おすすめの製品
アッセイ
≥98% (HPLC)
フォーム
powder
色
white to beige
溶解性
DMSO: 2 mg/mL, clear
保管温度
2-8°C
SMILES記法
Clc1c(cccc1)OC2CCN(CC2)C(=O)Nc3cc(ccc3)C(=O)NC
InChI
1S/C20H22ClN3O3/c1-22-19(25)14-5-4-6-15(13-14)23-20(26)24-11-9-16(10-12-24)27-18-8-3-2-7-17(18)21/h2-8,13,16H,9-12H2,1H3,(H,22,25)(H,23,26)
InChI Key
DPYTYQFYDLYWHZ-UHFFFAOYSA-N
生物化学的／生理学的作用
A939572 is an orally available piperidine-aryl urea-based small molecule that inhibits stearoyl-CoA desaturase 1 (SCD1) with high potency (IC50 = 37 nM/hSCD1 and <4 nM/mSCD1) with little hERG channel blockade activity (IC50 >100 μM). When administered in ob/ob mice, A939572 effectively reduces desaturation indices in vivo (18:0/18:1n9 ratio from 26.9 to 8.47 in liver; from 15.4 to 7.35 in plasma post 5-day 10 mg/kg bid p.o.). A939572 is a useful tool for probing SCD1-mediated physiological and pathological processes both in cultures (50 nM-10 μM) and in vivo (5-10 mg/kg i.p. or 10 mg/kg p.o. in mice).
Orally available, potent and selective stearoyl-CoA-desaturase 1 (SCD1) inhibitor.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
SML2356-25MG:
SML2356-BULK:
SML2356-VAR:
SML2356-5MG:
最新バージョンのいずれかを選択してください：
試験成績書（COA）
Lot/Batch Number
Justyna Janikiewicz et al.
Journal of lipid research, 56(10), 1901-1911 (2015-08-22)
Autophagy is indispensable for the proper architecture and flawless functioning of pancreatic β-cells. A growing body of evidence indicates reciprocal communication between autophagic pathways, apoptosis, and intracellular lipids. The way in which elevated levels of free saturated or unsaturated FAs
Mark Kin Fai Ma et al.
Journal of hepatology, 67(5), 979-990 (2017-06-26)
We investigated the functional role and clinical significance of stearoyl-CoA desaturase-1 (SCD1) mediated endoplasmic reticulum (ER) stress in regulating liver tumor-initiating cells (T-ICs) and sorafenib resistance, with the aim of developing a novel therapeutic strategy against hepatocellular carcinomas (HCCs). We
Mohamed A Lounis et al.
Biochimica et biophysica acta, 1861(11), 1662-1670 (2016-08-02)
Stearoyl-CoA desaturase 1 (SCD1) is a delta-9 fatty acid desaturase that catalyzes the synthesis of mono-unsaturated fatty acids (MUFA). SCD1 is a critical control point regulating hepatic lipid synthesis and β-oxidation. Scd1 KO mice are resistant to the development of
Hyeonwoo Kim et al.
Cell reports, 13(3), 495-503 (2015-10-13)
Some cancer cells exhibit elevated levels of free fatty acids (FAs) as well as high levels of β-catenin, a transcriptional co-activator that promotes their growth. Here, we link these two phenomena by showing that unsaturated FAs inhibit degradation of β-catenin.
Mohamed A Lounis et al.
American journal of physiology. Endocrinology and metabolism, 313(6), E710-E720 (2017-08-31)
Stearoyl-CoA desaturase-1 (SCD1) is a key player in lipid metabolism. SCD1 catalyzes the synthesis of monounsaturated fatty acids (MUFA). MUFA are then incorporated into triacylglycerols and phospholipids. Previous studies have shown that Scd1 deficiency in mice induces metabolic changes in
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