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.
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- CAS No.: 1848233-59-9
- Formule: C25H26F3N5O4
- Masse moléculaire:517.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
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ABHD6 |
ABHD2 |
PAFAH2 |
PLA2G7 |
CES1 |
In Vitro
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.
In Vivo
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.
Chemical Information
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CAS No. 1848233-59-9
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Masse moléculaire 517.50
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DO53 Related Classifications
HY-121032 Related Classifications
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