Carglumic-Acid-N-Carbamyl-L-glutamic-acid-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECarglumic AcidCat. No.: HY-B0711CAS No.: 1188-38-1Synonyms: N-Carbamyl-L-glutamic acid分式: CHNO分量: 190.15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 : 3 mg/mL (15.78 m

2、M; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 5.2590 mL 26.2950 mL 52.5901 mL5 mM 1.0518 mL 5.2590 mL 10.5180 mL10 mM 0.5259 mL 2.6295 mL 5.2590 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。BIOLOGICAL ACTIVITY物活性 Carglumic acid (N-Carbamyl-L-glutamic acid)N-酰氨酸 (

3、NAG) 的功能类似物和氨甲酰磷酸合成酶 1 (CPS1) 的活化剂，于治疗与 N-酰氨酸合成酶 (NAGS) 缺陷相关的急性和慢性氨症。IC50 & Target CPS1 1体外研究Carglumic acid suppresses cell viability in the pancreatic ductal adenocarcinoma cell lines, triple-negative1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEbreast cancer cell lines, hepatoma cell lines, and

4、 human non-small cell lung carcinoma cell lines in a dose-dependent manner. The 50% inhibitory concentration (IC50) of Carglumic acid against those cell lines isbetween 5 and 7.5 mM. The results show that Carglumic acid does not induce complete cell cycle arrest.Instead, there are more sub-G1 cells

5、among Carglumic acid-treated AsPC1 and MDA-MB-231 cells thanamong untreated cells. In AsPC1 and HPDE-E6E7 cells, the IC50s of Carglumic acid are 5 mM and over 10mM, respectively . In MDA-MB-231 and MCF-12A cells, the IC50s of Carglumic acid are 5 mM and 6 mM,respectively 1.体内研究 The results show that

6、 Carglumic acid, but not the vehicle control, markedly inhibits tumor growth. In theorthotopic pancreatic cancer model, tumor growth inhibition by Carglumic acid on day 21 is 80% (P 1.PROTOCOLKinase Assay 1 Caspase activity is measured by using a fluorimetric caspase-3 assay kit. In brief, cells tha

7、t are treated withCarglumic Acid or that are left untreated are lysed in a lysis buffer, and 50 g of protein lysate is incubatedwith Ac-DEVD-AMC substrate in the assay buffer for 1 h. The resultant fluorescence signals are read byusing a fluorometer (excitation 360 nm, emission 460 nm), and the resu

8、lts are tabulated as fold changesrelative to the untreated control cells 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 Cell viability is evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Inbrief, var

9、ious cancer cell lines are seeded (1104 cells/well) in a 96-well plate and treated with differentdoses of Carglumic Acid. After 48 h, 50 L of MTT solution per well (stock solution concentration 5 mg/mL) isadded to each well, and the cells are incubated for 2 h more, followed by addition of 100 L of

10、dimethylsulfoxide to each well. Absorbance at 570 nm is measured immediately using a multiwell scanner 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal For orthotopic cancer models, AsPC1/luc human pancreatic cancer cells (1106) are injected int

11、o theAdministration 1 pancreas of nude mice or MDA-MB-231 human triple-negative breast cancer cells (3106) are injected intothe mammary fat pad of nude mice. Carglumic acid is administered to mice 5 days after tumor inoculation inthe pancreatic cancer model and 7 days after tumor inoculation in the

12、triple-negative breast cancer model.Tumor-bearing mice receive a Carglumic acid dose of 120 mg/kg orally every day for 10 days, 60 mg/kgorally three times per week for 2 weeks, or 60 mg/kg intravenously three times per week for 2 weeks. Tumorvolume is determined by measuring luciferase signals using

13、 the in vivo imaging system in the pancreaticcancer model 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chen CT, et al. Carglumic acid promotes apoptosis and suppresses cancer cell proliferation in vitro and in vivo. Am J Cancer Res. 2015Nov 15;5(12):3560-9.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www