| Identification | Back Directory | [Name]
trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid | [CAS]
1031336-60-3 | [Synonyms]
ABT-046
DGAT-1 INHIBITOR; ABT 046;ABT046
trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid
2-(trans-4-(4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl)cyclohexyl)acetic acid
2-((1R,4R)-4-(4-(7-AMINOPYRAZOLO[1,5-A]PYRIMIDIN-6-YL)PHENYL)CYCLOHEXYL)ACETIC ACID
Cyclohexaneacetic acid, 4-[4-(7-aMinopyrazolo[1,5-a]pyriMidin-6-yl)phenyl]-, trans- | [Molecular Formula]
C20H22N4O2 | [MDL Number]
MFCD22124521 | [MOL File]
1031336-60-3.mol | [Molecular Weight]
350.41 |
| Chemical Properties | Back Directory | [density ]
1.39 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 66.67 mg/mL (190.26 mM; Need ultrasonic) | [form ]
Powder | [pka]
4.72±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1[1]. | [in vivo]
ABT-046 (0.03-3 mg/kg; i.g.; once) significantly reduced postprandial triglycerides in CD-1 mice[1].
ABT-046 (0.3 mg/kg; i.g.; once) abolishes the postprandial triglyceride excursion in diet-induced obesity mice[1]. | Animal Model: | Male CD-1 mice, postprandial hyperlipidemia model[1] | | Dosage: | 0.03, 0.3, or 3 mg/kg | | Administration: | Oral gavage, single dose | | Result: | Showed a dose-dependent reduction in serum triglycerides starting at 0.03 mg/kg and increasing through the higher doses (40, 60, and 90% reduction from vehicle at 0.03, 0.3, and 3.0 mg/kg, respectively). The ascending pharmacodynamics correlated well with a linear increase in plasma exposure going from 0.03 to 3 mg/kg (C2h = 0.033, 0.36, and 3.10 μg/mL at 0.03, 0.3, and 3.0 mg/kg, respectively). |
| Animal Model: | Male C57BL/6J diet-induced obesity (DIO) mice[1] | | Dosage: | 0.3 mg/kg | | Administration: | Oral gavage, single dose | | Result: | Afforded a sustained reduction in serum triglyceride concentrations throughout the experiment.
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| Animal Model: | CD-1 mice and Sprague-Dawley rats[1] | | Dosage: | 10 mg/kg or 5 mg/kg | | Administration: | Intravenous injection or oral gavage (Pharmacokinetic Analysis) | | Result: | Selected Pharmacokinetic Properties of ABT-046a[1]
| mouse (10 mg/kg) | rat (5 mg/kg) | | ivb | | | T1/2 (h) | 4.6 | 3.8 | | Vss (L/kg) | 0.3 | 0.3 | | Clp (L/h/kg) | 0.1 | 0.05 | | pob | | | T1/2 (h) | 5.1 | 5.6 | | Cmax (μg/mL) | 17.4 | 9.3 | | AUC (μg h/mL) | 151 | 130 | | F (%) | 78 | 91 |
a All values are mean values ± SEMs (n = 3 unless specified otherwise).
b 1% Tween-80 in water.
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| [References]
[1] Yeh VS, et al. Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of Acyl-CoA: Diacylglycerol acyltransferase 1. J Med Chem. 2012 Feb 23;55(4):1751-1757. DOI:10.1021/jm201524g |
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