Chiglitazar
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MedKoo CAT#: 326910

CAS#: 743438-45-1 (free base)

Description: Chiglitazar, also known as CS-038, is a potent and selective PPAR agonist potentially for the treatment of type 2 diabetes. Chiglitazar improves insulin resistance and dyslipidemia in MSG obese rats. Chiglitazar showed transactivating activity in each PPARα, γ, and δ subtype and upregulated the expression of PPARα and/or PPARδ downstream genes involved in the key processes of lipid metabolism and thermogenesis. Comparable blood glucose lowering effect was observed between chiglitazar and rosiglitazone, but chiglitazar did not significantly increase the body weight in KKAy and fat pad weight in db/db mice.

Chemical Structure

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Chiglitazar
CAS# 743438-45-1 (free base)
Instruction

Theoretical Analysis

MedKoo Cat#: 326910
Name: Chiglitazar
CAS#: 743438-45-1 (free base)
Chemical Formula: C36H29FN2O4
Exact Mass: 572.21
Molecular Weight: 572.636
Elemental Analysis: C, 75.51; H, 5.10; F, 3.32; N, 4.89; O, 11.18

Price and Availability

Size Price Availability Quantity
5mg USD 550 2 Weeks
10mg USD 950 2 Weeks
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Related CAS #: 2213406-75-6 (racemate free base)   1959588-75-0 (racemate sodium)   743438-45-1 (free base)    

Synonym: CS-038; CS 038; CS038; Chiglitazar;

IUPAC/Chemical Name: (S)-3-(4-(2-(9H-carbazol-9-yl)ethoxy)phenyl)-2-((2-(4-fluorobenzoyl)phenyl)amino)propanoic acid

InChi Key: QNLWMPLUWMWDMQ-YTTGMZPUSA-N

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

SMILES Code: O=C(O)[C@@H](NC1=CC=CC=C1C(C2=CC=C(F)C=C2)=O)CC3=CC=C(OCCN4C5=C(C6=C4C=CC=C6)C=CC=C5)C=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 572.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Deeks ED. Chiglitazar: First Approval. Drugs. 2022 Jan;82(1):87-92. doi: 10.1007/s40265-021-01648-1. PMID: 34846697.


2: DeFronzo RA. Chiglitazar: a novel pan-PPAR agonist. Sci Bull (Beijing). 2021 Aug 15;66(15):1497-1498. doi: 10.1016/j.scib.2021.04.012. Epub 2021 Apr 13. PMID: 36654276.


3: Jia W, Ma J, Miao H, Wang C, Wang X, Li Q, Lu W, Yang J, Zhang L, Yang J, Wang G, Zhang X, Zhang M, Sun L, Yu X, Du J, Shi B, Xiao C, Zhu D, Liu H, Zhong L, Xu C, Xu Q, Liang G, Zhang Y, Li G, Gu M, Liu J, Yuan G, Yan Z, Yan D, Ye S, Zhang F, Ning Z, Cao H, Pan D, Yao H, Lu X, Ji L. Chiglitazar monotherapy with sitagliptin as an active comparator in patients with type 2 diabetes: a randomized, double-blind, phase 3 trial (CMAS). Sci Bull (Beijing). 2021 Aug 15;66(15):1581-1590. doi: 10.1016/j.scib.2021.02.027. Epub 2021 Feb 16. PMID: 36654287.


4: Zhou Y, Wang H, Wang Y, Xu X, Li F, Zhou J, Shan T, Huang R, Cai T, Liu X, Su X, Li H, Ma J. Comparative Evaluation of Chiglitazar and Sitagliptin on the Levels of Retinol-Binding Protein 4 and Its Correlation With Insulin Resistance in Patients With Type 2 Diabetes. Front Endocrinol (Lausanne). 2022 Apr 25;13:801271. doi: 10.3389/fendo.2022.801271. PMID: 35547000; PMCID: PMC9081976.


