309913-42-6

309913-42-6 structure

Name: SX 011
Chemical Name: 2-[6-chloro-5-[4-[(4-fluorophenyl)methyl]piperidine-1-carbonyl]-1-methylindol-3-yl]-N,N-dimethyl-2-oxoacetamide
CAS Number: 309913-42-6
Molecular Formula: C₂₆H₂₇ClFN₃O₃
Molecular Weight: 483.96
Create Date: 2016-10-21 21:53:06
Modify Date: 2024-01-21 10:42:18
SX 011 is a p38 inhibitor with IC50s of 9 nM and 90 nM against p38α and p38β, respectively. SX 011 also inhibits JNK-2 with an IC50 of 100 nM. SX-011 is orally bioavailable[1].

Name	2-[6-chloro-5-[4-[(4-fluorophenyl)methyl]piperidine-1-carbonyl]-1-methylindol-3-yl]-N,N-dimethyl-2-oxoacetamide
Synonyms	sx 011

Description	SX 011 is a p38 inhibitor with IC50s of 9 nM and 90 nM against p38α and p38β, respectively. SX 011 also inhibits JNK-2 with an IC50 of 100 nM. SX-011 is orally bioavailable[1].
Related Catalog	Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK Research Areas >> Inflammation/Immunology Signaling Pathways >> MAPK/ERK Pathway >> JNK
Target	p38α:9 nM (IC50) p38β:90 nM (IC50) p38δ:> 300,000 nM (IC50) p38γ:> 300,000 nM (IC50) JNK2:100 nM (IC50) JNK1:> 300,000 nM (IC50)
In Vitro	SX-011 抑制 LPS 刺激的人外周血单个核细胞 (PBMC) TNFα 和白细胞介素-1β (IL-1β)，IC50 分别为 200 nM 和 900 nM。此外，IL-6 (IC50 250 nM) 和 IL-8 (IC50 100 nM) 在该实验中被显著抑制[2]。
In Vivo	SX-011 在临床前物种中具有口服利用率 (rat, 24%; monkey, 29%; dog, 43%)，并已证明对大鼠急性和慢性炎症模型均有效。Rat t1/2 = 30 min[1][2]。
References	[1]. Lee MR, et al. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein. Curr Med Chem. 2005;12(25):2979-94. [2]. Hynes J Jr, et al. Small molecule p38 inhibitors: novel structural features and advances from 2002-2005. Curr Top Med Chem. 2005;5(10):967-85.