SR-18292 | CAS#2095432-55-4 | PGC-1α inhibitor

MedKoo Cat#: 530568 | Name: SR-18292

Description:

WARNING: This product is for research use only, not for human or veterinary use.

SR-18292 is a proliferator-activated receptor-γ coactivator-1α (PGC-1α) inhibitor. SR-18292 reduces blood glucose, strongly increases hepatic insulin sensitivity, and improves glucose homeostasis in dietary and genetic mouse models of T2D.

Chemical Structure

SR-18292

CAS#2095432-55-4

Theoretical Analysis

MedKoo Cat#: 530568

Name: SR-18292

CAS#: 2095432-55-4

Chemical Formula: C23H30N2O2

Exact Mass: 366.2307

Molecular Weight: 366.51

Elemental Analysis: C, 75.37; H, 8.25; N, 7.64; O, 8.73

Price and Availability

Size	Price	Availability
25mg	USD 250.00	2 Weeks
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,850.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 6,450.00	2 Weeks

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Synonym

SR-18292; SR 18292; SR18292.

IUPAC/Chemical Name

1-((1H-indol-4-yl)oxy)-3-(tert-butyl(4-methylbenzyl)amino)propan-2-ol

InChi Key

BNRANURXPKRRKP-UHFFFAOYSA-N

InChi Code

InChI=1S/C23H30N2O2/c1-17-8-10-18(11-9-17)14-25(23(2,3)4)15-19(26)16-27-22-7-5-6-21-20(22)12-13-24-21/h5-13,19,24,26H,14-16H2,1-4H3

SMILES Code

CC(C=C1)=CC=C1CN(C(C)(C)C)CC(O)COC2=CC=CC3=C2C=CN3

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, DMF, and ethanol

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

Type 2 diabetes (T2D) is a worldwide epidemic with a medical need for additional targeted therapies. Suppression of hepatic glucose production (HGP) effectively ameliorates diabetes and can be exploited for its treatment. Targeting PGC-1α acetylation in the liver, a chemical modification known to inhibit hepatic gluconeogenesis, could be potentially used for treatment of T2D.

Product Data

Product Data

Instruction

View handling instruction

Biological target:

SR-18292 is a PGC-1α inhibitor, a coactivator of transcription factors for genes involved in gluconeogenesis.

In vitro activity:

Pretreatment of C2c12 myoblast cultures with SR-18292 abolished the protection of HSPA12A from Bupivacaine-induced death and mitochondrial loss in C2c12 cells. Reference: Toxicol Appl Pharmacol. 2022 Jan 1;434:115798. https://pubmed.ncbi.nlm.nih.gov/34793778/

In vivo activity:

PPARGC1A inhibition through small interfering RNA and SR-18292 treatment counteracted CLU-dependent cytoprotection, leading to mitophagy-associated cell death. Co-treatment of SR-18292 with cisplatin synergistically suppresses tumor growth in oral cancer xenograft models. Reference: Autophagy. 2024 Mar 6:1-25. https://pubmed.ncbi.nlm.nih.gov/38447939/

	Solvent	mg/mL	mM
Solubility
	DMF	25.0	68.21
	DMSO	25.0	68.21
	Ethanol	10.0	27.28

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 366.51 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.

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:

1. Wang L, Xie Y, Xiao B, He X, Ying G, Zha H, Yang C, Jin X, Li G, Ping L, Wang J, Weng Q. Isorhamnetin alleviates cisplatin-induced acute kidney injury via enhancing fatty acid oxidation. Free Radic Biol Med. 2024 Feb 20;212:22-33. doi: 10.1016/j.freeradbiomed.2023.12.010. Epub 2023 Dec 13. PMID: 38101584. 2. Mao Q, Yu W, Liu S, Cao X, Dai Y, Zhang X, Min X, Liu L, Ding Z. Downregulation of HSPA12A underlies myotoxicity of local anesthetic agent bupivacaine through inhibiting PGC1α-mediated mitochondrial integrity. Toxicol Appl Pharmacol. 2022 Jan 1;434:115798. doi: 10.1016/j.taap.2021.115798. Epub 2021 Nov 15. PMID: 34793778. 3. Praharaj PP, Patra S, Singh A, Panigrahi DP, Lee HY, Kabir MF, Hossain MK, Patra SK, Patro BS, Patil S, Klionsky DJ, Chae HJ, Bhutia SK. CLU (clusterin) and PPARGC1A/PGC1α coordinately control mitophagy and mitochondrial biogenesis for oral cancer cell survival. Autophagy. 2024 Mar 6:1-25. doi: 10.1080/15548627.2024.2309904. Epub ahead of print. PMID: 38447939. 4. Yang C, Sui G, Li D, Wang L, Zhang S, Lei P, Chen Z, Wang F. Exogenous IGF-1 alleviates depression-like behavior and hippocampal mitochondrial dysfunction in high-fat diet mice. Physiol Behav. 2021 Feb 1;229:113236. doi: 10.1016/j.physbeh.2020.113236. Epub 2020 Oct 31. PMID: 33137345.

