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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESDMACat. No.: HY-101410CAS No.: 30344-00-4Synonyms: Symmetric dimethylarginine; NG,NG-Dimethyl-L-arginine分式: CHNO分量: 202.25作靶点: Endogenous Metabolite作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C
2、 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (247.22 mM; ultrasonic and adjust pH to 3 with 1M HCl)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.9444 mL 24.7219 mL 49.4438 mL5 mM 0.9889 mL 4.9444 mL 9.8888 mL10 mM 0.4944 mL 2.4722 mL 4.9444 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。体内实验
3、请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (12.36 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (1
4、2.36 mM); Clear solution3. 请依序添加每种溶剂: 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (12.36 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY物活性 SDMA (Symmetric dimethylarginine)氧化氮 (NO) 合酶活性的内源性抑制剂。IC50 & Target Human Endogenous Metabolite体外研究
5、SDMA is the structural isomer of the cardiovascular risk marker asymmetric dimethylarginine, as anendogenous marker of renal function. SDMA does not directly inhibit NOS but is a competitor of argininetransport. SDMA is primarily eliminated by renal excretion and is a promising endogenous marker ofg
6、lomerular filtration rate 1. SDMA inhibits dose dependently the NO synthesis in intact endothelial cells,whereas it has no effect on protein expression of NOS 1. SDMA is involved in the inflammatory process ofchronic kidney disease, activating NF-B and resulting in enhanced expression of IL-6 and TN
7、F- 2.体内研究 SDMA is highly stable in serum and plasma, and the assay demonstrates excellent analytical performance.In unaffected dogs, SDMA remains unchanged whereas in affected dogs, SDMA increases during diseaseprogression, correlating strongly with an increase in sCr and decrease in GFR 3. Chronic
8、SDMA infusionleads to a significant increase of SDMA levels in mice, but the GFR did not change at 4 weeks. Nohistological changes are observed, particularly no effect on fibrosis or endothelias nitric oxide synthaseexpression. There is neither an effect of SDMA on systolic blood pressure nor on eje
9、ction fraction 4.PROTOCOLCell Assay 2 SDMA stock solution is prepared in 0.9% NaCl and diluted in the cell culture medium or in heparinized wholeblood resulting in a maximal uremic concentration of 6.1 M SDMA. Whole blood is incubated with saline(control) or different doses of ADMA (0.6, 3.6, and 36
10、 M) or SDMA (1.5, 3.1, and 6.1 M) for 2 hours in ahumidified atmosphere of 5% CO2 in air at 37C. Cells are finally stained for intracellular TNF- or IL-6.Samples are analyzed with a flow cytometer 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal
11、 Mice: Eight-week-old male C57Bl/6 mice receives vehicle-controlled infusion of SDMA (250 mol/kg/days) forAdministration 4 28 days using osmotic minipumps (n=24/group). Glomerular filtration rate, cardiac function and bloodpressure are monitored. Blood samples for SDMA determination are obtained at
12、baseline, 2 and 4 weeks.Mice are euthanized at 4 weeks to obtain tissue for renal histology 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Bode-B?ger SM,et al. Symmetrical dimethylarginine: a new combined parameter for renal function and
13、 extent ofcoronary artery disease.2. Schepers E, et al. Symmetric dimethylarginine as a proinflammatory agent in chronic kidney disease.Clin J Am Soc Nephrol. 2011Oct;6(10):2374-83.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. Nabity MB, et al. Symmetric Dimethylarginine Assay Validation, Stab
14、ility, and Evaluation as a Marker for the EarlyDetection of ChronicKidney Disease in Dogs. J Vet Intern Med. 2015 Jul-Aug;29(4):1036-44.4. Veldink H, et al. Effects of chronic SDMA infusion on glomerular filtration rate, blood pressure, myocardial function and renal histology inC57BL6/J mice. Nephrol Dial Transplant. 2013 Jun;28(
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