H-151
目录号: PL11539 纯度: ≥99%
CAS No. :941987-60-6
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中文名称
H-151
中文别名
1-(4-乙基苯基)-3-(1H-吲哚-3-基)脲
英文名称
H-151
英文别名
1-(4-ethylphenyl)-3-(1H-indol-3-yl)urea;N-(4-ethylphenyl)-N'-1H-indol-3-yl-urea;H 151;H151;STING antagonist;3-(4-ethylphenyl)-1-(1H-indol-3-yl)urea;H151 pound>>H 151;GTPL10122;BCP29964;s6652;AK00799464;N-(4-Ethylphenyl)-N′-1H-indol-3-ylurea (ACI);H 151 (pharmacological agent);H-151
Cas No.
941987-60-6
分子式
C17H17N3O
分子量
279.34
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
H-151 是一种有效,选择性和共价的 STING 拮抗剂,在体外和体内均具有显着的抑制活性。H-151 减少 TBK1 磷酸化并抑制 STING 棕榈酰化。H-151 可用于自身炎症性疾病的研究。
生物活性
H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease.
性状
Solid
IC50 & Target[1][2]
STING
体外研究(In Vitro)
H-151 (0.02-2 μM) reduces IFNβ luciferase reporter measurements of HEK293T cells.
H-151 (0.5 μM; 2 h) inhibits the phosphorylation of TBK1 in THP-1 cells.
H-151 (1 μM; 3 h) suppresses hsSTING palmitoylation. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
H-151 (750 nmol per mouse; a single i.p.) markedly reduces systemic cytokine responses in CMA-treated mice.
H-151 (750 nmol per mouse; i.p. daily for 7 d) exhibits notable efficacy in Trex1 mice that expressed a bioluminescent IFNβ reporter.
H-151 (750 nmol per mouse; i.p.) reaches effective systemic levels, displays a short half-life in the serum and forms an adduct to mmSTING in wild-type mice. 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;In solvent -80°C 6 months
参考文献
[1]. Haag SM, et al. Targeting STING with covalent small-molecule inhibitors. Nature. 2018 Jul;559(7713):269-273.
溶解度数据
In Vitro: DMSO : 31.25 mg/mL (111.87 mM; ultrasonic and warming and heat to 60°C)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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