WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H124877
CAS#: 2455519-86-3
Description: ZYIL-1 is a NLRP3 inhibitor. ZYIL1 prevents NLRP3-induced apoptosis-associated speck-like protein containing a caspase activation and recruitment domain oligomerization, thus inhibiting NLRP3 inflammasome pathway. ZYIL1 showed rapid oral absorption. ZYIL1 is extremely potent (IC50 in nanomolar range) in human whole blood and supressed inflammation caused by the NLRP3 inflammasome. Robust effect on disease biomarkers including CRP, Serum Amyloid A (SAA), IL-6, WBC, was also observed.
Hodoodo Cat#: H124877
Name: ZYIL-1
CAS#: 2455519-86-3
Chemical Formula: C21H29N3O3S
Exact Mass: 403.19
Molecular Weight: 403.540
Elemental Analysis: C, 62.50; H, 7.24; N, 10.41; O, 11.89; S, 7.94
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Synonym: ZYIL-1; ZYIL1; ZYIL 1
IUPAC/Chemical Name: (R,E)-2-(1,2-dimethylpyrrolidin-2-yl)-N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)ethene-1-sulfonamide
InChi Key: HAMGPBKPACGWND-ZOXUKVPXSA-N
InChi Code: InChI=1S/C21H29N3O3S/c1-21(10-5-12-24(21)2)11-13-28(26,27)23-20(25)22-19-17-8-3-6-15(17)14-16-7-4-9-18(16)19/h11,13-14H,3-10,12H2,1-2H3,(H2,22,23,25)/b13-11+/t21-/m1/s1
SMILES Code: O=C(NS(/C=C/[C@@]1(C)CCCN1C)(=O)=O)NC2=C3CCCC3=CC4=C2CCC4
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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: n recent years, a new target closely linked to a variety of diseases has appeared in the researchers' vision, which is the NLRP3 inflammasome. With the deepening of the study of NLRP3 inflammasome, it was found that it plays an extremely important role in a variety of physiological pathological processes, and NLRP3 inflammasome was also found to be associated with some age-related diseases. It is associated with the development of insulin resistance, Alzheimer's disease, Parkinson's, cardiovascular aging, hearing and vision loss. At present, the only clinical approach to the treatment of NLRP3 inflammasome-related diseases is to use anti-IL-1β antibodies, but NLRP3-specific inhibitors may be better than the IL-1β antibodies. This article reviews the relationship between NLRP3 inflammasome and aging diseases: summarizes some of the relevant experimental results reported in recent years, and introduces the biological signals or pathways closely related to the NLRP3 inflammasome in a variety of aging diseases, and also introduces some promising small molecule inhibitors of NLRP3 inflammasome for clinical treatment, such as: ZYIL1, DFV890 and OLT1177, they have excellent pharmacological effects and good pharmacokinetics.
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The following data is based on the product molecular weight 403.54 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 |
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1: Yuan Z, Yu D, Gou T, Tang G, Guo C, Shi J. Research progress of NLRP3 inflammasome and its inhibitors with aging diseases. Eur J Pharmacol. 2023 Oct 15;957:175931. doi: 10.1016/j.ejphar.2023.175931. Epub 2023 Jul 24. PMID: 37495038.
2: Parmar DV, Kansagra KA, Momin T, Patel HB, Jansari GA, Bhavsar J, Shah C, Patel JM, Ghoghari A, Barot A, Sharma B, Viswanathan K, Patel HV, Jain MR. Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Oral NLRP3 Inflammasome Inhibitor ZYIL1: First-in-Human Phase 1 Studies (Single Ascending Dose and Multiple Ascending Dose). Clin Pharmacol Drug Dev. 2023 Feb;12(2):202-211. doi: 10.1002/cpdd.1162. Epub 2022 Sep 5. PMID: 36065092; PMCID: PMC10087697.
3: Hissaria P, Kansagra K, Patel H, Momin T, Ghoghari A, Patel H, Sharma B. Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ZY-IL1 in Three Patients with Cryopyrin-Associated Periodic Syndromes. Clin Pharmacol Drug Dev. 2023 Aug 14. doi: 10.1002/cpdd.1318. Epub ahead of print. PMID: 37577847.
