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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENifedipineCat. No.: HY-B0284CAS No.: 21829-25-4Synonyms: BAY-a-1040分式: CHNO分量: 346.33作靶點(diǎn): Calcium Channel; Autophagy作通路: Membrane Transporter/Ion Channel; Neuronal Signaling;Autophagy儲(chǔ)存式: 4C, protect from light* In solvent : -80

2、C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 116.7 mg/mL (336.96 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.8874 mL 14.4371 mL 28.8742 mL5 mM 0.5775 mL 2.8874 mL 5.7748 mL10 mM 0.2887 mL 1.4437 mL 2.8874 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑

3、配制儲(chǔ)備液,并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Nifedipine (BAY-a-1040)有效的鈣離通道 (calcium channel) 阻滯劑,常于治療肌功能不全。體外研究Nifedipine (BAY-a-1040) (100 M) significantly lowers the viability of the WKPT-0293 Cl.2 Cells, andtreatment of nifedipine (10 or 100 M) plus FAC induces a significant reduction in cell via

4、bility, but there areno significant differences in viability between the control cells and the cells treated with 100 M of FAC or 11/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEand 10 M of nifedipine.Nifedipine (BAY-a-1040) (1, 10, or 100 M) significantly increases iron level inWKPT-0293 Cl.2 cel

5、ls. Nifedipine treatment also increases expression of TfR1, DMT1+IRE and DMT1-IRE inWKPT-0293 Cl.2 cells. In addition, co-treatment with nifedipine (100 M) and FAC (100 M) increases TfR1,DMT1+IRE and DMT1-IRE expression in WKPT-0293 Cl.2 cells 2. Nifedipine plus ritodrine produces asignificantly gre

6、ater inhibition of contractility than each drug alone in the midrange of concentrations. Thecombination of nifedipine plus nitroglycerin or nifedipine plus atosiban produces a significantly greaterinhibition than nitroglycerin or atosiban alone but not greater than nifedipine. The combination of nif

7、edipineplus NS-1619 (Ca2+-activated K+ BKCa channel opener) reduces the inhibitory effect of each drug 3.Nifedipine (BAY-a-1040) (2 M) significantly inhibits P. capsici mycelial growth and sporulation. Nifedipine(BAY-a-1040)-induced inhibition of mycelial growth is calcium-dependent. Nifedipine (0.5

8、 M) increases P.capsici sensitivity to H2O2 in a calcium-dependent manner. Nifedipine inhibition of P. capsici virulence andexpression of genes involved in pathogenicity 4.體內(nèi)研究 In Nifedipine (BAY-a-1040) (50 mg/kg)- and CsA-treated rats, the BL dimensions (BLi and BLk), MDdimensions (MDk) and vertic

9、al dimensions (VHi and VHk) are significantly increased (P 0.05) at the end ofthe 4th week 1.PROTOCOLCell Assay 2 Cell viability is assessed using an MTT assay. Briefly, a total of 25 L MTT (1 g/L in PBS) is added to eachwell before incubation is conducted at 37C for 4 h. The assay is stopped by the

10、 addition of a 100 L lysisbuffer (20% SDS in 50% NNdimethylformamide, pH 4.7). Optical density (OD) is measured at the 570 nmwavelength by the use of an ELX-800 microplate assay reader and the results are expressed as apercentage of the absorbance measured in the control cells.MCE has not independen

11、tly confirmed the accuracy of these methods. They are for reference only.Animal All the 30 rats are randomLy distributed into three equal groups of ten animals each. Group 1 (control)Administration 1 receive olive oil for the 8 weeks. Group 2 and Group 3 receive a combination of CsA (30 mg/kg body w

12、eight)and Nf (50 mg/kg body weight) in olive oil for 8 weeks. In Group 3 rats, Azi (10 mg/kg body weight) is addedto this regimen, in the 5th week. The total study period is 8 weeks.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Med Chem.

13、 2019 Aug. Front Endocrinol (Lausanne). 2018 Nov 30;9:721.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Ratre MS, et al. Effect of azithromycin on gingival overgrowth induced by cyclosporine A + nifedipine combination therapy: A2/3 Master of Small Molecules 您邊的抑制劑師www.MedChem

14、Emorphometric analysis in rats. J Indian Soc Periodontol. 2016 Jul-Aug;20(4):396-401.2. Yu SS, et al. Nifedipine Increases Iron Content in WKPT-0293 Cl.2 Cells via Up-Regulating Iron Influx Proteins. Front Pharmacol. 2017Feb 13;8:603. Carvajal JA, et al. The Synergic In Vitro Tocolytic Effect of Nifedipine Plus Ritodrine on Human Myometrial Contractility. Reprod Sci.2017 Apr;24(4):635-640.4. Liu P, et al. The L-type Ca(2+) Channel Blocker Nifedipine Inhibits Mycelial Growth, Sporulation, and Virulence of Phytophthora capsici.Front Microbio

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