[CAS NO. 1073612-91-5] CY-09
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PRODUCTS SPECIFICATIONS [1073612-91-5]
Store
Catalog
SLK-S5774
Brand
Selleck
CAS
1073612-91-5
DESCRIPTION [1073612-91-5]
Overview
| MDL | MFCD31619349 |
|---|---|
| Molecular Weight | 423.43 |
| Molecular Formula | C19H12F3NO3S2 |
| SMILES | O=C(O)C1=CC=C(/C=C(SC(N2CC3=CC=CC(C(F)(F)F)=C3)=S)\C2=O)C=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3617 mL | 11.8083 mL | 23.6167 mL |
| 5 mM | 0.4723 mL | 2.3617 mL | 4.7233 mL |
| 10 mM | 0.2362 mL | 1.1808 mL | 2.3617 mL |
| 50 mM | 0.0472 mL | 0.2362 mL | 0.4723 mL |
Description
CY-09 is a specific inhibitor that directly targeted NLRP3 itself。 It is tested against the five major cytochrome P450 enzymes 1A2, 2C9, 2C19, 2D6, and 3A4 with half maximal inhibitory concentration (IC50) values of 18.9, 8.18, >50, >50, and 26.0 µM, respectively.
Targets
| NLRP3 inflammasome [1] |
In vitro
CY-09 specifically blocks NLRP3 activation in macrophages. CY-09 inhibits NLRP3 oligomerization and inflammasome assembly. CY-09 directly binds to NLRP3 and inhibits its ATPase activity. The metabolic stability of CY-09 was first evaluated using human and mouse liver microsomes, exhibiting favorable stability with the half-life >145 min for both human and mouse microsomes. The metabolic stability of CY-09 was first evaluated using human and mouse liver microsomes, exhibiting favorable stability with the half-life >145 min for both human and mouse microsomes, which exhibited low risk of drug-drug interactions.
In vivo
CY-09 inhibits NLRP3 activation in vivo and prevents neonatal lethality in a mouse model of CAPS. In pharmacokinetic studies evaluted in C57BL/6J mice administered a single i.v. or oral dose, CY-09 exhibits favorable pharmacokinetics, with a half-life of 2.4 h, an area under the curve of 8,232 (h·ng)/ml, and bioavailability of 72%. CY-09 reverses metabolic disorders in diabetic mice by inhibition of NLRP3-dependent inflammation. CY-09 treatment has remarkable beneficial effects for metainflammation, hyperglycemia, and insulin resistance in diabetic mice.
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