Efonidipine

Name: Efonidipine
Brand: TargetMol
SKU: T2323
Price: 169 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.47%

货号 T2323Cas号 111011-63-3

别名 依福地平, NZ-105, (±)-Efonidipine

Efonidipine (NZ-105) 是一种二氢吡啶类钙通道阻滞剂，可阻断 T 型和 L 型钙通道。

Efonidipine

一键复制产品信息

很棒

纯度: 99.47%

货号 T2323 别名 依福地平, NZ-105, (±)-EfonidipineCas号 111011-63-3

Efonidipine (NZ-105) 是一种二氢吡啶类钙通道阻滞剂，可阻断 T 型和 L 型钙通道。

规格	价格	库存
1 mg	¥ 169	现货
5 mg	¥ 372	现货
10 mg	¥ 596	现货
25 mg	¥ 1,130	现货
50 mg	¥ 1,730	现货
100 mg	¥ 2,920	现货
200 mg	¥ 4,230	现货
1 mL x 10 mM (in DMSO)	¥ 517	现货

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COA LCMS HNMR 产品操作手册

产品介绍

Efonidipine AI Summary

Efonidipine inhibits the Digoxin transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells with an IC50 of 13000.0 nM. It also inhibits Daunorubicin transepithelial transport in the same cells, showing IC50 values of 17300.0 nM and 20600.0 nM when tested with (-)-efonidipine and (+)-efonidipine, respectively. This compound demonstrates moderate potency against human tyrosyl-DNA phosphodiesterase 1 (TDP1), with potency values of 21136.0 nM and 29855.4 nM in the absence and presence of CPT, respectively. It further exhibits inhibitory activity against Lassa Virus and Marburg Virus binding or entry into cells with potency values of 22387.2 nM and 12589.3 nM, respectively. Efonidipine shows antiviral activity against SARS-CoV-2, inhibiting the induced cytotoxicity of Caco-2 cells and VERO-6 cells at a 10 µM concentration after a 48-hour exposure. It demonstrates a 9.96% inhibition rate of the SARS-CoV-2 3CL-Pro protease at 20 µM and an 18.0% inhibition rate of the SARS-CoV-2 main protease at a 100 µM concentration, with an IC50 value of 38500.0 nM for the main protease. Additionally, it exhibits a hit score of 0.1344 in antiviral activity assays against the SARS-CoV-2 (USA-WA1/2020 strain) in HRCE cells. Lastly, Efonidipine displays moderate inhibition of human HDAC6 enzyme activity with a commercial peptide substrate, showing a 5.26% inhibition rate, but demonstrates a slight negative inhibition of -2.05% with a custom peptide substrate, suggesting potential variability in bioactivity depending on the substrate used..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Efonidipine (NZ-105)(NZ-105) is a dihydropyridine calcium channel blocker, blocking both T-type and L-type calcium channels.
别名	依福地平, NZ-105, (±)-Efonidipine

化学信息

分子量	631.66
分子式	C₃₄H₃₈N₃O₇P
CAS No.	111011-63-3
Smiles	C(OCCN(CC1=CC=CC=C1)C2=CC=CC=C2)(=O)C=3C(C(=C(C)NC3C)P4(=O)OCC(C)(C)CO4)C5=CC(N(=O)=O)=CC=C5
密度	1.3g/cm3

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 22.5 mg/mL (35.62 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (3.17 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5831 mL	7.9157 mL	15.8313 mL	79.1565 mL
5 mM	0.3166 mL	1.5831 mL	3.1663 mL	15.8313 mL
10 mM	0.1583 mL	0.7916 mL	1.5831 mL	7.9157 mL
20 mM	0.0792 mL	0.3958 mL	0.7916 mL	3.9578 mL