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MedKoo Cat#: 584491 | Name: CY 09
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Description:

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

CY 09 is a NLRP3 inhibitor that blocks NLRP3 inflammasome assembly and activation, and displays therapeutic effects on mouse models of cryopyrin-associated autoinflammatory syndrome (CAPS) and type 2 diabetes. CY-09 Alleviates the Depression-like Behaviors via Inhibiting NLRP3 Inflammasome-Mediated Neuroinflammation in Lipopolysaccharide-Induced Mice. CY-09 attenuates the progression of osteoarthritis via inhibiting NLRP3 inflammasome-mediated pyroptosis.

Chemical Structure

CY 09
CY 09
CAS#1073612-91-5

Theoretical Analysis

MedKoo Cat#: 584491

Name: CY 09

CAS#: 1073612-91-5

Chemical Formula: C19H12F3NO3S2

Exact Mass: 423.0211

Molecular Weight: 423.42

Elemental Analysis: C, 53.90; H, 2.86; F, 13.46; N, 3.31; O, 11.34; S, 15.14

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 3,750.00 Ready to ship
2g USD 6,250.00 Ready to ship
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Synonym
CY 09; CY-09; CY09
IUPAC/Chemical Name
4-[[4-Oxo-2-thioxo-3-[[3-(trifluoromethyl)phenyl]methyl]-5-thiazolidinylidene]methyl]benzoic acid
InChi Key
DJTINRHPPGAPLD-OQLLNIDSSA-N
InChi Code
InChI=1S/C19H12F3NO3S2/c20-19(21,22)14-3-1-2-12(8-14)10-23-16(24)15(28-18(23)27)9-11-4-6-13(7-5-11)17(25)26/h1-9H,10H2,(H,25,26)/b15-9+
SMILES Code
O=C(O)C1=CC=C(/C=C(SC(N2CC3=CC=CC(C(F)(F)F)=C3)=S)\C2=O)C=C1
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
>3 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:
CY-09 is a selective and direct NLRP3 inhibitor.
In vitro activity:
This research was conducted to confirm whether NLRP3 expression and activity are impacted in the development of OA and to detect the role of CY-09, a selective and direct inhibitor of NLRP3 in the in vitro and in vivo models of OA. The findings corroborated that the expression of NLRP3 is stimulated in OA cartilage. CY-09 can maintain extracellular matrix (ECM) homeostasis and regulate inflammation in TNF-α treated chondrocytes via inhibition of NLRP3 inflammasome-mediated pyroptosis. In conclusion, the research indicates that experimental OA activated the NLRP3 activity, and pharmacological inhibition of NLRP3 inflammasome activation by CY-09 protects chondrocytes against inflammation and attenuates OA development. Biochem Biophys Res Commun. 2021 May 14;553:119-125. https://pubmed.ncbi.nlm.nih.gov/33765556/
In vivo activity:
In diabetic mice, NLRP3-dependent low-grade metainflammation in metabolic organs, such as liver or adipose tissue, is critical for the development of T2D (Stienstra et al., 2010; Yan et al., 2013). To further confirm that CY-09 reverses metabolic disorders through inhibition of NLRP3 activation, it was examined whether CY-09 treatment inhibited NLRP3 inflammasome activation and metainflammation in diabetic mice. As expected, NLRP3-dependent IL-1β production in serum, liver, or adipose tissues of HFDtreated mice was impaired by CY-09 treatment (Fig. 9, A–C). The caspase-1 cleavage observed in adipose tissue of HFD-treated mice was also suppressed by CY-09 (Fig. 9 D), indicating that CY-09 treatment can inhibit metabolic stress-induced inflammasome activation in vivo. In addition, the production of TNF-α and MCP-1, which are inflammasome-independent cytokines, were also decreased in HFD-treated mice (Fig. 9, E–H), which was consistent with the observation in Nlrp3−/− mice. These results suggest that CY-09 treatment not only blocks metabolic stress-induced NLRP3 inflammasome activation but also suppresses NLRP3-dependent metainflammation. Thus, these results indicate that CY-09 can treat metabolic disorders by inhibition of NLRP3 inflammasome in diabetic mice. J Exp Med. 2017 Nov 6; 214(11): 3219–3238. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5679172/
Solvent mg/mL mM
Solubility
DMSO 65.0 152.61
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 423.42 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:
1. Sun R, Peng M, Xu P, Huang F, Xie Y, Li J, Hong Y, Guo H, Liu Q, Zhu W. Low-density lipoprotein receptor (LDLR) regulates NLRP3-mediated neuronal pyroptosis following cerebral ischemia/reperfusion injury. J Neuroinflammation. 2020 Nov 5;17(1):330. doi: 10.1186/s12974-020-01988-x. PMID: 33153475; PMCID: PMC7643474. 2. Zhang Y, Lin Z, Chen D, He Y. CY-09 attenuates the progression of osteoarthritis via inhibiting NLRP3 inflammasome-mediated pyroptosis. Biochem Biophys Res Commun. 2021 May 14;553:119-125. doi: 10.1016/j.bbrc.2021.03.055. Epub 2021 Mar 22. PMID: 33765556. 3. Wang X, Sun K, Zhou Y, Wang H, Zhou Y, Liu S, Nie Y, Li Y. NLRP3 inflammasome inhibitor CY-09 reduces hepatic steatosis in experimental NAFLD mice. Biochem Biophys Res Commun. 2021 Jan 1;534:734-739. doi: 10.1016/j.bbrc.2020.11.009. Epub 2020 Nov 16. PMID: 33213837 4. Jiang H, He H, Chen Y, Huang W, Cheng J, Ye J, Wang A, Tao J, Wang C, Liu Q, Jin T, Jiang W, Deng X, Zhou R. Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J Exp Med. 2017 Nov 6;214(11):3219-3238. doi: 10.1084/jem.20171419. Epub 2017 Oct 11. PMID: 29021150; PMCID: PMC5679172.
In vitro protocol:
1. Sun R, Peng M, Xu P, Huang F, Xie Y, Li J, Hong Y, Guo H, Liu Q, Zhu W. Low-density lipoprotein receptor (LDLR) regulates NLRP3-mediated neuronal pyroptosis following cerebral ischemia/reperfusion injury. J Neuroinflammation. 2020 Nov 5;17(1):330. doi: 10.1186/s12974-020-01988-x. PMID: 33153475; PMCID: PMC7643474. 2. Zhang Y, Lin Z, Chen D, He Y. CY-09 attenuates the progression of osteoarthritis via inhibiting NLRP3 inflammasome-mediated pyroptosis. Biochem Biophys Res Commun. 2021 May 14;553:119-125. doi: 10.1016/j.bbrc.2021.03.055. Epub 2021 Mar 22. PMID: 33765556.
In vivo protocol:
1. Wang X, Sun K, Zhou Y, Wang H, Zhou Y, Liu S, Nie Y, Li Y. NLRP3 inflammasome inhibitor CY-09 reduces hepatic steatosis in experimental NAFLD mice. Biochem Biophys Res Commun. 2021 Jan 1;534:734-739. doi: 10.1016/j.bbrc.2020.11.009. Epub 2020 Nov 16. PMID: 33213837. 2. Jiang H, He H, Chen Y, Huang W, Cheng J, Ye J, Wang A, Tao J, Wang C, Liu Q, Jin T, Jiang W, Deng X, Zhou R. Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J Exp Med. 2017 Nov 6;214(11):3219-3238. doi: 10.1084/jem.20171419. Epub 2017 Oct 11. PMID: 29021150; PMCID: PMC5679172.