5: Wang Y, Li H, Gao H, Xu X, Cai T, Wang H, Zhou Y, Huang R, Su X, Ma J. Effect of chiglitazar and sitagliptin on glucose variations, insulin resistance and inflammatory-related biomarkers in untreated patients with type 2 diabetes. Diabetes Res Clin Pract. 2022 Jan;183:109171. doi: 10.1016/j.diabres.2021.109171. Epub 2021 Dec 6. Erratum in: Diabetes Res Clin Pract. 2022 Aug;190:109885. PMID: 34883184.


6: Cheng HS, Tan WR, Low ZS, Marvalim C, Lee JYH, Tan NS. Exploration and Development of PPAR Modulators in Health and Disease: An Update of Clinical Evidence. Int J Mol Sci. 2019 Oct 11;20(20):5055. doi: 10.3390/ijms20205055. PMID: 31614690; PMCID: PMC6834327.


7: Zhou H, Jiang Y, Huang Y, Zhong M, Qin D, Xie C, Pan G, Tan J, Deng M, Zhao H, Zhou Y, Tang Y, Lai Q, Fang Z, Luo Y, Jiang Y, Xu B, Zha J. Therapeutic inhibition of PPARα-HIF1α-PGK1 signaling targets leukemia stem and progenitor cells in acute myeloid leukemia. Cancer Lett. 2023 Feb 1;554:215997. doi: 10.1016/j.canlet.2022.215997. Epub 2022 Nov 15. PMID: 36396101.


8: Ji L, Song W, Fang H, Li W, Geng J, Wang Y, Guo L, Cai H, Yang T, Li H, Yang G, Li Q, Liu K, Li S, Liu Y, Shi F, Li X, Gao X, Tian H, Ji Q, Su Q, Zhou Z, Wang W, Zhou Z, Li X, Xu Y, Ning Z, Cao H, Pan D, Yao H, Lu X, Jia W. Efficacy and safety of chiglitazar, a novel peroxisome proliferator-activated receptor pan-agonist, in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled, phase 3 trial (CMAP). Sci Bull (Beijing). 2021 Aug 15;66(15):1571-1580. doi: 10.1016/j.scib.2021.03.019. Epub 2021 Mar 23. PMID: 36654286.


9: Li X, Yu J, Wu M, Li Q, Liu J, Zhang H, Zhu X, Li C, Zhang J, Ning Z, Ding Y. Pharmacokinetics and Safety of Chiglitazar, a Peroxisome Proliferator-Activated Receptor Pan-Agonist, in Patients < 65 and ≥ 65 Years With Type 2 Diabetes. Clin Pharmacol Drug Dev. 2021 Jul;10(7):789-796. doi: 10.1002/cpdd.893. Epub 2020 Dec 20. PMID: 33345463.


10: Yuan F, Li J, Li X, Li H, Chen W, Yang M, Chen H, Sheng L, Liu C, Wu Y, Xu H. Pharmacokinetic Interaction of Chiglitazar with CYP3A4 Inducer or Inhibitor: An Open-Label, Sequential Crossover, Self-Control, 3-Period Study in Healthy Chinese Volunteers. Clin Pharmacol Drug Dev. 2023 Feb;12(2):168-174. doi: 10.1002/cpdd.1198. Epub 2022 Dec 30. PMID: 36583526.


11: Pan DS, Wang W, Liu NS, Yang QJ, Zhang K, Zhu JZ, Shan S, Li ZB, Ning ZQ, Huang L, Lu XP. Chiglitazar Preferentially Regulates Gene Expression via Configuration-Restricted Binding and Phosphorylation Inhibition of PPARγ. PPAR Res. 2017;2017:4313561. doi: 10.1155/2017/4313561. Epub 2017 Sep 19. PMID: 29056962; PMCID: PMC5625810.


