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Purity: ≥98%
Saroglitazar (ZYH1; Lipaglyn) is an approved drug for the treatment of type 2 diabetes mellitus and dyslipidemia, acting as a novel dual PPAR α/γ agonist. It is approved for use in India by the Drug Controller General of India. Saroglitazar has demonstrated reduction of triglycerides (TG), LDL cholesterol, VLDL cholesterol, non-HDL cholesterol and an increase in HDL cholesterol a characteristic hallmark of atherogenic diabetic dyslipidemia (ADD). Saroglitazar is novel first in class drug which acts as a dual PPAR agonist at the subtypes α (alpha) and γ (gamma) of the peroxisome proliferator-activated receptor (PPAR). Agonist action at PPARα lowers high blood triglycerides, and agonist action on PPARγ improves insulin resistance and consequently lowers blood sugar.
| 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].
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| References | |
| Additional Infomation |
Saroglitazar is a monocarboxylic acid that is (2S)-2-ethoxy-3-(p-ethoxyphenyl)propanoic acid in which one of the methyl hydrogens of the p-ethoxy substituent has been replaced by the nitrogen of 2-methyl-5-[4-(methylthio)phenyl]-1H-pyrrole. An agonist at the subtypes alpha and gamma of the peroxisome proliferator-activated receptor (PPAR) with predominant PPARalpha activity, it is used in the treatment of type 2 diabetes. It has a role as a PPARgamma agonist, a hypoglycemic agent and a PPARalpha agonist. It is a member of pyrroles, a monocarboxylic acid, a methyl sulfide and an aromatic ether.
Saroglitazar has been investigated for the treatment of Fatty Liver. |
| 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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