Atorvastatin-hemicalcium-salt-CI-981-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAtorvastatin hemicalcium saltCat. No.: HY-17379CAS No.: 134523-03-8Synonyms: CI-981; Atorvastatin hemicalcium分式: CHCa.FNO分量: 577.67作靶点: HMG-CoA Reductase (HMGCR); Autophagy作通路: Metabolic Enzyme/Protease; Autophagy储存式: Powder -20

2、C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (86.55 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.7311 mL 8.6555 mL 17.3109 mL5 mM 0.3462 mL 1.7311 mL 3.4622 mL10 mM 0.1731 mL 0.8655 mL 1.7311 mL请根据产品在不同溶剂中的溶解度，选择合

3、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 (4.33 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubilit

4、y: 2.5 mg/mL (4.33 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Atorvastatin hemicalcium salt是有效的 HMG-CoA 还原酶抑制剂，IC50 值为 8 nM。IC50 & Target IC50: 8 nM (HMG-CoA)体外研究 Atorvastatin (0.03 to 1 M) inhibits FCS-induced SV-SMC proliferation and invasion 2. Ator

5、vastatinpromotes the expansion of myeloid-derived suppressor cells (MDSCs) in vitro. Atorvastatin-derived MDSCssuppressed T cell responses by NO production 3.体内研究 Atorvastatin (1-90 mg/kg, p.o.) reduces the mechanical inflammatory hypernociception induced by LPS in adose-dependent manner. Atorvastat

6、in (30 mg/kg, p.o.) shows Antinociceptive effect of atorvastatin ismediated by inhibition of HMG-CoA reductase 1. Atorvastatin promotes MDSCs accumulation in C57BL/6mice 3.PROTOCOLCell Assay 2 Briefly, SV-SMC from 5 different patients are seeded into 24-well cell culture plates at a density of1104 c

7、ells per well in full growth medium. Cells are incubated overnight and then quiesced in serum freemedium for 3 days before transfer to full growth medium (10% FCS) containing 5 different statins(simvastatin, atorvastatin, fluvastatin, lovastatin, and pravastatin)at a range of concentrations. All sta

8、tins aretested on cells from each individual patient. Medium and drugs are replaced after 2 days, and viable cellnumbers are determined in triplicate wells after 4 days using Trypan Blue and a hemocytometer. Theincrease in cell number is calculated by subtracting the starting cell number (day 0) fro

9、m the final cell number(day 4). Data are then normalized to control values (no statin) to correct for differences in proliferation ratesbetween cells from different patients.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal To investigate the effec

10、t of atorvastatin on lipopolysaccharide (LPS)-induced inflammatory hypernociception,Administration 1 mice are pretreated orally with either atorvastatin, at doses of 1, 3, 10, 30 and 90 mg/kg or vehicle (PBS)once a day for 3 consecutive days. At 2 h after the last dose of atorvastatin, mice receive

11、an i.pl. injection ofLPS (100 ng/paw) or saline (vehicle for LPS). The animals are also treated with atorvastatin (30 mg/kg) for 1or 2 days before LPS challenge. The hypernociceptive responses are assessed 0.5, 1, 3, 5, 7 and 24 h afterLPS or saline i.pl. injections.MCE has not independently confirm

12、ed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Endocrinology. 2018 May 1;159(5):2008-2021.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Santodomingo-Garzn T, et al. Atorvastatin inhibits inflammatory

13、hypernociception. Br J Pharmacol. 2006 Sep;149(1):14-22.2. Turner NA, et al. Comparison of the efficacies of five different statins on inhibition of human saphenous vein smooth muscle cellproliferation and invasion. J Cardiovasc Pharmacol. 2007 Oct;50(4):458-61.3. Lei A, et al. Atorvastatin promotes the expansion of myeloid-derived suppressor cells and attenuates murine colitis. Immunology. 2016Aug 22.Mc