1: Methods In Medicine CAM. Retracted: CY-09 Inhibits NLRP3 Inflammasome Activation to Relieve Pain via TRPA1. Comput Math Methods Med. 2023 Aug 2;2023:9759851. doi: 10.1155/2023/9759851. PMID: 37564771; PMCID: PMC10412149. 2: Zhang T, Wu X, Liu B, Huang H, Zhou C, Liang P. The contribution of probiotics for the double-edge effect of cefazolin on postoperative neurocognitive disorders by rebalancing the gut microbiota. Front Neurosci. 2023 Apr 27;17:1156453. doi: 10.3389/fnins.2023.1156453. PMID: 37179548; PMCID: PMC10174111. 3: Han S, He Z, Hu X, Li X, Zheng K, Huang Y, Xiao P, Xie Q, Ni J, Liu Q. Inhibiting NLRP3 Inflammasome Activation by CY-09 Helps to Restore Cerebral Glucose Metabolism in 3×Tg-AD Mice. Antioxidants (Basel). 2023 Mar 15;12(3):722. doi: 10.3390/antiox12030722. PMID: 36978970; PMCID: PMC10045645. 4: Chi S, Li S, Xu Z, Yang G, Song Y, Liao Z, Yang C, Wu X. The involvement of DDX3X in compression-induced nucleus pulposus pyroptosis. Biochem Biophys Res Commun. 2023 May 7;655:1-10. doi: 10.1016/j.bbrc.2023.02.074. Epub 2023 Mar 3. PMID: 36907112. 5: Paguaga ME, Penn JS, Uddin MI. A novel optical imaging probe for targeted visualization of NLRP3 inflammasomes in a mouse model of age-related macular degeneration. Front Med (Lausanne). 2023 Jan 10;9:1047791. doi: 10.3389/fmed.2022.1047791. PMID: 36703888; PMCID: PMC9871584. 6: Tousif S, Singh AP, Umbarkar P, Galindo C, Wheeler N, Toro Cora A, Zhang Q, Prabhu SD, Lal H. Ponatinib Drives Cardiotoxicity by S100A8/A9-NLRP3-IL-1β Mediated Inflammation. Circ Res. 2023 Feb 3;132(3):267-289. doi: 10.1161/CIRCRESAHA.122.321504. Epub 2023 Jan 10. PMID: 36625265; PMCID: PMC9898181. 7: Zhu Q, Zheng F, You W, Kang X, Chen C, Pan Z, Zhou J, Hu W. Expression of Histone H1 in Rats with Traumatic Brain Injury and the Effect of the NLRP3 Inflammasome Pathway. World Neurosurg. 2023 Mar;171:e286-e290. doi: 10.1016/j.wneu.2022.12.009. Epub 2022 Dec 9. PMID: 36509326. 8: Wang Y, Liu YJ, Zhang MM, Zhou H, Gao YH, Cheng WJ, Ye ZW, Yuan ZY, Xu GH, Li CF, Yi LT. CY-09 Alleviates the Depression-like Behaviors via Inhibiting NLRP3 Inflammasome-Mediated Neuroinflammation in Lipopolysaccharide-Induced Mice. ACS Chem Neurosci. 2022 Dec 7;13(23):3291-3302. doi: 10.1021/acschemneuro.2c00348. Epub 2022 Nov 18. PMID: 36399525. 9: Wang A, Zheng N, Jia Q, Chen Y, Xu S. S100A9‑containing serum exosomes obtained from patients with burn injuries promote myocardial cell pyroptosis through NLRP3. Exp Ther Med. 2022 Sep 1;24(5):646. doi: 10.3892/etm.2022.11583. PMID: 36277145; PMCID: PMC9532836. 10: Bai X, Liu P, Shen H, Zhang Q, Zhang T, Jin X. Water-extracted Lonicera japonica polysaccharide attenuates allergic rhinitis by regulating NLRP3-IL-17 signaling axis. Carbohydr Polym. 2022 Dec 1;297:120053. doi: 10.1016/j.carbpol.2022.120053. Epub 2022 Sep 3. PMID: 36184153. 