2767369-80-0
2767369-80-0 structure
- Name: NLRP3-IN-14
- Chemical Name: NLRP3-IN-14
- CAS Number: 2767369-80-0
- Molecular Formula: C27H28N2O4
- Molecular Weight: 444.52
- Catalog: Signaling Pathways Immunology/Inflammation NOD-like Receptor (NLR)
- Create Date: 2023-05-06 08:43:21
- Modify Date: 2024-01-05 16:59:29
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NLRP3-IN-14 is a potent and selective NLRP3 inflammasome inhibitor (KD: 5.87 μM). NLRP3-IN-14 inhibits IL-1β release with an IC50 of 0.131 μM. NLRP3-IN-14 can be used for the research of inflammation[1].
| Name | NLRP3-IN-14 |
|---|
| Description | NLRP3-IN-14 is a potent and selective NLRP3 inflammasome inhibitor (KD: 5.87 μM). NLRP3-IN-14 inhibits IL-1β release with an IC50 of 0.131 μM. NLRP3-IN-14 can be used for the research of inflammation[1]. |
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| Related Catalog | |
| Target |
NLRP3 inflammasome:5.87 μM (Kd) |
| In Vitro | NLRP3-IN-14 (化合物 5j) 抑制 IL-1β 释放，IC50 为 0.131 μM (ELISA 测定) [1]。 NLRP3-IN-14 (2 μM，3 小时) 抑制小鼠腹膜巨噬细胞 (PM) 中 IL-1β (p17) 和 caspase-1 (p20) 的分泌[1]。 NLRP3-IN-14 通过抑制 ASC 寡聚化来抑制 NLRP3 炎性体复合物的形成[1]。 NLRP3-IN-14 (10 μM，5 小时) 随着温度升高抑制蛋白质 NLRP3 的降解[1]。 NLRP3-IN-14 在人和小鼠肝微粒体中表现出代谢稳定性 (T1/2: 866.3 min; Clint: 1.6 μL/min/mg)[1]. Western Blot Analysis[1] Cell Line: Mice peritoneal macrophages(PMs) Concentration: 2 μM Incubation Time: 3 h Result: Inhibited the secretion of IL-1β (p17) and caspase-1 (p20), without affecting pro-IL-1β and pro-caspase-1. |
| In Vivo | NLRP3-IN-14 (化合物 5j) (50 mg/kg;i.p.) 在败血症小鼠模型中表现出抗炎作用[1]。 Animal Model: LPS-induced inflammatory septic mouse model[1] Dosage: 50 mg/kg Administration: i.p. Result: Decreased the release of IL-1β in mouse serum. Relieved thickening of the alveolar wall in lung. Animal Model: Mice[1] Dosage: 20 or 5 mg/kg Administration: p.o. or i.v. Result: Pharmacokinetic profile of NLRP3-IN-14 (compound 5j). parameter dose (mg/kg) T1/2 (h) Tmax (h) F (%) PO 20 9.225 0.389 3.0 IV 5 5.028 0.083 |
| References |
| Molecular Formula | C27H28N2O4 |
|---|---|
| Molecular Weight | 444.52 |