| Identification | Back Directory | [Name]
3-Thiopheneacetamide, N-[(5-chloro-2-propoxyphenyl)methyl]-N-[2-[4-[(2-propyn-1-ylamino)sulfonyl]phenyl]ethyl]- | [CAS]
2454246-18-3 | [Synonyms]
3-Thiopheneacetamide, N-[(5-chloro-2-propoxyphenyl)methyl]-N-[2-[4-[(2-propyn-1-ylamino)sulfonyl]phenyl]ethyl]- | [Molecular Formula]
C27H29ClN2O4S2 | [MDL Number]
MFCD32263442 | [MOL File]
2454246-18-3.mol | [Molecular Weight]
545.11 |
| Chemical Properties | Back Directory | [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) | [form ]
A crystalline solid | [pka]
9.32±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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> | Animal Model: | Sprague-Dawley rats (200-250 g) | | Dosage: | 20 mg/kg (Pharmacokinetic Analysis) | Administration: | Iv | | Result: | < td class="col2"> Had an intermediate terminal plasma half-life (t 1/2 ) of 6.6 hours after iv administration. |
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