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SW033291

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Chemical Structure| 459147-39-8 同义名 : -
CAS号 : 459147-39-8
货号 : A509020
分子式 : C21H20N2OS3
纯度 : 99%+
分子量 : 412.591
MDL号 : MFCD02973087
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(84.83 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 25 mg/mL(60.59 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
靶点

  • Dehydrogenase

    15-PGDH, IC50:1.5 nM

    15-PGDH, Ki:0.1 nM
描述 15-hydroxyprostaglandin dehydrogenase (15-PGDH), that acts in vivo as a negative regulator of prostaglandin levels and activity, catalyzes the first step in the degradation of prostanoid family molecules, oxidizing the prostanoid 15-hydroxyl group to a ketone, and thereby abrogating binding to prostaglandin receptors. SW033291 is a potent inhibitor of 15-PGDH enzyme activity with IC50 and Kiapp of 1.5 nM and 0.1 nM, respectively. In Vaco-503 cells, SW033291 (2.5 μM) decreased cellular 15-PGDH enzyme activity by 85%. Treatment of A549 cells with SW033291 increased PGE2 levels by 3.5-fold at 500 nM, with 50% of maximal stimulation (EC50) at approximately 75 nM. Importantly, mice injected with SW033291 closely phenocopied 15-PGDH knockout mice, with 10 mg/kg SW033291 inducing a 2-fold increase in PGE2 levels in bone marrow, colon, lung and liver. Mice injected with SW033291 for three consecutive days showed similar significant benefits, including a doubling of peripheral neutrophil counts, a 65% increase in marrow SKL cells, and a 71% increase in marrow SLAM cells. In functional assays, bone marrow from SW033291-treated (10 mg/kg IP twice daily for 5 doses) mice showed significant 55% increases in the numbers of hematopoietic colonies generated after plating into methylcellulose. Likewise, ex vivo treatment of harvested bone marrow cells with SW033291 induced a significant 50% increase in hematopoietic colony formation[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.24mL

4.85mL

2.42mL
参考文献

[1]Zhang Y, Desai A, et al. TISSUE REGENERATION. Inhibition of the prostaglandin-degrading enzyme 15-PGDH potentiates tissue regeneration. Science. 2015 Jun 12;348(6240):aaa2340.

[2]Zhang Y, Desai A, Yang SY, et al. TISSUE REGENERATION. Inhibition of the prostaglandin-degrading enzyme 15-PGDH potentiates tissue regeneration. Science. 2015;348(6240):aaa2340