11: Yang M, Zhao L. The Selective NLRP3-Inflammasome Inhibitor CY-09 Ameliorates Kidney Injury in Diabetic Nephropathy by Inhibiting NLRP3- inflammasome Activation. Curr Med Chem. 2023;30(28):3261-3270. doi: 10.2174/0929867329666220922104654. PMID: 36154582. 12: Jin GN, Lu JM, Lan HW, Lu YN, Shen XY, Xu X, Piao LX. Protective effect of ginsenoside Rh2 against Toxoplasma gondii infection-induced neuronal injury through binding TgCDPK1 and NLRP3 to inhibit microglial NLRP3 inflammasome signaling pathway. Int Immunopharmacol. 2022 Nov;112:109176. doi: 10.1016/j.intimp.2022.109176. Epub 2022 Sep 5. PMID: 36067653. 13: Wu Y, Chang J, Ge J, Xu K, Zhou Q, Zhang X, Zhu N, Hu M. Isobavachalcone's Alleviation of Pyroptosis Contributes to Enhanced Apoptosis in Glioblastoma: Possible Involvement of NLRP3. Mol Neurobiol. 2022 Nov;59(11):6934-6955. doi: 10.1007/s12035-022-03010-2. Epub 2022 Sep 2. PMID: 36053436. 14: Wrublewsky S, Speer T, Nalbach L, Boewe AS, Pack M, Alansary D, Roma LP, Hoffmann MDA, Schmitt BM, Weinzierl A, Menger MD, Laschke MW, Ampofo E. Targeting Pancreatic Islet NLRP3 Improves Islet Graft Revascularization. Diabetes. 2022 Aug 1;71(8):1706-1720. doi: 10.2337/db21-0851. PMID: 35622000. 15: Zhou FW, Zhang T, Jin Y, Ma YF, Xian ZP, Wu ZM, Yu GD. [Effects of NLRP3-mediated pyroptosis on olfaction dysfunction in allergic rhinitis]. Zhonghua Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2022 Apr 7;57(4):433-441. Chinese. doi: 10.3760/cma.j.cn115330-20210629-00383. PMID: 35527434. 16: Lu J, Xie S, Deng Y, Xie X, Liu Y. Blocking the NLRP3 inflammasome reduces osteogenic calcification and M1 macrophage polarization in a mouse model of calcified aortic valve stenosis. Atherosclerosis. 2022 Apr;347:28-38. doi: 10.1016/j.atherosclerosis.2022.03.005. Epub 2022 Mar 10. PMID: 35299058. 17: Li N, Wang Y, Wang X, Sun N, Gong YH. Pathway network of pyroptosis and its potential inhibitors in acute kidney injury. Pharmacol Res. 2022 Jan;175:106033. doi: 10.1016/j.phrs.2021.106033. Epub 2021 Dec 14. PMID: 34915124. 18: Zhu Y, Huang G, Yang Y, Yong C, Yu X, Wang G, Yi L, Gao K, Tian F, Qian S, Zhou E, Zou Y. Chinese Herbal Medicine Suyin Detoxification Granule Inhibits Pyroptosis and Epithelial-Mesenchymal Transition by Downregulating MAVS/NLRP3 to Alleviate Renal Injury. J Inflamm Res. 2021 Dec 7;14:6601-6618. doi: 10.2147/JIR.S341598. PMID: 34908861; PMCID: PMC8665879. 19: Guo X, Xu X, Li T, Yu Q, Wang J, Chen Y, Ding S, Zhu L, Zou G, Zhang X. NLRP3 Inflammasome Activation of Mast Cells by Estrogen via the Nuclear- Initiated Signaling Pathway Contributes to the Development of Endometriosis. Front Immunol. 2021 Sep 22;12:749979. doi: 10.3389/fimmu.2021.749979. PMID: 34630429; PMCID: PMC8494307. 20: Huang Z, Chen H, Wang S, Wei H, Wang X, Shen R, Wang Y, Lin R, Lin J. Corrigendum: NLRP3 Overexpression Associated With Poor Prognosis and Presented as an Effective Therapeutic Target in Osteosarcoma. Front Pharmacol. 2021 Sep 2;12:753231. doi: 10.3389/fphar.2021.753231. Erratum for: Front Pharmacol. 2021 Jul 28;12:724923. PMID: 34539420; PMCID: PMC8444229.