In vitro protocol:

In vivo protocol:

1. Praharaj PP, Patra S, Singh A, Panigrahi DP, Lee HY, Kabir MF, Hossain MK, Patra SK, Patro BS, Patil S, Klionsky DJ, Chae HJ, Bhutia SK. CLU (clusterin) and PPARGC1A/PGC1α coordinately control mitophagy and mitochondrial biogenesis for oral cancer cell survival. Autophagy. 2024 Mar 6:1-25. doi: 10.1080/15548627.2024.2309904. Epub ahead of print. PMID: 38447939. 2. Yang C, Sui G, Li D, Wang L, Zhang S, Lei P, Chen Z, Wang F. Exogenous IGF-1 alleviates depression-like behavior and hippocampal mitochondrial dysfunction in high-fat diet mice. Physiol Behav. 2021 Feb 1;229:113236. doi: 10.1016/j.physbeh.2020.113236. Epub 2020 Oct 31. PMID: 33137345.

1: Sharabi K, Lin H, Tavares CDJ, Dominy JE, Camporez JP, Perry RJ, Schilling R, Rines AK, Lee J, Hickey M, Bennion M, Palmer M, Nag PP, Bittker JA, Perez J, Jedrychowski MP, Ozcan U, Gygi SP, Kamenecka TM, Shulman GI, Schreiber SL, Griffin PR, Puigserver P. Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes. Cell. 2017 Mar 23;169(1):148-160.e15. doi: 10.1016/j.cell.2017.03.001. PMID: 28340340; PMCID: PMC5398763. 2: Weihrauch M, Handschin C. Pharmacological targeting of exercise adaptations in skeletal muscle: Benefits and pitfalls. Biochem Pharmacol. 2018 Jan;147:211-220. doi: 10.1016/j.bcp.2017.10.006. Epub 2017 Oct 20. PMID: 29061342; PMCID: PMC5850978. 3: Xie K, Wang Y, Yin L, Wang Y, Chen H, Mao X, Wang G. Hydrogen Gas Alleviates Sepsis-Induced Brain Injury by Improving Mitochondrial Biogenesis Through the Activation of PGC-α in Mice. Shock. 2021 Jan 1;55(1):100-109. doi: 10.1097/SHK.0000000000001594. PMID: 32590694. 4: Han H, Dong Y, Ma X. Dihydromyricetin Protects Against Gentamicin-Induced Ototoxicity via PGC-1α/SIRT3 Signaling in vitro. Front Cell Dev Biol. 2020 Jul 28;8:702. doi: 10.3389/fcell.2020.00702. PMID: 32850822; PMCID: PMC7399350. 5: Yang C, Sui G, Li D, Wang L, Zhang S, Lei P, Chen Z, Wang F. Exogenous IGF-1 alleviates depression-like behavior and hippocampal mitochondrial dysfunction in high-fat diet mice. Physiol Behav. 2021 Feb 1;229:113236. doi: 10.1016/j.physbeh.2020.113236. Epub 2020 Oct 31. PMID: 33137345. 6: Zhou HY, Long CX, Luo L, Chen YY, Liu PP, Xiao ZH. [Effect of mogroside VI on acute liver injury induced by sepsis in mice and related mechanisms]. Zhongguo Dang Dai Er Ke Za Zhi. 2020 Nov;22(11):1233-1239. Chinese. doi: 10.7499/j.issn.1008-8830.2007088. PMID: 33172561; PMCID: PMC7666382. 7: Raggi C, Taddei ML, Sacco E, Navari N, Correnti M, Piombanti B, Pastore M, Campani C, Pranzini E, Iorio J, Lori G, Lottini T, Peano C, Cibella J, Lewinska M, Andersen JB, di Tommaso L, Viganò L, Di Maira G, Madiai S, Ramazzotti M, Orlandi I, Arcangeli A, Chiarugi P, Marra F. Mitochondrial oxidative metabolism contributes to a cancer stem cell phenotype in cholangiocarcinoma. J Hepatol. 2021 Jun;74(6):1373-1385. doi: 10.1016/j.jhep.2020.12.031. Epub 2021 Jan 21. PMID: 33484774. 8: Yang C, Yang W, He Z, Guo J, Yang X, Wang R, Li H. Kaempferol Alleviates Oxidative Stress and Apoptosis Through Mitochondria-dependent Pathway During Lung Ischemia-Reperfusion Injury. Front Pharmacol. 2021 Mar 4;12:624402. doi: 10.3389/fphar.2021.624402. PMID: 33746757; PMCID: PMC7969663. 9: Chen N, Ge MM, Li DY, Wang XM, Liu DQ, Ye DW, Tian YK, Zhou YQ, Chen JP. β2-adrenoreceptor agonist ameliorates mechanical allodynia in paclitaxel-induced neuropathic pain via induction of mitochondrial biogenesis. Biomed Pharmacother. 