sb 220025

Modify Date: 2024-01-12 17:48:58

sb 220025 Structure
sb 220025 structure
Common Name sb 220025
CAS Number 165806-53-1 Molecular Weight 338.38
Density N/A Boiling Point N/A
Molecular Formula C18H19FN6 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of sb 220025


SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation[1][2].

 Names

Name sb 220025

 sb 220025 Biological Activity

Description SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation[1][2].
Related Catalog
Target

p38:60 nM (IC50)

p56-Lck:3.5 μM (IC50)

PKC:2.89 μM (IC50)

In Vitro SB 220025 (20 μM; 6 h) 显着降低 HUVEC 细胞中响应球型脂联素 (gAd) 的 IL-8 基因表达[1]。 RT-PCR[1] Cell Line: HUVEC cells Concentration: 20 μM Incubation Time: 6 h Result: Inhibited MCP-1 gene expression.
In Vivo SB 220025 (3-50 mg/kg; p.o.; single) 可抑制体内炎症细胞因子的产生[2]。 SB 220025 (5, 30, 50 mg/kg; i.p.; bid) 抑制小鼠气囊肉芽肿模型的血管生成[2]。 SB 220025 (30 mg/kg; p.o.; twice a day for 3, 5, 7 or 14 days) 防止小鼠气囊血管生成模型第 3 天后发生的血管生成增加[2]。 SB 220025 (50 mg/kg; p.o.; b.i.d.; 10 days) 在慢性炎症疾病模型中有效地阻止关节炎的进展[2]。 Animal Model: Acute model of LPS-induced TNF-a expression[2]. Dosage: 3-50 mg/kg Administration: Oral administration; single; 30 min before challenge with LPS. Result: Dosedependently inhibited TNF-a production with an ED50 value of 7.5 mg/kg, and showed more than 80% inhibition when at 50 mg/kg. Animal Model: Murine air pouch granuloma model[2]. Dosage: 5, 30, 50 mg/kg Administration: Intraperitoneal injection; bisindie (bid, twice a day). Result: Caused a dose-dependent reduction in angiogenesis. Animal Model: Murine air pouch granuloma model[2]. Dosage: 30 mg/kg Administration: Oral administration; twice a day from day 0 until removal of granuloma tissue at days 3, 5, 7 or 14. Result: Did not affect the initial burst of angiogenesis but did prevent the increase in angiogenesis that occurs after day 3.
References

[1]. Tomizawa A, et al. Induction of gene expression in response to globular adiponectin in vascular endothelial cells. Life Sci. 2009 Sep 9;85(11-12):457-61.  

[2]. Jackson JR, et al. Pharmacological effects of SB 220025, a selective inhibitor of P38 mitogen-activated protein kinase, in angiogenesis and chronic inflammatory disease models. J Pharmacol Exp Ther. 1998 Feb;284(2):687-92.  

 Chemical & Physical Properties

Molecular Formula C18H19FN6
Molecular Weight 338.38
Exact Mass 338.16600
PSA 81.65000
LogP 3.56290

 Safety Information

HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%
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