JNJ0966

目录号: PL07414 纯度: ≥99%
JNJ0966 是一种高选择性 MMP-9 酶原抑制剂,其 IC50 值为 440 nM。
CAS No. :315705-75-0
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中文名称
JNJ0966
英文名称
JNJ0966
英文别名
JNJ0966;N-(2-((2-methoxyphenyl)amino)-4'-methyl-[4,5'-bithiazol]-2'-yl)acetamide;Oprea1_109350;Oprea1_487426;BCP25926;JNJ 0966;s5696;N-[5-[2-(2-methoxyanilino)-1,3-thiazol-4-yl]-4-methyl-1,3-thiazol-2-yl]acetamide;N-(2-(2-Methoxyphenylamino)-4'-methyl-4,5'-bithiazol-2'-yl)acetamide;N-[2-[(2-Me
Cas No.
315705-75-0
分子式
C16H16N4O2S2
分子量
360.45
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
JNJ0966 是一种高选择性 MMP-9 酶原抑制剂,其 IC50 值为 440 nM。
生物活性
JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC 50 of 440 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 440 nM (MMP-9 zymogen)
体外研究(In Vitro)
JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC50 of 440 nM. The activations of proMMP-1, proMMP-2, and proMMP-3 are not significantly different in the presence or absence of 10 μM JNJ0966, whereas proMMP-9 activation by trypsin is significantly attenuated by JNJ0966. The addition of JNJ0966 to the reaction results in a significant reduction in fully processed MMP-9 and an apparent accumulation of the intermediate species. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
The exposures of JNJ0966 are dose-dependent, with plasma and brain concentrations for the 10-mg/kg dose of 77.5±31.1 ng/mL (215 nM) and 481.6±162.5 ng/g (~1336 nM), respectively, whereas the 30-mg/kg dose achieves 293.6±118.4 ng/mL (815 nM) in plasma and 1394.0±649.1 ng/g (~3867 nM) in brain. JNJ0966 is preferentially partitioned in brain, with brain/plasma ratios of 6.2 for the 10-mg/kg dose and 4.7 for the 30-mg/kg dose. 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
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Scannevin RH, et al. Discovery of a highly selective chemical inhibitor of matrix metalloproteinase-9 (MMP-9) thatallosterically inhibits zymogen activation. J Biol Chem. 2017 Oct 27;292(43):17963-17974.
溶解度数据
In Vitro: DMSO : 100 mg/mL (277.43 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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