2021 Dec;144:112331. doi: 10.1016/j.biopha.2021.112331. Epub 2021 Oct 19. PMID: 34673421. 10: Mao Q, Yu W, Liu S, Cao X, Dai Y, Zhang X, Min X, Liu L, Ding Z. Downregulation of HSPA12A underlies myotoxicity of local anesthetic agent bupivacaine through inhibiting PGC1α-mediated mitochondrial integrity. Toxicol Appl Pharmacol. 2022 Jan 1;434:115798. doi: 10.1016/j.taap.2021.115798. Epub 2021 Nov 15. PMID: 34793778. 11: Shi PZ, Wang JW, Wang PC, Han B, Lu XH, Ren YX, Feng XM, Cheng XF, Zhang L. Urolithin a alleviates oxidative stress-induced senescence in nucleus pulposus- derived mesenchymal stem cells through SIRT1/PGC-1α pathway. World J Stem Cells. 2021 Dec 26;13(12):1928-1946. doi: 10.4252/wjsc.v13.i12.1928. PMID: 35069991; PMCID: PMC8727228. 12: Xiao J, Li W, Li G, Tan J, Dong N. STK11 overexpression prevents glucocorticoid-induced osteoporosis via activating the AMPK/SIRT1/PGC1α axis. Hum Cell. 2022 Jul;35(4):1045-1059. doi: 10.1007/s13577-022-00704-6. Epub 2022 May 11. PMID: 35543972. 13: Zhang C, Fu Q, Shao K, Liu L, Ma X, Zhang F, Zhang X, Meng L, Yan C, Zhao X. Indole-3-acetic acid improves the hepatic mitochondrial respiration defects by PGC1a up-regulation. Cell Signal. 2022 Nov;99:110442. doi: 10.1016/j.cellsig.2022.110442. Epub 2022 Aug 18. PMID: 35988807. 14: Li K, Gao L, Zhou S, Ma YR, Xiao X, Jiang Q, Kang ZH, Liu ML, Liu TX. Erythropoietin promotes energy metabolism to improve LPS-induced injury in HK-2 cells via SIRT1/PGC1-α pathway. Mol Cell Biochem. 2023 Mar;478(3):651-663. doi: 10.1007/s11010-022-04540-y. Epub 2022 Aug 24. PMID: 36001204. 15: Tseng C, Han Y, Lv Z, Song Q, Wang K, Shen H, Chen Z. Glucose-stimulated PGC-1α couples with CBP and Runx2 to mediate intervertebral disc degeneration through transactivation of ADAMTS4/5 in diet-induced obesity mice. Bone. 2023 Feb;167:116617. doi: 10.1016/j.bone.2022.116617. Epub 2022 Nov 18. PMID: 36403758. 16: Liu L, Wang B, Yang W, Jiang Q, Loor JJ, Ouyang L, Tang H, Chang R, Peng T, Xu C. Sirtuin 3 relieves inflammatory responses elicited by lipopolysaccharide via the PGC1α-NFκB pathway in bovine mammary epithelial cells. J Dairy Sci. 2023 Feb;106(2):1315-1329. doi: 10.3168/jds.2022-22114. Epub 2022 Dec 7. PMID: 36494223. 17: Zhou J, Shen R, Makale EC, Zhong W, Chen Z, Huang Q. SS31 Confers Cerebral Protection by Reversing Mitochondrial Dysfunction in Early Brain Injury Following Subarachnoid Hemorrhage, via the Nrf2- and PGC-1α-Dependent Pathways. Neurochem Res. 2023 May;48(5):1580-1595. doi: 10.1007/s11064-022-03850-3. Epub 2022 Dec 27. PMID: 36574150. 18: Li Y, Zhu Y, Li S, Dong Y, Wan C, Yu X, Xin G, Wei Z, Li F, Wang Y, Zhang K, Chen Q, Zhang C, Wen E, Niu H, Huang W. Deoxyarbutin attenuates severe acute pancreatitis via the HtrA2/PGC-1α pathway. Free Radic Res. 2022 Sep- Oct;56(9-10):651-665. doi: 10.1080/10715762.2022.2163244. Epub 2023 Jan 2. PMID: 36592372. 19: Pang X, Cheng J, Wu T, Sun L. SIRT3 ameliorates polycystic ovary syndrome through FOXO1/PGC-1α signaling pathway. Endocrine. 2023 Apr;80(1):201-211. doi: 10.1007/s12020-022-03262-x. Epub 2023 Jan 4. PMID: 36598711. 20: Zhang J, Li J, Liu Y, Liang R, Mao Y, Yang X, Zhang Y, Zhu L. Effect of resveratrol on skeletal slow-twitch muscle fiber expression via AMPK/PGC-1α signaling pathway in bovine myotubes. Meat Sci. 2023 Oct;204:109287. doi: 10.1016/j.meatsci.2023.109287. Epub 2023 Jul 20. PMID: 37490793.