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品質水準
アッセイ
≥98% (HPLC)
フォーム
powder
色
white to beige
溶解性
DMSO: 20 mg/mL, clear
保管温度
room temp
SMILES記法
O=C(ON1C(CCC1=O)=O)N2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=C(Cl)C=C4)CC2
InChI
1S/C22H21Cl2N3O4/c23-17-5-1-15(2-6-17)21(16-3-7-18(24)8-4-16)25-11-13-26(14-12-25)22(30)31-27-19(28)9-10-20(27)29/h1-8,21H,9-14H2
InChI Key
BEADRWVIFHOSGN-UHFFFAOYSA-N
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アプリケーション
MJN110 has been used as a monoacylglycerol lipase (MAGL) inhibitor to study its effect on aggressive grooming in rats. It has also been used to inhibit lipid droplet formation.
生物化学的／生理学的作用
MJN110 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) with >10,000 selectivity over FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA). MJN110 inhibits rat, mouse and human MAGL with IC50 values ranging from < 100 nM in rat to an IC50 of ~1 nM with 10- and 100-fold selectivity over closely related ABHD6, a serine hydrolase that acts as an alternative hydrolase of 2-AG, and LYPLA1/2 in human PC3 cells. MJN110 showed potent anti-hyperalgesic activity in a rat model of diabetic neuropathy, showing a therapeutic potential for treating diabetes chronic pain.
特徴および利点
This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
シグナルワード
Warning
危険有害性情報
危険有害性の分類
Acute Tox. 4 Oral
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
SML0872-25MG:
SML0872-BULK:
SML0872-IP:
SML0872-VAR:
SML0872-5MG:
最新バージョンのいずれかを選択してください：
A L Thompson et al.
The Journal of pharmacology and experimental therapeutics, 373(2), 230-238 (2020-02-15)
Metastatic breast cancer is prevalent worldwide, and one of the most common sites of metastasis is long bones. Of patients with disease, the major symptom is pain, yet current medications fail to adequately result in analgesic efficacy and present major
Robert A Owens et al.
Neuropharmacology, 125, 80-86 (2017-07-05)
Substantial challenges exist for investigating the cannabinoid receptor type 1 (CB
Lipid droplet-dependent fatty acid metabolism controls the immune suppressive phenotype of tumor-associated macrophages
Wu H, et al.
EMBO Molecular Medicine (2019)
Jae Won Chang et al.
ACS chemical biology, 8(7), 1590-1599 (2013-05-25)
Serine hydrolases are one of the largest and most diverse enzyme classes in Nature. Inhibitors of serine hydrolases are used to treat many diseases, including obesity, diabetes, cognitive dementia, and bacterial and viral infections. Nonetheless, the majority of the 200+
Elizabeth A Fucich et al.
Journal of neurophysiology, 123(2), 707-717 (2020-01-09)
Our previous work showed that lateral fluid percussion injury to the sensorimotor cortex (SMC) of anesthetized rats increased neuronal synaptic hyperexcitability in layer 5 (L5) neurons in ex vivo brain slices 10 days postinjury. Furthermore, endocannabinoid (EC) degradation inhibition via
資料
DISCOVER Bioactive Small Molecules for Neuroscience
関連コンテンツ
神経科学分野における低分子生理活性物質の創薬研究
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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