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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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APX-115, also known as EWHA 18278,is a novel,potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury.APX-115 protects development of diabetic nephropathy in podocyte specific NOX5 transgenic mice. APX-115 might be a promising therapeutic agent for the treatment of DN because of its pan-NOX inhibitory activity, including its NOX5 inhibitory activity, and also owing to its anti-inflammatory effect.
| ln Vitro |
In high glucose-induced cell lines, the production of pro-inflammatory and fibrotic molecules is almost entirely inhibited by APX-115 free base (5 μM; 60 min) [2]. While enhancing factors and fibrotic processes, APX-115 free base in the kidney reduces Nox gene upregulation and protein expression [2].
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| ln Vivo |
Insulin resistance in diabetic mice can be markedly improved by APX-115 free base (oral gavage; 60 mg/kg/day; 12 weeks) [2]. Diabetic muscle signaling and urine protein excretion can both be decreased by APX-115 free base therapy.
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| Animal Protocol |
Animal/Disease Models: Sixweeks old male diabetic db/db mice (C57BLKS/J-leprdb/leprdb) [2]
Doses: 60 mg/kg Route of Administration: po (oral gavage); levels[2]. Daily; for 12 weeks Experimental Results: Dramatically improved insulin resistance in diabetic mice. |
| References |
[1]. Kwon G, et al. A novel pan-Nox inhibitor, APX-115, protects kidney injury in streptozotocin-induced diabetic mice: possible role of peroxisomal and mitochondrial biogenesis. Oncotarget. 2017 Jun 16;8(43):74217-74232.
[2]. Cha JJ, et al. APX-115, a first-in-class pan-NADPH oxidase (Nox) inhibitor, protects db/db mice from renal injury. Lab Invest. 2017 Apr;97(4):419-431. |
| Molecular Formula |
C17H17N3O
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|---|---|
| Molecular Weight |
279.343
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| Exact Mass |
279.1372
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| CAS # |
1270084-92-8
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| Related CAS # |
APX-115;1395946-75-4
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| SMILES |
OC1=C(CCC)C(C2=CC=CC=C2)=NN1C3=NC=CC=C3
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| InChi Key |
LQKQLKMTJOMCMJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17N3O/c1-2-8-14-16(13-9-4-3-5-10-13)19-20(17(14)21)15-11-6-7-12-18-15/h3-7,9-12,21H,2,8H2,1H3
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| Chemical Name |
3-phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol
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| Synonyms |
EWHA-18278 EWHA 18278 EWHA18278APX-115 free base APX 115 APX115
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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 : ~250 mg/mL (~894.97 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.45 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 (7.45 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 (7.45 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 | 3.5799 mL | 17.8993 mL | 35.7987 mL | |
| 5 mM | 0.7160 mL | 3.5799 mL | 7.1597 mL | |
| 10 mM | 0.3580 mL | 1.7899 mL | 3.5799 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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