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Derenofylline

Name: Derenofylline
Brand: TargetMol
SKU: T8312
Price: 170 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 98.09%

货号 T8312Cas号 251945-92-3

别名 地瑞茶碱

Derenofylline 是一个有选择性的、具有口服活性的腺苷A1受体的拮抗剂，可抑制心肌纤维化，降低蛋白尿，对腺苷A1、A3和A2A 受体的Ki 值分别为 1、200 和 398 nM。

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Derenofylline

一键复制产品信息

很棒

纯度: 98.09%

货号 T8312 别名 地瑞茶碱Cas号 251945-92-3

规格	价格	库存
1 mg	¥ 170	现货
5 mg	¥ 397	现货
10 mg	¥ 642	现货
25 mg	¥ 1,390	现货
50 mg	¥ 2,020	现货
100 mg	¥ 2,850	现货
200 mg	¥ 3,970	现货
1 mL x 10 mM (in DMSO)	¥ 437	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

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纯度: 98.09%

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COA LCMS HNMR 产品操作手册

产品介绍

Derenofylline AI Summary

Derenofylline exhibits broad-spectrum antiviral activity, including notable inhibition of Zika virus in human A549 cells with an IC50 of 58.6 nM. It demonstrates a dose-dependent cytotoxicity, showing low cytotoxicity at concentrations of 0.1 μM and 1 μM, but increased cytotoxicity at 10 μM and 100 μM. Against SARS-CoV-2, Derenofylline inhibits virus-induced cytotoxicity in Caco-2 cells by 6.39% at 10 μM after 48 hours, as measured by high content imaging. Furthermore, it partially inhibits the SARS-CoV-2 3CL-Pro protease with a 2.152% inhibition rate at 20 μM. The compound also shows a minor inhibitory effect on SARS-CoV-2 in VERO-6 cells with a 0.19% inhibition at 10 μM after 48 hours. In addition to its antiviral properties, Derenofylline is a potent antagonist of the human adenosine A1 receptor, displaying high binding affinity with Ki values ranging from 0.4 nM to 1.698 nM in different cell assays, and affecting forskolin-stimulated cAMP accumulation. It demonstrates a dissociation constant (Kd) of 5.46 nM, a low off-rate affinity with a rate constant (K) of 0.0034 /s, and high on-rate affinity with a rate constant (K) of 6.27 x 10^5 M/s. The compound also demonstrates mixed inhibition of human histone deacetylase 6 (HDAC6), showing -31.91% inhibition in an enzymatic assay using a commercial peptide substrate and 2.15% inhibition with a custom peptide substrate. This multifaceted bioactivity suggests potential therapeutic applications in viral infections and modulation of adenosine A1 receptor-related pathways..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Derenofylline is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM)
靶点活性	A2A receptor:398 nM (Ki), A1 receptor:1 nM(Ki), A3 receptor:200 nM (Ki)
别名	地瑞茶碱

化学信息

分子量	308.38
分子式	C₁₈H₂₀N₄O
CAS No.	251945-92-3
Smiles	O[C@H]1CC[C@@H](CC1)Nc1nc(nc2[nH]ccc12)-c1ccccc1
密度	1.37 g/cm3 (Predicted)

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 (72.96 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (16.21 mM), Sonication is recommended.

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	3.2428 mL	16.2138 mL	32.4275 mL	162.1376 mL
5 mM	0.6486 mL	3.2428 mL	6.4855 mL	32.4275 mL
10 mM	0.3243 mL	1.6214 mL	3.2428 mL	16.2138 mL
20 mM	0.1621 mL	0.8107 mL	1.6214 mL	8.1069 mL
50 mM	0.0649 mL	0.3243 mL	0.6486 mL	3.2428 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。