SX 011

Names

[ Name ]:
SX 011

[Synonym ]:
sx 011

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₆H₂₇ClFN₃O₃

[ Molecular Weight ]:
483.96

[ Exact Mass ]:
483.17200

[ PSA ]:
62.62000

[ LogP ]:
4.27450

Related Compounds

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