trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid

Product Name: trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid
CAS No.: 1031336-60-3
Chemical Name: trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid
Synonyms: ABT-046;ABT 046,ABT046;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-
CBNumber: CB52589759
Molecular Formula: C20H22N4O2
Formula Weight: 350.41
MOL File: 1031336-60-3.mol

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trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-1213
Product name: ABT-046
Purity: 99.25%
Packaging: 5mg
Price: $294
Updated: 2021/12/16

ChemScene

Product number: CS-1213
Product name: ABT-046
Purity: 99.25%
Packaging: 10mg
Price: $516
Updated: 2021/12/16

ChemScene

Product number: CS-1213
Product name: ABT-046
Purity: 99.25%
Packaging: 50mg
Price: $1850
Updated: 2021/12/16

ChemScene

Product number: CS-1213
Product name: ABT-046
Purity: 99.25%
Packaging: 100mg
Price: $2714
Updated: 2021/12/16

Crysdot

Product number: CD31004789
Product name: ABT-046
Purity: 98+%
Packaging: 5mg
Price: $172
Updated: 2021/12/16

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trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid Chemical Properties,Usage,Production

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 (C_2h = 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.

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-046^a^[1]

	mouse (10 mg/kg)	rat (5 mg/kg)
	iv^b
T_1/2 (h)	4.6	3.8
V_ss (L/kg)	0.3	0.3
Clp (L/h/kg)	0.1	0.05
	po^b
T_1/2 (h)	5.1	5.6
C_max (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.

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

trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid Preparation Products And Raw materials

Raw materials

Preparation Products

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trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid Suppliers

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1031336-60-3, trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acidRelated Search:

Cyclohexaneacetic acid, 4-[4-(7-aMinopyrazolo[1,5-a]pyriMidin-6-yl)phenyl]-, trans-

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

ABT-046

trans-4-[4-(7-Aminopyrazolo[1,5-a]pyrimidin-6-yl)phenyl]cyclohexaneacetic acid

DGAT-1 INHIBITOR; ABT 046;ABT046

ABT 046,ABT046

1031336-60-3