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| 25mg |
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Purity: ≥98%
GSK2795039 is a novel and potent small molecule NADPH oxidase 2 inhibitor with a mean pIC50 of 6 in different cell-free assays.
| ln Vitro |
Reduces the presence of caspase-3-positive PC12 cells and the combined effect of FeSO4 and LPS on enhanced levels of apoptosis when GSK2795039 (25 μM; 24 hours) is administered [2].
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|---|---|
| ln Vivo |
GSK2795039 (ip; 100 mg/kg; one hour ago) lowers serum amylase levels brought on by systemic cerulein injection and decreases activity in a mouse model of acute pancreatitis [1].
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| Cell Assay |
Apoptosis analysis[2]
Cell Types: PC12 Cell Tested Concentrations: 25 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished apoptosis in PC12 cells. |
| Animal Protocol |
Animal/Disease Models: C57BL6 mice [1]
Doses: 100 mg/kg Route of Administration: intraperitoneal (ip) injection; 100 mg/kg; 1 hour before Experimental Results: Causes a 50% reduction in serum amylase activity levels. |
| References |
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| Molecular Formula |
C23H26N6O2S
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|---|---|
| Molecular Weight |
450.5565
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| Exact Mass |
450.183
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| Elemental Analysis |
C, 61.31; H, 5.82; N, 18.65; O, 7.10; S, 7.12
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| CAS # |
1415925-18-6
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| PubChem CID |
71090129
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| Appearance |
White to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
691.5±65.0 °C at 760 mmHg
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| Flash Point |
372.0±34.3 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.707
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
773
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C([H])=C([H])N(C([H])([H])[H])N=1)(N([H])C1C([H])=C([H])N=C2C=1C(=C([H])N2C([H])(C([H])([H])[H])C([H])([H])[H])C1C([H])=C([H])C2C([H])([H])C([H])([H])N(C([H])([H])[H])C=2C=1[H])(=O)=O
|
| InChi Key |
FMWVTCZKCXPKFW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H26N6O2S/c1-15(2)29-14-18(17-6-5-16-8-11-27(3)20(16)13-17)22-19(7-10-24-23(22)29)26-32(30,31)21-9-12-28(4)25-21/h5-7,9-10,12-15H,8,11H2,1-4H3,(H,24,26)
|
| Chemical Name |
N-(1-Isopropyl-3-(1-methylindolin-6-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-methyl-1H-pyrazole-3-sulfonamide
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| Synonyms |
GSK-2795039; GSK 2795039; GSK2795039
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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 |
| 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) |
DMSO : ~100 mg/mL (~221.95 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (22.19 mM) in 20% DMSO, 20% Tween 80, 60% polyethylene glycol 200 (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
Solubility in Formulation 2: 6.67 mg/mL (14.80 mM) in 15% Cremophor EL + 85% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.55 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. Solubility in Formulation 4: ≥ 2.5 mg/mL (5.55 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 corn oil and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2195 mL | 11.0973 mL | 22.1946 mL | |
| 5 mM | 0.4439 mL | 2.2195 mL | 4.4389 mL | |
| 10 mM | 0.2219 mL | 1.1097 mL | 2.2195 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.
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