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Chiglitazar (CS-038; CS038; Bilessglu) is a dual agonist of PPARα/γ (peroxisome proliferator-activated receptor) approved in China in 2021 for the treatment of type 2 diabetes. It activates PPARα/γ/δ with EC50s of 1.2, 0.08, and 1.7 μM, respectively. Chiglitazar is configuration-restricted non-thiazolidinedione PPAR agonist developed by Chengdu Chipscreen in China.
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| ln Vitro |
Chiglitazar being studied in comparison to rosiglitazone and pioglitazone for PPARγ and WY14643 for PPARα in terms of dosage response. Chiglitazar has a notable increase in both isoform activation. Chiglitazar exhibits PPARγ activating activity that is stronger than pioglitazone but weaker than rosiglitazone. Chiglitazar is more effective than pioglitazone, rosiglitazone, or WY14643, a selective PPARα agonist, in terms of PPARα activation[1].
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| ln Vivo |
Plasma glucose levels in the MSG rats treated with rosiglitazone or Chiglitazar after insulin administration are consistently lower than in the vehicle-treated control group. Animals treated with rosiglitazone and chiglitazar had lower fasting PI levels than the control group. Chiglitazar and rosiglitazone-treated MSG obese rats had considerably higher ISIs than the control group. Chiglitazar additionally improves the HOMA indices. The glucose readings in the 5 and 10 mg/kg Chiglitazar and Rosiglitazone treatment groups are considerably lower than those in the vehicle treatment group for IPGTT at 30 minutes after glucose loading. The treatment groups' integrated glucose response during the IPGTT is substantially lower than that of the control groups[1].
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| References |
| Molecular Formula |
C36H29FN2O4
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|---|---|
| Molecular Weight |
572.6364
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| Exact Mass |
572.211
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| CAS # |
743438-45-1
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| Related CAS # |
2213406-75-6 (racemate free base);1959588-75-0 (racemate sodium);743438-45-1;
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| PubChem CID |
71402018
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| Appearance |
Light yellow to khaki solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
779.8±60.0 °C at 760 mmHg
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| Flash Point |
425.4±32.9 °C
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| Vapour Pressure |
0.0±2.8 mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
8.72
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
43
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| Complexity |
895
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC=C2C(=C1)C3=CC=CC=C3N2CCOC4=CC=C(C=C4)C[C@@H](C(=O)O)NC5=CC=CC=C5C(=O)C6=CC=C(C=C6)F
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| InChi Key |
QNLWMPLUWMWDMQ-YTTGMZPUSA-N
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| InChi Code |
InChI=1S/C36H29FN2O4/c37-26-17-15-25(16-18-26)35(40)30-9-1-4-10-31(30)38-32(36(41)42)23-24-13-19-27(20-14-24)43-22-21-39-33-11-5-2-7-28(33)29-8-3-6-12-34(29)39/h1-20,32,38H,21-23H2,(H,41,42)/t32-/m0/s1
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| Chemical Name |
(S)-3-(4-(2-(9H-carbazol-9-yl)ethoxy)phenyl)-2-((2-(4-fluorobenzoyl)phenyl)amino)propanoic acid
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| Synonyms |
CS038 CS 038 CS-038
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~174.64 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.37 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 | 1.7463 mL | 8.7315 mL | 17.4630 mL | |
| 5 mM | 0.3493 mL | 1.7463 mL | 3.4926 mL | |
| 10 mM | 0.1746 mL | 0.8731 mL | 1.7463 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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