硝苯地平作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetNifedipineCat. No.: HY-B0284CAS No.: 21829-25-4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 : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL

2、 (288.74 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration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配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month

3、(protect from light)。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天 使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可 以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubili

4、ty: 2.5 mg/mL (7.22 mM); Clear solution此案可獲得 2.5 mg/mL (7.22 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。BIOLOGICAL ACTIVITYPage 1 of 2 www.MedChemE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。

5、體外研究 Nifedipine (BAY-a-1040) (100 M) significantly lowers the viability of the WKPT-0293 Cl.2 Cells, and treatment ofnifedipine (10 or 100 M) plus FAC induces a significant reduction in cell viability, but there are no significantdifferences in viability between the control cells and the cells treat

6、ed with 100 M of FAC or 1 and 10 M ofnifedipine.Nifedipine (BAY-a-1040) (1, 10, or 100 M) significantly increases iron level in WKPT-0293 Cl.2 cells.Nifedipine treatment also increases expression of TfR1, DMT1+IRE and DMT1-IRE in WKPT-0293 Cl.2 cells. Inaddition, co-treatment with nifedipine (100 M)

7、 and FAC (100 M) increases TfR1, DMT1+IRE and DMT1-IREexpression in WKPT-0293 Cl.2 cells2. Nifedipine plus ritodrine produces a significantly greater inhibition ofcontractility than each drug alone in the midrange of concentrations. The combination of nifedipine plusnitroglycerin or nifedipine plus

8、atosiban produces a significantly greater inhibition than nitroglycerin or atosibanalone but not greater than nifedipine. The combination of nifedipine plus NS-1619 (Ca2+-activated K+ BKCachannel opener) reduces the inhibitory effect of each drug3. Nifedipine (BAY-a-1040) (2 M) significantly inhibit

9、s P.capsici mycelial growth and sporulation. Nifedipine (BAY-a-1040)-induced inhibition of mycelial growth is calcium-dependent. Nifedipine (0.5 M) increases P. capsici sensitivity to H2O2 in a calcium-dependent manner. Nifedipineinhibition of P. capsici virulence and expression of genes involved in

10、 pathogenicity4.體內(nèi)研究 In Nifedipine (BAY-a-1040) (50 mg/kg)- and CsA-treated rats, the BL dimensions (BLi and BLk), MD dimensions(MDk) and vertical dimensions (VHi and VHk) are significantly increased (P 0.05) at the end of the 4th week1.PROTOCOLCell Assay 2 Cell viability is assessed using an MTT as

11、say. Briefly, a total of 25 L MTT (1 g/L in PBS) is added to each well beforeincubation is conducted at 37C for 4 h. The assay is stopped by the addition of a 100 L lysis buffer (20% SDS in 50%NNdimethylformamide, pH 4.7). Optical density (OD) is measured at the 570 nm wavelength by the use of an EL

12、X-800 microplate assay reader and the results are expressed as a percentage of the absorbance measured in the controlcells.MCE has not independently 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 ani

13、mals each. Group 1 (control) receive oliveAdministration 1 oil for the 8 weeks. Group 2 and Group 3 receive a combination of CsA (30 mg/kg body weight) and Nf (50 mg/kgbody weight) in olive oil for 8 weeks. In Group 3 rats, Azi (10 mg/kg body weight) is added to this regimen, in the 5thweek. The tot

14、al 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. 2019 Sep 12;62(17):7961-7975. Front Endocrinol (Lausanne). 2018 Nov 30;9:721. J Neurophysiol. 2019 Nov 13.See more customer validations on HYPERLINK www.M

15、edChemE www.MedChemEREFERENCES1. Ratre MS, et al. Effect of azithromycin on gingival overgrowth induced by cyclosporine A + nifedipine combination therapy: A morphometric analysis inPage 2 of 3 www.MedChemErats. J Indian Soc Periodontol. 2016 Jul-Aug;20(4):396-401.2. Yu SS, et al. Nifedipine Increas

16、es Iron Content in WKPT-0293 Cl.2 Cells via Up-Regulating Iron Influx Proteins. Front Pharmacol. 2017 Feb 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 Mi