YQ128

CAS NO.：2454246-18-3
Empirical Formula: C27H29ClN2O4S2
Molecular Weight: 545.11
MDL number: MFCD32263442
Update Date: 2025-07-04 15:27:57

What is YQ128?

Biological Activity

YQ128 is a potent and selective second-generation NLRP3 inflammasome inhibitor with IC50 of 0.30 μM. YQ128 significantly and selectively inhibited the production of IL-1β, but not TNF-α. YQ128 can cross the blood-brain barrier to reach the central nervous system. YQ128 has anti-inflammatory activity.

in vitro

YQ128 (0.3-100 μM; 30 mins) dose dependently suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC ₅₀ of 1.59 μM.
YQ128 (20 μM; 2 hours) shows no significant toxic effects on hCMEC/D3 cells.

Cell Viability Assay

< td class="col1"> Cell Line:

Mouse peritoneal macrophages
Concentration:	0.3, 1.0, 3.0, 10, 30, 100 μM
Incubation Time:	30 mins
Result:	Suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC ₅₀ of 1.59 μM.

in vivo

YQ128 (iv; 20 mg/kg) has an intermediate terminal plasma half-life (t _1/2 ) of 6.6 hours after iv administration.
YQ128 (oral ; 20 mg/kg) shows delayed gastrointestinal absorption with at _max and c _max of 12 h and 73 ng/mL, respectively. Oral bioavailability (F _{oral < /sub> ) is estimated as 10%.
YQ128 exhibits extensive extravascular distribution with a large steady-state volume of distribution (Vd _ss ) of 8.5 L/kg and rapid total clearance (CL _tot ) of 41 mL/min/kg.
has been shown to trigger IL-1β production in a NLRP3-dependent manner in C57BL/6 mice. < /p>}

< tr> Administration: < td class="col2"> Had an intermediate terminal plasma half-life (t _1/2 ) of 6.6 hours after iv administration.

Animal Model:	Sprague-Dawley rats (200-250 g)
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Iv
Result:

Properties of YQ128

Boiling point:	705.8±70.0 °C(Predicted)
Density	1.287±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: 250 mg/mL (458.62 mM)
pka	9.32±0.50(Predicted)
form	A crystalline solid
color	White to off-white

Safety information for YQ128

Computed Descriptors for YQ128

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