SPHINX31
目录号: PL11454 纯度: ≥99%
CAS No. :1818389-84-2
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中文名称
SPHINX31
中文别名
N-(2-(4-(吡啶-2-基甲基)哌嗪-1-基)-5-(三氟甲基)苯基)-5-(吡啶-4-基)呋喃-2-甲酰胺
英文名称
SPHINX31
英文别名
SPHINX31
Cas No.
1818389-84-2
分子式
C27H24F3N5O2
分子量
507.51
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
SPHINX31 是一种有效的、丝氨酸/富含精氨酸的蛋白激酶1 (SRPK1) 的选择性抑制剂,其IC50 值为 5.9 nM。SPHINX31 能够抑制富丝氨酸/精氨酸剪接因子 1 (SRSF1) 的磷酸化。SPHINX31 还能降低促血管生成基因 VEGF-A165a 亚型的 mRNA 表达。SPHINX31 可用于研究新生血管性眼病。
生物活性
SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC 50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A 165 a isoform. SPHINX31 can be used to research neovascular eye disease.
性状
Solid
IC50 & Target[1][2]
IC50: 5.9 nM (SRPK1)
VEGF-A165a
体外研究(In Vitro)
SPHINX31 (0.3-10 μM; 24 h) significantly down-regulates the expression of VEGF-A165a mRNA.
SPHINX31 (0.3 μM; 24 h) suppresses SRSF1 phosphorylation and nuclear localization.
SPHINX31 (0.3-10 μM; 24 h) decreases pre-tube formation and the rate of migration for human umbilical vein endothelial cells (HUVECs). has not independently confirmed the accuracy of these methods. They are for reference only.RT-PCR
体内研究(In Vivo)
SPHINX31 (200 μg/mL; twice daily topical eye drops) protects the retinal endothelial permeability barrier from diabetes-associated loss of integrity. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
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]. Batson J, et al. Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease. ACS Chem Biol. 2017 Mar 17;12(3):825-832.
[2]. Supradit K, et al. Inhibition of serine/arginine-rich protein kinase-1 (SRPK1) prevents cholangiocarcinoma cells induced angiogenesis. Toxicol In Vitro. 2022 Aug;82:105385.
溶解度数据
In Vitro: DMSO : 17.33 mg/mL (34.15 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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