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Rosiglitazone (maleate)

$66$198

Products Details

Product Description

– Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).

Web ID

– HY-14600

Storage Temperature

– 4°C (Powder, sealed storage, away from moisture)

Shipping

– Room Temperature

Applications

– COVID-19-anti-virus

Molecular Formula

– C22H23N3O7S

Citations

– Front Mol Biosci. 2022 Feb 4;8:766887.|Pharmaceuticals. 2022, 15(9), 1055.|Acta Pharmacol Sin. 2023 May 24.|Adipocyte. 2021 Dec;10(1):646-657.|Adv Sci (Weinh). 2023 Jul 10;e2301088.|Am J Cancer Res. 2020 Apr 1;10(4):1182-1193.|Aquaculture. 2024 Jan 15, 578, 740081.|Biochem Biophys Res Commun. 2020 Mar 26;524(1):70-76.|Biochemistry (Moscow). 2021 May;86(5):568-576.|Biochim Biophys Acta Mol Cell Biol Lipids . 2020 Aug;1865(8):158711.|Biomed Pharmacother. 2020 Sep;129:110356.|Biomed Pharmacother. October 2022, 113653.|Biomedicines. 2021, 9(6), 677.|Bioorg Chem. 7 October 2022, 106191.|Bioorgan Med Chem. 15 February 2022, 116615.|Br J Pharmacol. 2020 May;177(10):2286-2302.|Cancer Cell Int. 2023 Aug 11;23(1):164.|Cancer Res. 2022 Apr 15;82(8):1503-1517.|Carcinogenesis. 2023 Mar 31;bgad015.|Cell Commun Signal. 2023 Sep 30;21(1):268.|Cell Death Differ. 2022 Nov 3.|Cell Death Dis. 2023 Apr 6;14(4):246.|Cell Death Discov. 2022 Apr 30;8(1):236.|Cell Metab. 2021 Mar 2;33(3):581-597.e9.|Cell Metab. 2023 Sep 7;S1550-4131(23)00304-2.|Cell Mol Biol Lett. 2022 Feb 2;27(1):11.|Cell Prolif. 2023 Jun 15;e13520.|Cell Signal. 2022 Mar 6;110299.|Cells. 2022, 11(1), 86.|Chem Eng J. 2023 Aug 6, 145212.|Chinese Pharmacological Bulletin. 2017, 33(4): 517-521. |Circulation. 2022 Nov 30.|Drug Dev Res. 2023 Apr 13.|Ecotoxicol Environ Saf. 2022 Jun 15;238:113611.|Endocr J. 2021 Oct 29.|Environ Int. 2023 Nov 25, 108354.|Eur J Med Chem. 2021 Aug 25;225:113807.|Eur J Med Chem. 5 February 2022, 114061.|Eur J Pharmacol. 2019 Jan 15;843:134-144.|Eur J Pharmacol. 2020 Sep 5;882:173300.|Eur J Pharmacol. 2022 Jul 31;175175.|Eur J Pharmacol. 2023 Oct 12:176113.|Food Funct. 2019 Dec 11;10(12):7983-7994.|Food Science and Human Wellness. 2023 Nov;12(6);2061-2072.|Free Radic Biol Med. 2018 Aug 21;126:259-268. |Front Cell Dev Biol. 2020 Jul 29;8:703.|Front Mol Neurosci. 2017 Sep 14;10:293.|Front Pharmacol. 2022 Jun 27;13:919202.|Front Physiol. 2019 Mar 1;10:165.|Front Vet Sci. 2023 Nov 17:10:1277586.|Immunol Invest. 2021 Apr 8;1-18.|Int Immunopharmacol. 2021 Jan;90:107150.|iScience. 10 October 2022, 105319.|iScience. 2023 Feb 28;26(4):106289.|J Cell Mol Med. 2019 Oct;23(10):7029-7042. |J Cell Physiol. 2019 Nov;234(11):20694-20703. |J Exp Med. 2022 May 2;219(5):e20211906.|J Zhejiang Univ Sci B. 2020 Dec; 21(12): 990–998.|Kidney Blood Press Res. 2021 Jul 28;1-12.|Life Sci. 2021 Jan 5;119013.|Nat Commun. 2023 Jun 2;14(1):3208.|Nat Commun. 2023 May 15;14(1):2779.|Oxid Med Cell Longev. 2021 Oct 14;2021:5527137.|Patent. US20180263995A1.|Pharmacol Res. 2020 Mar;153:104679.|Phytother Res. 2022 Nov 3.|PPAR Res. 2023 Nov 8:2023:6422804.|PPAR Res. 28 Sept 2022.|PPAR Res. 2019 Jul 1;2019:2715176. |Prog Neuropsychopharmacol Biol Psychiatry. 2023 Mar 25;110758.|Redox Biol. 2023 Jun.|Ren Fail. 2022 Dec;44(1):2056-2065.|Reprod Domest Anim. 2023 Sep 15.|Research Square Print. 2022 Aug.|Sci Total Environ. 2023 May 16;888:164073.|Sci Total Environ. 27 October 2022, 159755.|Stem Cells Dev. 2022 Sep 21.|Theranostics. 2022 Jan 24;12(4):1904-1920.|Theranostics. 2022 Nov 7;12(18):7699-7716.

References

– [1]Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6.|[2]Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8.|[3]Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70.|[4]Majeed Y, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels. Mol Pharmacol. 2011 Jun;79(6):1023-30.|[5]Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220.

CAS Number

– 155141-29-0

Molecular Weight

– 473.50

Compound Purity

– 99.88

SMILES

– O=C(O)/C=CC(O)=O.CN(CCOC1=CC=C(CC2C(NC(S2)=O)=O)C=C1)C3=CC=CC=N3

Clinical Information

– Launched

Research Area

– Cancer; Metabolic Disease; Inflammation/Immunology

Solubility

– DMSO : 100 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL (ultrasonic)

Target

– Autophagy;Ferroptosis;PPAR;TRP Channel

Isoform

– PPARγ

Pathway

– Apoptosis;Autophagy;Cell Cycle/DNA Damage;Membrane Transporter/Ion Channel;Neuronal Signaling;Vitamin D Related/Nuclear Receptor

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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