ITX5061
目录号: PL08737 纯度: ≥98%
CAS No. :1252679-52-9
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中文名称
ITX5061
中文别名
N-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide,hydrochloride
英文名称
ITX5061
英文别名
ITX5061;ITX 5061;J4RA8K2Q2A;BCP30784;Q27281205;1-Naphthaleneacetamide, N-(5-(1,1-dimethylethyl)-2-methoxy-3- ((methylsulfonyl)amino)phenyl)-4-(2-(4-morpholinyl)ethoxy)-alpha-oxo-, hydrochloride (1:1);N-[5-Tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl;N-(5-(tert-butyl)-2-methoxy-3-(methylsulfonamido)phenyl)-2-(4-(2-morpholinoethoxy)naphthalen-1-yl)-2-oxoacetamide hydrochloride;N-[5-(1,1-Dimethylethyl)-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-[2-(4-morpholinyl)ethoxy]-alpha-oxo-1-naphthaleneacetamide hydrochloride;1-Naphthaleneacetamide, N-(5-(1,1-dimethylethyl)-2-methoxy-3- ((me;ITX-5061 HCl
Cas No.
1252679-52-9
分子式
C30H38ClN3O7S
分子量
620.16
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
ITX5061 是 一个 II 型 p38 MAPK 抑制剂,也是清道夫受体 B1 (SR-B1) 的拮抗剂。
生物活性
ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
性状
Solid
IC50 & Target[1][2]
p38 MAPK, SR-B1
体内研究(In Vivo)
ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1). Treatment of ITX5061 (30 mg/kg/day) for mice results in a 50% increase in HDL-C levels compare to baseline. ApoA-I levels are moderately (+15 %) but significantly increased in ITX5061-treated HuAITg mice, compare to mice receive vehicle. ITX5061 significantly decreases HDL-CE catabolism with an FCR of 1.86±0.40 pools/d vs 2.47±0.26 pools/d in the control group (P<0.05), while calculated production rates are identical in both groups (129±24 μg/g/d vs 129±16 μg/g/d). Moreover, accumulation of [H] CE in the liver is significantly lower in ITX5061-treated mice indicating that increased HDL-CE levels are due to reduced uptake by the liver. has not independently confirmed the accuracy of these methods. They are for reference
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Masson D, et al. Increased HDL cholesterol and apoA-I in humans and mice treated with a novel SR-BI inhibitor. Arterioscler Thromb Vasc Biol. 2009 Dec;29(12):2054-60.
溶解度数据
In Vitro: DMSO : ≥ 83.3 mg/mL (134.32 mM)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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