2454246-18-3
2454246-18-3 結(jié)構(gòu)式
基本信息
3-Thiopheneacetamide, N-[(5-chloro-2-propoxyphenyl)methyl]-N-[2-[4-[(2-propyn-1-ylamino)sulfonyl]phenyl]ethyl]-
N-[(5-chloro-2-propoxyphenyl)methyl]-N-(2-{4-[(pr op-2-yn-1-yl)sulfamoyl]phenyl}ethyl)-2-(thiophen- 3-yl)acetamide
物理化學(xué)性質(zhì)
常見問題列表
|
NLRP3 0.30 μM (IC 50 ) |
IL-1β
|
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
| 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. |
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 a t
max
and c
max
of 12 h and 73 ng/mL, respectively. Oral bioavailability (F
oral
) 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.
YQ128 (10 mg/kg) has been shown to trigger IL-1β production in a NLRP3- dependent manner in C57BL/6 mice.
| Animal Model: | Sprague-Dawley rats (200-250 g) |
| Dosage: | 20 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Iv |
| Result: | Had an intermediate terminal plasma half-life (t 1/2 ) of 6.6 hours after iv administration. |