Dehydronitrosonisoldipine (Synonyms: 尼索地平杂质3)
目录号: PL06601 纯度: ≥98%
CAS No. :87375-91-5
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中文名称
Dehydronitrosonisoldipine
英文名称
Dehydronitrosonisoldipine
英文别名
3,5-Pyridinedicarboxylic acid, 2,6-dimethyl-4-(2-nitrosophenyl)-, methyl2-methylpropyl ester;2,6-dimethyl-5-(3-methylbutan-2-yloxycarbonyl)-4-(2-nitrosophenyl)pyridine-3-carboxylate;2,6-Dimethyl-5-{[(3-methylbutan-2-yl)oxy]carbonyl}-4-(2-nitrosophenyl)pyridine-3-carboxylate
Cas No.
87375-91-5
分子式
C20H21N2O5
分子量
369.39
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
Dehydronitrosonisoldipine,是尼索地平 Nisoldipine (HY-17402) 的衍生物,是一种可逆且具有细胞渗透性的 SARM1 抑制剂。Dehydronitrosonisoldipine 主要通过阻断 SARM1 的激活而不是阻断其酶活性来发挥作用。Dehydronitrosonisoldipine 通过共价修饰半胱氨酸抑制 SARM1 和轴突退化 (AxD),也抑制 Vincristine 激活的神经元 cADPR 的产生。Dehydronitrosonisoldipine 可用于研究神经退行性疾病。
生物活性
Dehydronitrosonisoldipine, a derivative of Nisoldipine (HY-17402), is an irreversible and cell-permeant sterile alpha and TIR motif-containing 1 (SARM1) inhibitor. Dehydronitrosonisoldipine acts mainly by blocking SARM1 activation but not its enzymatic activities. Dehydronitrosonisoldipine inhibits SARM1 and axon degenration (AxD) by covalently modifying cysteines, also inhibits the Vincristine-activated cADPR production in neurons. Dehydronitrosonisoldipine can be used for researching neurodegenerative disorders.
性状
Solid
IC50 & Target[1][2]
SARM1, Calcium Channel
体外研究(In Vitro)
Dehydronitrosonisoldipine exhibits an IC50 of 4 μM in the SARM1-dN-expression cells, and decreases the cellular cADPR in cells expressing SARM1, but not in expressing SAM-TIR cells. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Li WH, et al. Permeant fluorescent probes visualize the activation of SARM1 and uncover an anti-neurodegenerative drug candidate. Elife. 2021 May 4;10:e67381.
[2]. Baranda AB, et al. Instability of calcium channel antagonists during sample preparation for LC-MS-MS analysis of serum samples. Forensic Sci Int. 2006 Jan 6;156(1):23-34.
溶解度数据
In Vitro: DMSO : 100 mg/mL (269.98 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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