SKF-86002 dihydrochloride

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CAS NO:

116339-68-5

SKF-86002 dihydrochloride 是一种具有口服活性的p38 MAPK抑制剂，具有抗炎、抗关节炎活性，可用于缓解疼痛的研究。SKF-86002 dihydrochloride 抑制脂多糖 (LPS) 刺激人单核细胞产生 IL-1 和 TNF-α。SKF-86002 dihydrochloride 能抑制脂氧合酶和环氧合酶介导的花生四烯酸代谢。

生物活性

SKF-86002 dihydrochloride is an orally activep38 MAPKinhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyteIL-1and TNF-α production (IC₅₀= 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid^[1]^[2]^[3].

体外研究
(In Vitro)

SKF-86002 dihydrochloride (10 μM; 1 hour) inhibits apoptosis induced by stress stimulation with UV irradiation (UV)^[1].
SKF-86002 dihydrochloride does not inhibit UV-induced apoptosis in undifferentiated HL-60 cells^[1].
SKF-86002 dihydrochloride (10 μM; 72 hours) prevent IL-4-induced monocyte or U937 cell CD23 surface expression and protein formation with no effect on CD23 mRNA levels^[4].

Western Blot Analysis^[4]

Cell Line:	U937 cells
Concentration:	10 μM
Incubation Time:	72 hours
Result:	Reduced CD23 levels on IL-4-treated U937 cells.

体内研究
(In Vivo)

SKF-86002 dihydrochloride (10-90 mg/kg; p.o.; daily; for 22 days) has antiarthritic activity^[5].

Animal Model:	Lewis rats, with adjuvant-induced arthritis (AA)^[5]
Dosage:	10 mg/kg, 30 mg/kg, 90 mg/kg
Administration:	Oral administration, daily, for 22 days
Result:	Significantly decreased hindleg volumes after injection of adjuvant.

分子量

370.27

Formula

C₁₆H₁₄Cl₂FN₃S

CAS 号

116339-68-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.