貨號	規格	價格	上海	北京	武漢	南京
S83551-1mg	99.2%	￥387.60 S83551-1mg ￥387.60 現貨	10 10	-	-	-
S83551-5mg	99.2%	￥570.00 S83551-5mg ￥570.00 現貨	4 4	-	-	-
S83551-10mg	99.2%	￥1050.00 S83551-10mg ￥1050.00 現貨	6 6	-	-	-
S83551-25mg	99.2%	￥1972.00 S83551-25mg ￥1972.00 現貨	5 5	-	-	-
S83551-50mg	≥98%	￥3400.00 S83551-50mg ￥3400.00 2-3天	0 貨期：2-3天	-	-	-
S83551-100mg	≥98%	￥5900.00 S83551-100mg ￥5900.00 2-3天	0 貨期：2-3天	-	-	-

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產品介紹

ML355是有效的選擇性h12-LOX抑制劑，IC50為290 nM

產品描述：

ML355是有效的選擇性h12-LOX抑制劑，IC50為290 nM

靶點：

12-LOX;Lipoxygenase

體外研究：

ML355 displays nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases

體內研究：

In vivo PK studies where ML355 is administered as a solution via IV (3mpk) and PO (30mpk) demonstrated that ML355 is orally bioavailable (%F = 20) with good half-life (T1/2 = 2.9 hours). At 30 mpk dosing, ML355 achieves a Cmax of over 135 times the in vitro IC50 and remains over IC50 value for over 12 hours. The compound has low clearance (3.4 mL/min/kg) and good overall exposure (AUCinf) of 38 μM. Although, the volume of distribution (VD) observed is low (0.55 L/kg), the rest of the PK profiling results suggest a reasonable distribution between tissue and blood

細胞實驗：

Cell lines: U87 cells Concentrations: 10 μM Incubation Time: 24 h Method: Cells were treated with indicated concentration of drug for 24 h.

動物實驗：

Animal Models: C57BL/6 mice Dosages: 15 or 30 mg/kg Administration: p.o.

參考文獻：

1. Luci D, et al. Discovery of ML355, a Potent and Selective Inhibitor of Human 12-Lipoxygenase. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2013 Apr 12 [updated 2014 Sep 18]. 2. Yang X, et al. miR-18a promotes glioblastoma development by down-regulating ALOXE3-mediated ferroptotic and anti-migration activities. Oncogenesis. 2021 Feb 12;10(2):15. 3. Adili R, et al. First Selective 12-LOX Inhibitor, ML355, Impairs Thrombus Formation and Vessel Occlusion In Vivo With Minimal Effects on Hemostasis. Arterioscler Thromb Vasc Biol. 2017 Oct;37(10):1828-1839.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.265 ml	11.324 ml	22.649 ml
5 mM	0.453 ml	2.265 ml	4.53 ml
10 mM	0.226 ml	1.132 ml	2.265 ml
50 mM	0.045 ml	0.226 ml	0.453 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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