Basic info:
CY-09 is a specific NLRP3 inflammasome 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.
In vitro:
CY-09 specifically blocks NLRP3 activation in macrophages. This compound inhibits NLRP3 oligomerization and inflammasome assembly. It directly binds to NLRP3 and inhibits its ATPase activity.
The metabolic stability of this chemical 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 this compound 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[1].
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, this compound 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%.
It reverses metabolic disorders in diabetic mice by inhibition of NLRP3-dependent inflammation. This chemical treatment has remarkable beneficial effects for metainflammation, hyperglycemia, and insulin resistance in diabetic mice[1].
Biological Activity:
CY-09 is an NLRP3 inflammasone inhibitor. CY-09 binds directly to the ATP-binding motif of NLRP3 NACHT domain and inhibits its ATPase activity, blocking NLRP3 inflammasome assembly and activation.
In mouse models CY-09 showed therapeutic effects in type 2 diabetes and cryopyrin-associated auto-inflammatory syndrome (CAPS), which is caused by gain-of-function mutations of NLRP3.
Other specs:
M.W.: 423.43 Formula: C19H12F3NO3S2 CAS: 1073612-91-5
Appearance: Light yellow to yellow
Transportation condition:Room temperature in continental US; may vary elsewhere.
Storage:
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
- 20°C 1 month
CONTACT/Email address: Joy Wu Email: Joy@coreychem.com
