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SKF 86002 dihydrochloride

CAS# 116339-68-5

SKF 86002 dihydrochloride

Catalog No. BCC7236----Order now to get a substantial discount!

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SKF 86002 dihydrochloride: 5mg $104 In Stock
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Chemical structure

SKF 86002 dihydrochloride

3D structure

Chemical Properties of SKF 86002 dihydrochloride

Cas No. 116339-68-5 SDF Download SDF
PubChem ID 10339107 Appearance Powder
Formula C16H14Cl2FN3S M.Wt 370.27
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in water
Chemical Name 6-(4-fluorophenyl)-5-pyridin-4-yl-2,3-dihydroimidazo[2,1-b][1,3]thiazole;dihydrochloride
SMILES C1CSC2=NC(=C(N21)C3=CC=NC=C3)C4=CC=C(C=C4)F.Cl.Cl
Standard InChIKey GQQCNUNCYVXBTF-UHFFFAOYSA-N
Standard InChI InChI=1S/C16H12FN3S.2ClH/c17-13-3-1-11(2-4-13)14-15(12-5-7-18-8-6-12)20-9-10-21-16(20)19-14;;/h1-8H,9-10H2;2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SKF 86002 dihydrochloride

DescriptionInhibitor of p38 MAP kinase (IC50 = 0.1 - 1 μM). Potently inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM). Also inhibits 5-lipoxygenase- and cyclooxygenase-mediated arachidonic acid metabolism in RBL-1 cells (IC50 values are 10 and 100 μM respectively). Anti-inflammatory following oral administration in vivo.

SKF 86002 dihydrochloride Dilution Calculator

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SKF 86002 dihydrochloride Molarity Calculator

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Preparing Stock Solutions of SKF 86002 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.7007 mL 13.5037 mL 27.0073 mL 54.0146 mL 67.5183 mL
5 mM 0.5401 mL 2.7007 mL 5.4015 mL 10.8029 mL 13.5037 mL
10 mM 0.2701 mL 1.3504 mL 2.7007 mL 5.4015 mL 6.7518 mL
50 mM 0.054 mL 0.2701 mL 0.5401 mL 1.0803 mL 1.3504 mL
100 mM 0.027 mL 0.135 mL 0.2701 mL 0.5401 mL 0.6752 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on SKF 86002 dihydrochloride

Common and distinct intracellular signaling pathways in human neutrophils utilized by platelet activating factor and FMLP.[Pubmed:9062356]

J Clin Invest. 1997 Mar 1;99(5):975-86.

Stimulation of human neutrophils with chemoattractants FMLP or platelet activating factor (PAF) results in different but overlapping functional responses. We questioned whether these differences might reflect patterns of intracellular signal transduction. Stimulation with either PAF or FMLP resulted in equivalent phosphorylation and activation of the mitogen-activated protein kinase (MAPk) homologue 38-kD murine MAP kinase homologous to HOG-1 (p38) MAPk. Neither FMLP nor PAF activated c-jun NH2-terminal MAPk (JNKs). Under identical conditions, FMLP but not PAF, resulted in significant p42/44 (ERK) MAPk activation. Both FMLP and PAF activated MAP kinase kinase-3 (MKK3), a known activator of p38 MAPk. Both MAP ERK kinase kinase-1 (MEKK1) and Raf are activated strongly by FMLP, but minimally by PAF. Pertussis toxin blocked FMLP-induced activation of the p42/44 (ERK) MAPk cascade, but not that of p38 MAPk. A specific p38 MAPk inhibitor (SK&F 86002) blocked superoxide anion production in response to FMLP and reduced adhesion and chemotaxis in response to PAF or FMLP. These results demonstrate distinct patterns of intracellular signaling for two chemoattractants and suggest that selective activation of intracellular signaling cascades may underlie different patterns of functional responses.

A protein kinase involved in the regulation of inflammatory cytokine biosynthesis.[Pubmed:7997261]

Nature. 1994 Dec 22-29;372(6508):739-46.

Production of interleukin-1 and tumour necrosis factor from stimulated human monocytes is inhibited by a new series of pyridinyl-imidazole compounds. Using radiolabelled and radio-photoaffinity-labelled chemical probes, the target of these compounds was identified as a pair of closely related mitogen-activated protein kinase homologues, termed CSBPs. Binding of the pyridinyl-imidazole compounds inhibited CSBP kinase activity and could be directly correlated with their ability to inhibit cytokine production, suggesting that the CSBPs are critical for cytokine production.

SK&F 86002: a structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.[Pubmed:2823821]

Biochem Pharmacol. 1987 Oct 15;36(20):3463-70.

The effects of SK&F 86002 [5-(4-pyridyl)-6 (4-fluorophenyl)-2,3-dihydroimidazo (2,1-b) thiazole] on the generation of eicosanoids in vitro and on inflammatory responses in vivo are described and compared to other non-steroidal anti-inflammatory drugs. SK&F 86002 inhibited prostaglandin H2 (PGH2) synthase activity (IC50 120 microM) as well as prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50 70 microM) and its sonicate (IC50 100 microM) and human monocytes (IC50 1 microM). In addition, SK&F 86002 inhibited the generation of dihydroxyeicosatetraenoic acid (diHETE) and 5-hydroxyeicosatetraenoic acid (5-HETE) by a high speed supernatant fraction of RBL-1 cells (IC50 10 microM). Cellular production of 5-lipoxygenase products was inhibited by SK&F 86002 as measured by leukotriene B4 (LTB4) generation from human neutrophils (IC50 20 microM), leukotriene C4 (LTC4) generation by human monocytes (IC50 20 microM), and 5-HETE production by RBL-1 cells (IC50 40 microM). The in vivo profile of anti-inflammatory activity of SK&F 86002 supports the dual inhibition of arachidonate metabolism as indicated by its activity in inflammation models that are insensitive to selective cyclooxygenase inhibitors. The responses of arachidonic-acid-induced edema in the mouse ear and rat paw, as well as the cell infiltration induced by carrageenan in the mouse peritoneum and by arachidonic acid in the rat air pouch, were inhibited by SK&F 86002 and phenidone but not by the selective cyclooxygenase inhibitors naproxen and indomethacin.

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