12: Zhang XH, Tian YF, Huang GL, Cui WY, Sun Q, He WJ, Liu XJ. Advances in Studies of Chiglitazar Sodium, a Novel PPAR Pan-Agonist, for the Treatment of Type 2 Diabetes Mellitus. Curr Med Sci. 2023 Jun 16. doi: 10.1007/s11596-023-2760-3. Epub ahead of print. PMID: 37326885.


13: Wang Y, Li H, Gao H, Xu X, Cai T, Wang H, Zhou Y, Huang R, Su X, Ma J. Corrigendum to "Effect of chiglitazar and sitagliptin on glucose variations, insulin resistance and inflammatory-related biomarkers in untreated patients with type 2 diabetes" [Diabetes Res. Clin. Pract. 183 (2022) 109171]. Diabetes Res Clin Pract. 2022 Aug;190:109885. doi: 10.1016/j.diabres.2022.109885. Epub 2022 May 6. Erratum for: Diabetes Res Clin Pract. 2022 Jan;183:109171. PMID: 35527084.


14: He BK, Ning ZQ, Li ZB, Shan S, Pan DS, Ko BC, Li PP, Shen ZF, Dou GF, Zhang BL, Lu XP, Gao Y. In Vitro and In Vivo Characterizations of Chiglitazar, a Newly Identified PPAR Pan-Agonist. PPAR Res. 2012;2012:546548. doi: 10.1155/2012/546548. Epub 2012 Oct 22. PMID: 23150725; PMCID: PMC3486420.


15: Li PP, Shan S, Chen YT, Ning ZQ, Sun SJ, Liu Q, Lu XP, Xie MZ, Shen ZF. The PPARalpha/gamma dual agonist chiglitazar improves insulin resistance and dyslipidemia in MSG obese rats. Br J Pharmacol. 2006 Jul;148(5):610-8. doi: 10.1038/sj.bjp.0706745. Epub 2006 Jun 5. PMID: 16751799; PMCID: PMC1751868.


16: Xu HR, Zhang JW, Chen WL, Ning ZQ, Li XN. Pharmacokinetics, Safety and Tolerability of Chiglitazar, A Novel Peroxisome Proliferator-Activated Receptor (PPAR) Pan-Agonist, in Healthy Chinese Volunteers: A Phase I Study. Clin Drug Investig. 2019 Jun;39(6):553-563. doi: 10.1007/s40261-019-00779-4. PMID: 31037611.


17: Yi L, Zhang H, Zhang JW, You XM, Ning ZQ, Yu J, Qian LF, Miao LY. Study on Drug-Drug Interactions Between Chiglitazar, a Novel PPAR Pan-Agonist, and Metformin Hydrochloride in Healthy Subjects. Clin Pharmacol Drug Dev. 2019 Oct;8(7):934-941. doi: 10.1002/cpdd.668. Epub 2019 Feb 27. PMID: 30809967.


18: Chu NN, Li XN, Chen WL, Xu HR. Determination of chiglitazar, a dual alpha/gamma peroxisome proliferator-activated receptor (PPAR) agonist, in human plasma by liquid chromatography-tandem mass spectrometry. Pharmazie. 2007 Nov;62(11):825-9. PMID: 18065097.


19: Sullivan HJ, Wang X, Nogle S, Liao S, Wu C. To Probe Full and Partial Activation of Human Peroxisome Proliferator-Activated Receptors by Pan-Agonist Chiglitazar Using Molecular Dynamics Simulations. PPAR Res. 2020 Apr 1;2020:5314187. doi: 10.1155/2020/5314187. PMID: 32308671; PMCID: PMC7152983.


20: Zhang SJ, Zhang J, Guo JP, Niu YP. [Effects of Rosa roxburghii on insulin resistance in obese rats and its mechanisms]. Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2022 Nov;38(6):670-675. Chinese. doi: 10.12047/j.cjap.6328.2022.122. PMID: 37308415.