Tetrandrine-NSC-77037-d-Tetrandrine-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETetrandrineCat. No.: HY-13764CAS No.: 518-34-3Synonyms: NSC-77037；d-Tetrandrine分式: CHNO分量: 622.75作靶點: Calcium Channel; Potassium Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsI

2、n solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 5 mg/mL (8.03 mM; Need ultrasonic and warming)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 0.5 mg/mL (0.80 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.5 mg/mL (0.80 mM); Clear solution1/3 Master of Small

3、Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 0.5 mg/mL (0.80 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Tetrandrine (NSC-77037)種雙苯 異喹啉物堿，抑制電壓門控鈣離通道 (ICa) 和 Ca2+ 激活的鉀離通道。IC50 & Target Ca2+ current 1K+ current 1體外研究 The effects of Tetrandrine (NSC-77037), a bis-benzyl-iso

4、quinoline alkaloid, on voltage-gated Ca2+ currents(ICa) and on Ca2+-activated K+ current (IK(Ca) and channels in isolated nerve terminals of the ratneurohypophysis are investigated using patch-clamp techniques. The non-inactivating component of ICa isinhibited by external Tetrandrine (NSC-77037) in

5、a voltage- and dose-dependent manner, with an IC50=10.1M. Tetrandrine (NSC-77037) decreases the channel-open probability, within bursts, with an IC50=0.21 M1. To evaluate the effects of Tetrandrine on HCC cells, Huh7, HCCLM9 and Hep3B cells are treated with 0(DMSO), 0.5, 1, 2 or 4 M of Tetrandrine f

6、or 24 h. The cell proliferation assay indicates that Tetrandrineexhibits almost no effect on the inhibition of HCC cell proliferation at 0.5-2 M. However, Tetrandrine (NSC-77037) inhibits HCC cell migration in a dose-dependent manner. Furthermore, a wound-healing and transwellassay shows that 2 M Te

7、trandrine significantly inhibits HCC cell migration and invasion 2.體內(nèi)研究 To evaluate the effect of Tetrandrine (NSC-77037) on the inhibition of tumor metastasis in vivo, HCCLM9subcutaneous tumor xenograft models is established with athymic nude mice. When the tumor volume reachapproximately 50 mm3, n

8、ude mice are orally administered vehicle or Tetrandrine (NSC-77037) (30 mg/kg)every other day for 37 days. Tetrandrine (NSC-77037) treatment inhibits tumor growth by reducing the tumorvolume and weight 2.PROTOCOLCell Assay 2 Huh7, HCCLM9 and Hep3B cells are seeded in a 96-well plate at a cell densit

9、y of 5103 cells/well. The cellsare treated with the indicated concentrations (0-4 M) of Tetrandrine (NSC-77037) for 24 h. The cells aresubsequently stained with 20 L of MTS for 1-2 h, and the plates are read at 490 nm on a BioTek ELx800 2.MCE has not independently confirmed the accuracy of these met

10、hods. They are for reference only.Animal Mice 2 Four-week-old male athymic BALB/c nu/nu SPF mice (body weight range from 18 g to 20 g) areAdministration 2 used. HCCLM9 WT and HCCLM9 ATG7 KO cells (5 million) resuspended in 0.2 mL of PBS aresubcutaneously implanted into the right flank of each mouse.

11、 When the tumor volume reach approximately50 mm3, the tumor-bearing mice are randomly divided into control and treatment groups (n=6). The controland treatment groups are administered oral injection of vehicle (0.5% methylcellulose) and Tetrandrine at 30mg/kg of body weight every other day for 37 da

12、ys. During the treatment, the tumor volumes are measuredevery day and are calculated.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Wang G, et al. Tetrandrine blocks a slow, large-conductanc

13、e, Ca(2+)-activated potassium channel besides inhibiting a non-inactivatingCa2+ current in isolated nerve terminals of the rat neurohypophysis. Pflugers Arch. 1992 Sep;421(6):558-65.2. Zhang Z, et al. The plant alkaloid tetrandrine inhibits metastasis via autophagy-dependent Wnt/-catenin and metastatic tumor antigen 1signaling in human liver cancer cells. J Exp Clin Cancer Res. 2018 Jan 15;37(1):7.Mc