Saroglitazar |
Catalog No.GC30379 |
A PPARα and PPARγ dual agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 495399-09-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: |
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: [1]. Jain MR, et al. Saroglitazar, a novel PPARα/γ agonist with predominant PPARα activity, shows lipid-lowering and insulin-sensitizing effects in preclinical models. Pharmacol Res Perspect. 2015 Jun;3(3):e00136. |
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.
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].
[1]. Jain MR, et al. Saroglitazar, a novel PPARα/γ agonist with predominant PPARα activity, shows lipid-lowering and insulin-sensitizing effects in preclinical models. Pharmacol Res Perspect. 2015 Jun;3(3):e00136.
Cas No. | 495399-09-2 | SDF | |
Canonical SMILES | OC([C@@H](OCC)CC1=CC=C(OCCN2C(C)=CC=C2C3=CC=C(SC)C=C3)C=C1)=O | ||
Formula | C25H29NO4S | M.Wt | 439.57 |
Solubility | DMSO : ≥ 25 mg/mL (56.87 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.275 mL | 11.3748 mL | 22.7495 mL |
5 mM | 0.455 mL | 2.275 mL | 4.5499 mL |
10 mM | 0.2275 mL | 1.1375 mL | 2.275 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 2 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *