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FR 167653 (FR 167653 sulfate) Sale

(Synonyms: FR 167653 sulfate) 目录号 : GC32411

FR 167653 (FR 167653硫酸盐) (FR 167653 (FR 167653硫酸盐)),一种具有口服活性和选择性的p38 MAPK抑制剂,是TNF-α的强效抑制剂;和 IL-1β;通过特异性抑制 p38 MAPK 活性产生。

FR 167653 (FR 167653 sulfate) Chemical Structure

Cas No.:158876-66-5

规格 价格 库存 购买数量
250mg 待询 待询
500mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

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产品描述

FR-167653 is a selective p38 MAPK inhibitor.

[1]. Hattori S, et al. FR-167653, a selective p38 MAPK inhibitor, exerts salutary effect on liver cirrhosis through downregulation of Runx2.

Chemical Properties

Cas No. 158876-66-5 SDF
别名 FR 167653 sulfate
Canonical SMILES O=C(N1NC2=C(C3=CC=NC=C3)C(C4=CC=C(F)C=C4)=NN2CC1)C(C5=CC=CC=C5)=O.O=S(O)(O)=O
分子式 C24H20FN5O6S 分子量 525.51
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.9029 mL 9.5146 mL 19.0291 mL
5 mM 0.3806 mL 1.9029 mL 3.8058 mL
10 mM 0.1903 mL 0.9515 mL 1.9029 mL
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Research Update

FR167653, a dual inhibitor of interleukin-1 and tumor necrosis factor-alpha, ameliorates endotoxin-induced shock

Eur J Pharmacol 1997 May 30;327(2-3):169-74.PMID:9200556DOI:10.1016/s0014-2999(97)89657-4.

Increased production of interleukin-1 and tumor necrosis factor-alpha (TNF-alpha) have been implicated in the pathophysiology of a variety of diseases including circulatory shock. The present study evaluated the efficacy of FR167653 (1-[7-(4-fluorophenyl)-1,2,3,4-tetrahydro-8-pyridylpyrazolo[5,1-c] [1,2,4]triazin-2-yl]-2-phenylethanedione sulfate monohydrate), a dual inhibitor of interleukin-1 and TNF-alpha production, to protect rabbits from the shock and lethality induced by lipopolysaccharide. In this sepsis model, FR167653 at a dose of 0.32 mg/kg per h ameliorated the 7-day mortality from 93% in the placebo group to 47% in the FR167653-treated group and, at doses of 0.10-0.32 mg/kg per h, attenuated the hypotensive response to lipopolysaccharide challenge and returned mean arterial blood pressure to almost normal levels. The increases in plasma interleukin-1 and TNF-alpha levels evoked by lipopolysaccharide administration were also inhibited by treatment with FR167653, which was efficacious at doses of 0.1-0.32 mg/kg per h. In addition, FR167653 treatment attenuated the increases in plasma creatinine concentrations consistent with renal damage in a dose-dependent manner. These findings suggested that FR 167653 has a beneficial potential as a drug for septic shock or multiple organ dysfunction syndrome.