| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
NOX1 NOX4
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|---|---|
| ln Vitro |
The increase in O2 caused by high d-glucose is significantly reduced by GKT136901 hydrochloride (10 μM; 30 min).- generation as well as H2O2 generation in MPT cells [4]. In MPT cells, the effects of high D-glucose on p38MAP kinase activation are eliminated by GKT136901 hydrochloride (10 μM; 30 min) [4]. In HBMEC, GKT136901 hydrochloride (10 μM; 2 hours) reduces oxidative stress caused by methamphetamine (METH) [5]. HBMEC is protected from METH-induced blood-brain barrier (BBB) dysfunction by GKT136901 hydrochloride (10 μM; 2 hours) [5].
|
| ln Vivo |
In a mouse model of type 2 diabetes, GKT136901 hydrochloride (30-90 mg/kg; administered orally daily for 16 weeks) has renoprotective properties[6].
|
| Animal Protocol |
Animal/Disease Models: Male db/db and db/m mice (8 weeks)[6]
Doses: 30, 90 mg/kg Route of Administration: Daily po for 16 weeks Experimental Results: decreased albuminuria, thiobarbituric acid-reacting substances (TBARS) and renal ERK1 /2 phosphorylation and preserved renal structure in diabetic mice. Had no effect on plasma glucose, BP (blood pressure), and body weight. |
| References |
|
| Molecular Formula |
C19H20CL2N4O2
|
|---|---|
| Molecular Weight |
407.2937
|
| CAS # |
1254507-01-1
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| Related CAS # |
GKT136901;955272-06-7
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| PubChem CID |
155977664
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| Appearance |
Light yellow to light brown solid powder
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
27
|
| Complexity |
675
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1=C([H])C([H])=C([H])C([H])=C1N1C(C2([H])C([H])(C([H])([H])[H])N(C([H])([H])C3=C([H])C([H])=C([H])C([H])=N3)C(C([H])([H])C2([H])N1[H])=O)=O.Cl[H]
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 62.5 mg/mL (154.99 mM)
H2O: 4 mg/mL (9.92 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.16 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 (5.16 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4553 mL | 12.2763 mL | 24.5525 mL | |
| 5 mM | 0.4911 mL | 2.4553 mL | 4.9105 mL | |
| 10 mM | 0.2455 mL | 1.2276 mL | 2.4553 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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