SB-525334 - ALK5 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESB 525334Cat. No.: HY-12043CAS No.: 356559-20-1分式: CHN分量: 343.42作靶点: TGF- Receptor作通路: TGF-beta/Smad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 DMSO : 46 mg/mL (133.95 mM)* means soluble, but

2、saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9119 mL 14.5594 mL 29.1189 mL5 mM 0.5824 mL 2.9119 mL 5.8238 mL10 mM 0.2912 mL 1.4559 mL 2.9119 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，配制前请先配制澄的储备液，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；澄的储备液可以

3、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: 10 mg/mL (29.12 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 10 mg/mL (29.12 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecul

4、es 您边的抑制剂师www.MedChemESolubility: 10 mg/mL (29.12 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 SB 525334种有效，选择性的转化长因1受体 (ALK5) 抑制剂，IC50 为 14.3 nM。IC50 & Target IC50: 14.3 nM (ALK5) 1体外研究 SB525334 (1 M; for 15 minutes before stimulating with 0.625 ng/ml of TGF-1, assesses after 6 days)inhibits TGF-1-med

5、iated proliferation of familial idiopathic pulmonary arterial hypertension (iPAH) pulmonaryartery smooth muscle cells (PASMCs) at an IC50 of 295 nM 2.Cell Proliferation Assay 2Cell Line: PASMC cellsConcentration: 1 MIncubation Time: Pre-incubated for 15 minutes (before stimulating with 0.625 ng/ml o

6、f TGF-1), assessedafter 6 daysResult: Inhibited TGF-1-mediated proliferation of familial iPAH PASMCs at an IC50 of 295 nM.体内研究 SB525334 (3-30 mg/kg; p.o.; daily from days 17 to 35) significantly reverses pulmonary arterial pressure in arat model of pulmonary arterial hypertension (PAH) 2.Animal Mode

7、l: Adult male Sprague-Dawley rats (MCT rat model of pulmonary hypertension) 2Dosage: 3, 30 mg/kgAdministration: Oral administration; daily from days 17 to 35Result: Reduced the proportion of fully muscularized vessels to 28% at 3 mg/kg and returnedfully muscularized vessel distribution beyond that s

8、een at day 17 and approaching thephenotype observed in saline-exposed controls at 30 mg/kg.户使本产品发表的科研献 Glia. 2014 Feb;62(2):185-98. Cell Commun Signal. 2018 Dec 7;16(1):97. Biochim Biophys Acta. 2017 Dec 18;1864(3):721-734. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLI

9、NK / www.MedChemE2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEREFERENCES1. Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase inpuromycin-induced nephritis. J Pharmacol Exp Ther, 2005, 313(3), 943-951.2. Th

10、omas M, et al. ALK5 mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterialhypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrotaline. Am J Pathol,2009, 174(2), 380-389.3. Laping NJ, et al. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. Clin Cancer Res, 2007, 13(10),3087-3899.McePdfHeightCaution: Product has not been ful