化合物YQ128
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- CAS号:
- 2454246-18-3
- 英文名:
- YQ128
- 英文别名:
- YQ128;YQ128,inhibit,YQ 128,Inhibitor,NOD-like Receptor (NLR),Interleukin Related,YQ-128;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
- 中文名:
- 化合物YQ128
- 中文别名:
- 化合物YQ128
- CBNumber:
- CB98199880
- 分子式:
- C27H29ClN2O4S2
- 分子量:
- 545.11
- MOL File:
- 2454246-18-3.mol
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化合物YQ128化学性质
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沸点:
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705.8±70.0 °C(Predicted)
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密度:
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1.287±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 250 mg/mL (458.62 mM)
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形态:
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A crystalline solid
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酸度系数(pKa):
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9.32±0.50(Predicted)
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化合物YQ128性质、用途与生产工艺
YQ128 是有效的，选择性第二代 NLRP3 炎性体抑制剂，IC50 为 0.30 µM。YQ128 能显着和选择性地抑制 IL-1β 的产生，但不抑制 TNF-α 的产生。YQ128 可以穿过血脑屏障到达中枢神经系统。YQ128 具有抗炎活性。
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NLRP3
0.30 μM (IC
50
)
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IL-1β
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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
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Cell Line:
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Mouse peritoneal macrophages
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Concentration:
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0.3, 1.0, 3.0, 10, 30, 100 µM
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Incubation Time:
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30 mins
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Result:
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Suppressed the release of IL-1β from peritoneal macrophages upon LPS/ATP challenge with an IC
50
of 1.59 µM.
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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.
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Animal Model:
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Sprague-Dawley rats (200-250 g)
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Dosage:
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20 mg/kg (Pharmacokinetic Analysis)
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Administration:
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Iv
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Result:
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Had an intermediate terminal plasma half-life (t
1/2
) of 6.6 hours after iv administration.
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化合物YQ128
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-130252 | YQ128 | | 1 mg | 650元 |
| 2024/04/30 | HY-130252 | YQ128 | | 5 mg | 1300元 |
2454246-18-3, 化合物YQ128 相关搜索:
- 天然产物
- C27H29ClN2O4S2
- 化合物YQ128
- 2454246-18-3
- YQ128,inhibit,YQ 128,Inhibitor,NOD-like Receptor (NLR),Interleukin Related,YQ-128
- YQ128
- N-[(5-chloro-2-propoxyphenyl)methyl]-N-(2-{4-[(pr
op-2-yn-1-yl)sulfamoyl]phenyl}ethyl)-2-(thiophen-
3-yl)acetamide
- 3-Thiopheneacetamide, N-[(5-chloro-2-propoxyphenyl)methyl]-N-[2-[4-[(2-propyn-1-ylamino)sulfonyl]phenyl]ethyl]-