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N,N,2-三甲基-5-硝基苯磺酰胺
目录号: PC12654 纯度: ≥98%
CAS No. :433695-36-4
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中文名称
N,N,2-三甲基-5-硝基苯磺酰胺
中文别名
N,N,2-三甲基-5-硝基苯磺酰胺;2-甲基-5-硝基-N,N-二甲基苯磺酰胺;N,N,2-Trimethyl-5-nitrobenzenesulfonamide N,N,2-三甲基-5-硝基苯磺酰胺
英文名称
N,N,2-Trimethyl-5-nitrobenzenesulfonamide
英文别名
5-Nitro-2,N,N-trimethylbenzenesulfonamide;BRL-50481;N,N,2-Trimethyl-5-nitrobenzenesulfonamide;BRL 50481;Benzenesulfonamide,N,N,2-trimethyl-5-nitro;F1084-0159;BRL50481;Benzenesulfonamide, N,N,2-trimethyl-5-nitro-;03G869PR3P;N,N,2-Trimethyl-5-nitro-benzenesulfonamide;Cambridge id 6971444;GTPL5154;IFIUFCJFLGCQPH-UHFFFAOYSA-N;HMS3260P09;HMS3677O11;HMS3413O11;HMS3268D16;Tox21_500234;STL377005;BDBM50277784;BCP30210;s5837;TRA
Cas No.
433695-36-4
分子式
C9H12N2O4S
分子量
244.27
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

BRL-50481 is a novel and selective inhibitor of PDE7 with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 0.15 μM (PDE7A), 12 μM (PDE7B), 62 μM (PDE4), 490 μM (PDE3)

体外研究(In Vitro)

BRL-50481 increases the cAMP content (19.1±6.2% of IBMX response at 300 μM) but is considerably less potent. BRL-50481 (30 μM) fails to suppress proliferation by itself but significantly potentiates the effect of rolipram. BRL-50481 (30 μM) has no effect on IL-15-induced proliferation but augments the inhibitory effect of rolipram. Pretreatment (30 min) of human monocytes with BRL-50481 has, by itself, a negligible (~2 to 10%) inhibitory effect on TNFα output at all concentrations tested. BRL-50481 also potentiates the inhibitory effect of PGE2 on LPS-induced TNFα release. BRL-50481 has no significant effect by itself on κB-dependent transcription (5.6±1.9% inhibition at 30 μM) and fails to enhance the effect of rolipram (maximum inhibition, 52.9±2.7%; pIC30 value of 5.33±0.12). BRL-50481 suppresses, in a concentration-dependent manner, LPS-induced TNFα release in monocytes in which PDE7A1 is induced (21.7±1.6% inhibition at 30 μM at the 12-h time point).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 300 mg/mL (1228.15 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (insoluble)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.0938 mL 20.4692 mL 40.9383 mL
5 mM 0.8188 mL 4.0938 mL 8.1877 mL
10 mM 0.4094 mL 2.0469 mL 4.0938 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

搜索质检报告(COA)

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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