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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESRI-011381 hydrochlorideCat. No.: HY-100347A分式: CHClNO分量: 365.94作靶点: TGF-beta/Smad作通路: Stem Cell/Wnt; 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 : 33.33 mg/mL (91.08 mM; Nee

2、d ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7327 mL 13.6634 mL 27.3269 mL5 mM 0.5465 mL 2.7327 mL 5.4654 mL10 mM 0.2733 mL 1.3663 mL 2.7327 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;澄的储备液可以根据储存条

3、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 (6.83 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 (6.83 mM); Clear solution3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.83 mM);

4、 Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 SRI-011381 hydrochloride有服物活性的 TGF-beta 信号通路的激活剂,具有神经保护作 1。IC50 & Target TGF-beta 1体外研究 SRI-011381 hydrochloride promotes fibrillar A clearance by macrophages, as demonstrated by the dose-dependent decreases of A

5、in the conditioned medium derived from compound-treated macrophages 1.SRI-011381 hydrochloride (10 M) eliminates Saikosaponin A (SSA, 30 M)-induced protective effects onfibroblasts 2.体内研究 SRI-011381 hydrochloride protects mice against kainic acid-induced excitotoxicity and neurodegeneration1.SRI-011

6、381 hydrochloride (10-75 mg/kg; p.o.; 14 days) results in significant changes in hematologicalendpoints, most notably reductions in red blood cells (RBCs), hematocrit and hemoglobin 1.SRI-011381 hydrochloride (30 mg/kg; i.p.) activates TGF- signaling in SBE-luciferase bioluminescentreporter mice 1.S

7、RI-011381 hydrochloride is rapidly absorbed after oral administration to FBV mice with an oralbioavailability of approximately 50% 1.SRI-011381 hydrochloride reduces neurodegeneratio in APP751Lon, Swetransgenic mice 1.Animal Model: FBV mice 1Dosage: 10 mg/kg, 30 mg/kg, 75 mg/kgAdministration: Oral a

8、dministration; 14 daysResult: Resulted in significant changes in hematological endpoints, most notably reductions inred blood cells (RBCs), hematocrit and hemoglobin户使本产品发表的科研献 Dev Comp Immunol. 2018 Nov;88:144-151. Exp Eye Res. 2019 Mar 23;182:44-56. Mol Cell Biochem. 2019 Jun;456(1-2):95-104. Drug

9、 Dev Res. 2019 Aug 12. Curr Med Sci. 2019 Aug;39(4):534-540.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Benzyl urea derivatives for activating tgf-beta signaling. US 20160039756 A1. 2016. Feb2. Liu Y, et al. Saikosaponin A Protects From Pressure Overload-Induced Cardiac Fibrosis via Inhibiting Fibroblast Activation or Endothelial2/3 Master of Small Molecules 您边的抑制剂师www.MedChemECell EndMT. Int J Biol Sci. 2018 Oct 31;14(13):1923-1934.McePdfHeightCaution: Product has not been fully validated f

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