GSK3494245|2080410-41-7|(DDD01305143)-陌孚医药/Medlife

您当前的位置：

GSK3494245 (Synonyms: DDD01305143)

目录号: PL10736 纯度: ≥98%

CAS No. :2080410-41-7

商品编号	规格	价格	会员价
PL10736-5mg	5mg	¥6305.45	请登录
PL10736-10mg	10mg	¥10138.18	请登录
PL10736-50mg	50mg	询价	询价
PL10736-100mg	100mg	询价	询价
PL10736-10mM*1mLinDMSO	10mM*1mLinDMSO	¥6936.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称	GSK3494245
英文名称	GSK3494245
英文别名	GSK3494245;N-(4-fluoro-3-(3-morpholinoimidazo[1,2-a]pyrimidin-7-yl)phenyl)pyrrolidine-1-carboxamide
Cas No.	2080410-41-7
分子式	C₂₁H₂₃FN₆O₂
分子量	410.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

GSK3494245 (DDD01305143) 是一种有效的、具有口服活性的、选择性的可在夹在 β4 和 β5 亚基之间的位点结合寄生虫蛋白酶体 (proteasome) 的糜蛋白酶样活性抑制剂(对于 WT L.donovani蛋白酶体IC₅₀=0.16μM)。GSK3494245 适度抑制人蛋白酶体的糜蛋白酶样活性 (IC₅₀: 26S=13 µM；富集的 THP-1 提取物 IC₅₀=40 µM)。GSK3494245 具有良好的生物安全特性。

生物活性

GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC 50 =0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC 50 : purified 26S=13 μM; enriched THP-1 extracts IC 50 =40μM). GSK3494245 exhibits attractive biological and biosafety properties.

性状

Solid

体外研究(In Vitro)

GSK3494245 shows EC50 value of 5.7 μM in L. donovani intramacrophage assay, where the amastigotes are cultured in differentiated THP-1 cells. GSK3494245 demonstrates good selectivity over mammalian cell growth inhibition (THP-1 cells; EC50 > 50 μM).
GSK3494245 (DDD01305143) shows pEC50s of 6.5 and 5.8 against axenic amastigote and ld InMac, respectively. Ld InMac is the intramacrophage assay carried out in THP-1 cells with L. donovani amastigote. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

GSK3494245 (25 mg/kg; orally twice a day for 10 consecutive days) elicits a >95% reduction of parasite load in Infected mice (L. donovani, LV9). 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

ClinicalTrial

参考文献

[1]. Wyllie S, et al. Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition. Proc Natl Acad Sci U S A. 2019;116(19):9318-9323.
[2]. Thomas MG, et al. Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis. J Med Chem. 2019;62(3):1180-1202.

溶解度数据	In Vitro: DMSO : 100 mg/mL (243.64 mM; Need ultrasonic)配制储备液

搜索质检报告(COA)

产品使用指南

Data Sheet

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。

相关产品

The molarity calculator equation

The dilution calculator equation