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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%
Dilmapimod (SB-681323; GW-681323) is a novel p38 MAPK (mitogen-activated protein kinase) inhibitor that may be used to treat inflammatory conditions like COPD and RA. Prednisolone and SB-681323 both inhibited the p38 MAPK pathway, but the former did so more effectively. The production of TNF-alpha was suppressed by SB-681323. SB-681323 is a potent p38 MAPK inhibitor that may reduce inflammation in COPD.
Targets |
p38 MAPK
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ln Vitro |
Dilmapimod (SB-681323) potently inhibits p38 MAPK signaling, measured by inhibition of sorbitol-induced pHSP27 expression[1].
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References |
Molecular Formula |
C23H19F3N4O3
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Molecular Weight |
456.42
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Exact Mass |
456.14
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Elemental Analysis |
C, 60.52; H, 4.20; F, 12.49; N, 12.28; O, 10.52
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CAS # |
444606-18-2
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Related CAS # |
937169-00-1;444606-18-2;
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Appearance |
Solid powder
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SMILES |
CC1=C(C=CC(=C1)F)C2=C3C=CC(=O)N(C3=NC(=N2)NC(CO)CO)C4=C(C=CC=C4F)F
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InChi Key |
ORVNHOYNEHYKJG-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C23H19F3N4O3/c1-12-9-13(24)5-6-15(12)20-16-7-8-19(33)30(21-17(25)3-2-4-18(21)26)22(16)29-23(28-20)27-14(10-31)11-32/h2-9,14,31-32H,10-11H2,1H3,(H,27,28,29)
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Chemical Name |
8-(2,6-difluorophenyl)-2-(1,3-dihydroxypropan-2-ylamino)-4-(4-fluoro-2-methylphenyl)pyrido[2,3-d]pyrimidin-7-one
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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: ≥ 2.08 mg/mL (4.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.56 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1910 mL | 10.9548 mL | 21.9096 mL | |
5 mM | 0.4382 mL | 2.1910 mL | 4.3819 mL | |
10 mM | 0.2191 mL | 1.0955 mL | 2.1910 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00134693 | Completed | Drug: Prednisolone Drug: SB-681323 |
Arthritis, Rheumatoid | GlaxoSmithKline | June 21, 2005 | Phase 2 |
NCT00439881 | Completed | Drug: SB-681323 | Arthritis, Rheumatoid Inflammation |
GlaxoSmithKline | October 2006 | Phase 1 |
NCT00320450 | Completed | Drug: SB-681323 | Arthritis, Rheumatoid | GlaxoSmithKline | November 2005 | Phase 2 |
NCT00390845 | Completed | Drug: SB-681323 Drug: Placebo |
Pain, Neuropathic | GlaxoSmithKline | August 30, 2006 | Phase 2 |
NCT00291902 | Completed | Drug: SB-681323 | Coronary Heart Disease | GlaxoSmithKline | March 2006 | Phase 2 |