APX-115-free-base-Ewha-18278-free-base-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAPX-115 free baseCat. No.: HY-120801ACAS No.: 1270084-92-8Synonyms: Ewha-18278 free base分式: CHNO分量: 279.34作靶點(diǎn): NADPH Oxidase作通路: Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)

2、據(jù)體外實(shí)驗(yàn) DMSO : 250 mg/mL (894.97 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.5799 mL 17.8993 mL 35.7987 mL5 mM 0.7160 mL 3.5799 mL 7.1597 mL10 mM 0.3580 mL 1.7899 mL 3.5799 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄的?chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)

3、果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (7.45 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (7.45 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% co

4、rn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (7.45 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 APX-115 free base (Ewha-18278 free base)種有效的，服活性的，選擇性 Nox 抑制劑，對Nox1，Nox2 和 Nox4 的 Ki 值分別為 1.08 M，0.57 M 和 0.63 M。APX-115 free base 可有效預(yù)防糖尿病的腎損傷。IC50 & Target Ki: 1.08 M (Nox1

5、), 0.57 M (Nox2) and 0.63 M (Nox4) 1體外研究 APX-115 free base (5M; 60min) almost completely suppresses high glucose-induced proinflammatory andprofibrotic molecule expression in the mouse podocyte cell line 2.In the kidney, APX-115 free base attenuates Nox gene upregulation and protein expression while

6、 improvinginflammatory and fibrotic processes 2.體內(nèi)研究 APX-115 free base (oral gavage; 60mg/kg/day; for 12 weeks) significantly improves insulin resistance indiabetic mice 2.APX-115 free base treatment decreases the urinary excretion of albumin and plasma creatinine levels 2.Animal Model: Six-week-old

7、 male diabetic db/db mice (C57BLKS/J-leprdb/leprdb) 2Dosage: 60mg/kgAdministration: Oral gavage; per day; for 12 weeksResult: Significantly improved insulin resistance in diabetic mice.REFERENCES1. Kwon G, et al. A novel pan-Nox inhibitor, APX-115, protects kidney injury in streptozotocin-induced di

8、abetic mice: possible role ofperoxisomal 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. 2017Apr;97(4):419-431.McePdfHeightCaution: Product has not been fully validated for medical applications.F