DC Chemicals Limited
China
Product Name: SKF-86002 dihydrochloride
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Cao

116339-68-5

116339-68-5 structure

Name: SKF 86002 dihydrochloride
Chemical Name: SKF 86002 dihydrochloride
CAS Number: 116339-68-5
Molecular Formula: C₁₆H₁₄Cl₂FN₃S
Molecular Weight: 370.272
Catalog: Signaling Pathways MAPK/ERK Pathway p38 MAPK
Create Date: 2019-09-07 20:04:16
Modify Date: 2024-01-16 09:38:45
SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid[1][2][3].

Name	SKF 86002 dihydrochloride
Synonyms	6-(4-Fluorophenyl)-5-(4-pyridinyl)-2,3-dihydroimidazo[2,1-b][1,3]thiazole dihydrochloride 6-(4-Fluorophenyl)-5-(pyridin-4-yl)-2,3-dihydroimidazo[2,1-b][1,3]thiazole dihydrochloride Imidazo[2,1-b]thiazole, 6-(4-fluorophenyl)-2,3-dihydro-5-(4-pyridinyl)-, hydrochloride (1:2)

Description	SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid[1][2][3].
Related Catalog	Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK Research Areas >> Inflammation/Immunology
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.
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.
References	[1]. Frasch SC, et al. p38 mitogen-activated protein kinase-dependent and -independent intracellular signal transduction pathways leading to apoptosis in human neutrophils. J Biol Chem. 1998 Apr 3;273(14):8389-97. [2]. Griswold DE, et al. SK&F 86002: a structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid. Biochem Pharmacol. 1987 Oct 15;36(20):3463-70. [3]. Lee JC, et al. A protein kinase involved in the regulation of inflammatory cytokine biosynthesis. Nature. 1994;372(6508):739-746. [4]. L A Marshall, et al. Inhibitors of the p38 mitogen-activated kinase modulate IL-4 induction of low affinity IgE receptor (CD23) in human monocytes. J Immunol. 1998 Dec 1;161(11):6005-13. [5]. M J DiMartino, et al. Pharmacologic characterization of the antiinflammatory properties of a new dual inhibitor of lipoxygenase and cyclooxygenase. Agents Actions. 1987 Feb;20(1-2):113-23.

Molecular Formula	C₁₆H₁₄Cl₂FN₃S
Molecular Weight	370.272
Exact Mass	369.026947
Appearance	powder
Storage condition	Store at -20°C
Water Solubility	Soluble to 50 mM in sterile water

Hazard Codes	Xi

116339-68-5	72873-74-6
68941-21-9	124796-27-6
40737-54-0	127729-35-5
99295-33-7	71636-62-9
40737-62-0	34148-20-4