DS-6930
DS-6930 is a potent and selective agonist of PPARγ, with an EC50 of 41 nM. DS-6930 could robust reduce plasma glucose (PG), and with fewer PPARγ-related adverse effects than Rosiglitazone. DS-6930 can be used for the research of diabetes.
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- CAS No.: 1242328-82-0
- Formule: C23H21N3O4
- Masse moléculaire:403.43
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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
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Activité biologique
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PPARγ 41 nM (EC50) |
DS-6930 exhibits high potency in vitro with an intermediate PPARγ agonist activity (EC50=41 nM, Emax=68%), and possesses high PPARα or PPARδ selectivity (13% PPARα activation at 10 µM and no PPARδ activation at 10 µM) [1].
DS-6930 (10-100 µM) exhibits lower cell toxicity at 100 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DS-6930 (100-1000 mg/kg; p.o.for 4 weeks) does not affect any liver enzyme activities and has no remarkable change in relative heart weigh in F344 rats[1].
DS-6930 exhibits Cmax=0.0792 µg/mL, Tmax=1.8 h, and AUC0-24h=0.861 h•µg/mL following oral (0.3 mg/kg) administration on day 22 in rats[1].
DS-6930 exhibits Cmax=2.25 µg/mL, Tmax=5.0 h, T1/2=13.5 h, and AUClast=23.5 h•µg/mL following oral (3 mg/kg) administration in cynomolgus monkeys[1].
DS-6930 exhibits excellent bioavailability (F=89%), total body clearance (CL=2.06 mL/min/kg), and distribution volume at steady state (Vss=0.36 L/kg) following intravenous (1 mg/kg) administration in cynomolgus monkeys[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ZDF rats[1]
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Dosage:0.1, 0.3, 1, 3 mg/kg
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Administration:P.o. daily for 3 weeks
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Result:47% PG reduction at dose of 0.3 mg/kg vs vehicle control.
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Animal Model:Male ZDF rats[1]
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Dosage:0.3 mg/kg (Pharmacokinetic Analysis)
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Administration:P.o. daily for 22 days
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Result:Cmax=0.0792 µg/mL; Tmax=1.8 h; AUC0-24h=0.861 h•µg/mL.
Chemical Information
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CAS No. 1242328-82-0
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Masse moléculaire 403.43
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Formule C23H21N3O4
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SMILES
O=C(O)C1=CC=CC(OCC2=NC3=CC=C(OC4=NC=C(C)C=C4C)C=C3N2C)=C1
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DS-6930 Related Classifications
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