Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
SKF-86002 is a novel and potent inhibitor of the p38 MAP kinase with IC50 of 0.5-1 uM; it inhibits LPS-induced IL-1 and TNF-α production in human monocytes with IC50 of 1 μM. The production of dihydroxyeicosatetraenoic acid (diHETE) and 5-hydroxyeicosatetraenoic acid (5-HETE) by a high speed supernatant fraction of RBL-1 cells was inhibited by SKF-86002 (IC50 10 μM). In response to FMLP, SKF-86002 prevented the production of superoxide anion, and in response to PAF or FMLP, it decreased adhesion and chemotaxis. The dual inhibition of arachidonate metabolism is supported by the in vivo profile of SK&F 86002's anti-inflammatory activity, which is demonstrated by the drug's effectiveness in inflammation models that are resistant to selective cyclooxygenase inhibitors.
Targets |
p38 MAPK; TNF-α; IL-1 (IC50 = 1 μM)
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ln Vitro |
The effects of the non-steroidal anti-inflammatory drug SK&F 86002 [5-(4-pyridyl)-6 (4-fluorophenyl)-2,3-dihydroimidazo (2,1-b) thiazole] on the production of eicosanoids in vitro and on inflammatory responses in vivo are described.
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ln Vivo |
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Enzyme Assay |
Prostaglandin H2 (PGH2) synthase activity, prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50 70 microM), the sonicate of these cells (IC50 100 microM), and human monocytes (IC50 1 microM) were all inhibited by SK&F 86002 (IC50 120 microM). A high speed supernatant fraction of RBL-1 cells produced dihydroxyeicosatetraenoic acid (diHETE) and 5-hydroxyeicosatetraenoic acid (5-HETE), which were both inhibited by SK&F 86002 (IC50 10 microM).
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Cell Assay |
Leukotriene B4 (LTB4) generation from human neutrophils (IC50 20 microM), leukotriene C4 (LTC4) generation from human monocytes (IC50 20 microM), and 5-HETE production from RBL-1 cells (IC50 40 microM) were used to determine the effectiveness of SK&F 86002 in reducing cellular production of 5-lipoxygenase products. By acting in inflammation models that are resistant to selective cyclooxygenase inhibitors, SK&F 86002's in vivo profile of anti-inflammatory activity supports the dual inhibition of arachidonate metabolism. SK&F 86002 and phenidone inhibited the effects of arachidonic acid-induced edema in the mouse ear and rat paw, as well as cell infiltration brought on by carrageenan in the mouse peritoneum and by arachidonic acid in the rat air pouch, but not the selective cyclooxygenase inhibitors naproxen and indomethacin.
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Animal Protocol |
Lewis rats, with adjuvant-induced arthritis (AA)[5]
10 mg/kg, 30 mg/kg, 90 mg/kg Oral administration, daily, for 22 days |
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References |
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Molecular Formula |
C16H12FN3S
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Molecular Weight |
297.35
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Exact Mass |
297.07
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Elemental Analysis |
C, 64.63; H, 4.07; F, 6.39; N, 14.13; S, 10.78
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CAS # |
72873-74-6
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Related CAS # |
SKF-86002 dihydrochloride;116339-68-5
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Appearance |
Solid powder
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SMILES |
C1CSC2=NC(=C(N21)C3=CC=NC=C3)C4=CC=C(C=C4)F
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InChi Key |
YOELZIQOLWZLQC-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C16H12FN3S/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
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Chemical Name |
6-(4-fluorophenyl)-5-pyridin-4-yl-2,3-dihydroimidazo[2,1-b][1,3]thiazole
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3630 mL | 16.8152 mL | 33.6304 mL | |
5 mM | 0.6726 mL | 3.3630 mL | 6.7261 mL | |
10 mM | 0.3363 mL | 1.6815 mL | 3.3630 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
MEK1 inhibitor did not inhibit apoptosis.J Biol Chem.1998 Apr 3;273(14):8389-97. th> |
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HL-60 cells decreased JNK activation and acquired p38 as they became neutrophil-like.J Biol Chem.1998 Apr 3;273(14):8389-97. td> |
SK & F 86002 did not inhibit UV-induced apoptosis in undifferentiated HL-60 cells.J Biol Chem.1998 Apr 3;273(14):8389-97. td> |