Alagebrium-chloride-ALT711-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAlagebrium chlorideCat. No.: HY-106024BCAS No.: 341028-37-3Synonyms: ALT711分式: CHClNOS分量: 267.77作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 50 mg/mL (186.73 mM; Nee

2、d ultrasonic)DMSO : 25 mg/mL (93.36 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.7345 mL 18.6727 mL 37.3455 mL5 mM 0.7469 mL 3.7345 mL 7.4691 mL10 mM 0.3735 mL 1.8673 mL 3.7345 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。体内实验请根据您的实验动物和给药式选择适当的溶解案，

3、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 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.34 mM); Clear solution2. 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/

4、mL (9.34 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Alagebrium chloride种晚期糖基化终产物 (AGE) 抑制剂。IC50 & Target AGE 1体外研究 Alagebrium chloride is an advanced glycation end product (AGE) inhibitor. Endothelial cell (EC) proliferationis increased for all groups receiving Alagebrium (ALT-711), particularly when

5、 seeded on matrix from the AAoof obese (ZO) and diabetic (ZD) rats 2.体内研究 Blood pressure is not affected by treatment with Alagebrium. In diabetic RAGE apoE double-KO mice,treatment with Alagebrium is associated with a modest reduction in renal mass and reduces hyperfiltrationcompare with nontreated

6、 mice. Treatment with Alagebrium in diabetic RAGE apoE double-KO mice isassociated with a further reduction in glomerular collagen IV levels, approaching levels observed in controlmice 1. Body weight, heart rate (HR), and mean blood pressure (BP) are similar in Zucker lean (ZL), obese(ZO), and diabe

7、tic (ZD) groups in the absence or presence of Alagebrium (ALT-711). Alagebrium increasesblood flow (BF) in ZO rats but reduces distal vascular resistance in ZD rats. A decrease in neointimalhyperplasia (NH) intrastrut thickness as a function of local radius is found in all groups with Alagebriumtrea

8、tment. A significant increase in TGF- expression is also found in the AAo of ZL rats treated withAlagebrium 2.PROTOCOLCell Assay 2 Human aortic endothelial cells (HAECs) are seeded on decellularized matrices derived from the abdominalaorta (AAo) of Zucker lean (ZL), obese (ZO), and diabetic (ZD) rat

9、s with or without Alagebrium (ALT-711) (20g/mL in Dulbeccos PBS with 1 antibiotic-antimycotic). Experiments are performed when cells reach 80 to90% confluence. Flow chambers are sealed to the HAEC monolayers via a vacuum network. Flow is drivenby a Masterflex L/S peristaltic pump in a humidified cha

10、mber heated to 37C for 4 h. Leibovitz-15 medium,supplemented with 10% FBS, endothelial BulletKit, and 1 antibiotic-antimycotic solution, is used as the flowmedium to maintain pH in the absence of CO2 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Ani

11、mal RAGE apoE mice are randomized to be treated with Alagebrium (1 mg/kg/day by gavage), or no treatmentAdministration 1 (n=20/group). After 20 weeks of diabetes, mice are placed into individual metabolic cages for 24 h and urineis collected. Body weight as well as fluid and food intake are recorded

12、. Urinary albumin excretion is estimatedin urine samples by a mouse albumin enzyme-linked immunosorbent assay (ELISA) kit according to the kitprotocol. Urinary and serum creatinine concentrations are measured by high-performance liquidchromatography (HPLC). Systolic blood pressure is assessed by a n

13、oninvasive tail cuff method in consciousmice at the end of the study 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE户使本产品发表的科研献 Am J Transl Res. 2019 Mar 15;11(3):1569-1580.See more customer validation

14、s on HYPERLINK / www.MedChemEREFERENCES1. Watson AM, et al. Alagebrium reduces glomerular fibrogenesis and inflammation beyond preventing RAGEactivation in diabeticapolipoprotein E knockout mice. Diabetes. 2012 Aug;61(8):2105-13.2. Wang H, et al. Alagebrium inhibits neointimal hyperplasia and restores distributions of wall shear stress by reducing downstreamvascular resistance in obese and diabetic rats. Am J Physiol Heart Circ Physiol. 2015 Oct;