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Saroglitazar magnesium (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. Following oral glucose administration at a dose of 1 mg/kg (59%), the ED50s for these effects of AUC-glucose were found to be 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. Saxoliza shows promise as a novel therapeutic agent for the treatment of diabetes and dyslipidemia based on its efficacy and safety [1].
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| References |
| Molecular Formula |
C50H56MGN2O8S2
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|---|---|
| Molecular Weight |
901.423252105713
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| Exact Mass |
900.332
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| CAS # |
1639792-20-3
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| Related CAS # |
Saroglitazar;495399-09-2
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| PubChem CID |
121000421
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
63
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| Complexity |
526
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S(C)C1C=CC(=CC=1)C1=CC=C(C)N1CCOC1C=CC(=CC=1)C[C@@H](C(=O)[O-])OCC.S(C)C1C=CC(=CC=1)C1=CC=C(C)N1CCOC1C=CC(=CC=1)C[C@@H](C(=O)[O-])OCC.[Mg+2]
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| InChi Key |
UJYFZCVPOSZDMK-YPPDDXJESA-L
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| InChi Code |
InChI=1S/2C25H29NO4S.Mg/c2*1-4-29-24(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;/h2*5-14,24H,4,15-17H2,1-3H3,(H,27,28);/q;;+2/p-2/t2*24-;/m00./s1
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| Chemical Name |
magnesium (S)-2-ethoxy-3-(4-(2-(2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-1-yl)ethoxy)phenyl)propanoate
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~125 mg/mL (~138.67 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (3.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 27.5 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. Solubility in Formulation 2: 2.75 mg/mL (3.05 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (3.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1094 mL | 5.5468 mL | 11.0936 mL | |
| 5 mM | 0.2219 mL | 1.1094 mL | 2.2187 mL | |
| 10 mM | 0.1109 mL | 0.5547 mL | 1.1094 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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