DO53
DO53 is a serine hydrolase inhibitor that targets ABHD6, PAFAH2, PLA2G7, ABHD2 and CES1C. DO53 reduces LPS (HY-D1056A1)-induced cytokine production in the mouse brain, decreases fasting-induced refeeding behavior, and induces hypoactivity in mice. As a DAGL negative control, DO53 shows no activity against DAGLα/β in vivo, and does not affect brain lipid levels, DSE/DSI synaptic plasticity or LPS-induced anhidrosis in mice. DO53 can be used in studies related to LPS-induced neuroinflammation and fasting-induced refeeding.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1848233-59-9
- 分子式: C25H26F3N5O4
- 分子量:517.50
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
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ABHD6 |
ABHD2 |
PAFAH2 |
PLA2G7 |
CES1 |
体外実験
DO53 inhibits carboxylesterase activity in mouse liver membrane proteome, representing a shared off-target with active triazole urea DAGL inhibitors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male)[1]
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Dosage:3, 10, 30 and 50 mg/kg (4 hour treatment); 50 mg/kg (2, 4, 8, or 24 hour treatment)
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Administration:i.p.; single dose
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Result:Did not substantially inhibit DAGLα or DAGLβ activity in mouse brain at any tested dose (3, 10, 30, 50 mg/kg) at 4 hours postdosing.
Did not inhibit DAGLα or DAGLβ activity at 50 mg/kg at any time point (2, 4, 8, 24 hours) postdosing.
Inhibited the serine hydrolases ABHD6 and PLA2G7 at all tested doses and time points.
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Animal Model:C57BL/6 (male; LPS-induced neuroinflammation)[1]
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Dosage:50 mg/kg
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Administration:i.p.; single dose; administered 60-90 minutes prior to LPS treatment
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Result:Did not alter basal brain levels of 2-AG, arachidonic acid (AA), or prostaglandin E2 (PGE2), nor suppress LPS-induced elevations in brain 2-AG or PGE2.
Did not blunt LPS-induced anapyrexia (core body temperature reduction) in mice.
Reduced LPS-induced increases in brain interleukin-1β (IL-1β) cytokine levels to a similar degree as DAGL inhibitors DH376 and DO34.
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Animal Model:C57Bl/6J (12-week-old male)[2]
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Dosage:50 mg/kg
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Administration:i.p.; single dose
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Result:Reduced cumulative food intake significantly at 2 hours and 4 hours post-refeeding compared to vehicle-treated mice.
Elevated fat oxidation and suppressed carbohydrate oxidation relative to vehicle controls over the monitoring period.
Reduced normalized locomotor activity over 4 hours to approximately 40% of vehicle-treated levels.
化学情報
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CAS 番号 1848233-59-9
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分子量 517.50
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分子式 C25H26F3N5O4
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SMILES
O=C(OC(C)(C)C)N1CC(N(CC1)C(N2N=NC(C3=CC=C(C=C3)OC(F)(F)F)=C2)=O)C4=CC=CC=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Ogasawara D, et al. Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition. Proceedings of the National Academy of Sciences of the United States of America. 2016 Jan 05;113(1):26-33. [Content Brief]
[2]. Deng H, et al. Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding. Journal of medicinal chemistry. 2017 Jan 12;60(1):428-440. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
DO53 関連分類
HY-121032 関連分類
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