass |
439.182
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| Elemental Analysis |
C, 68.31; H, 6.65; N, 3.19; O, 14.56; S, 7.29
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| CAS # |
495399-09-2
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| Related CAS # |
Saroglitazar magnesium;1639792-20-3;Saroglitazar-d4
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| PubChem CID |
60151560
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| Appearance |
Light yellow to orange solid powder
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| LogP |
5.296
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
31
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| Complexity |
532
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| Defined Atom Stereocenter Count |
1
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| SMILES |
OC([C@@H](OCC)CC1=CC=C(OCCN2C(C)=CC=C2C3=CC=C(SC)C=C3)C=C1)=O
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| InChi Key |
MRWFZSLZNUJVQW-DEOSSOPVSA-N
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| InChi Code |
InChI=1S/C25H29NO4S/c1-4-29-24(25(27)28)17-19-6-10-21(11-7-19)30-16-15-26-18(2)5-14-23(26)20-8-12-22(31-3)13-9-20/h5-14,24H,4,15-17H2,1-3H3,(H,27,28)/t24-/m0/s1
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| Chemical Name |
(S)-2-ethoxy-3-(4-(2-(2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-1-yl)ethoxy)phenyl)propanoic acid
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| Synonyms |
ZYH1; ZYH-1; ZYH 1; trade name: Lipaglyn.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 25 mg/mL (~56.87 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2750 mL | 11.3748 mL | 22.7495 mL | |
| 5 mM | 0.4550 mL | 2.2750 mL | 4.5499 mL | |
| 10 mM | 0.2275 mL | 1.1375 mL | 2.2750 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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