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DGAT-1 inhibitor 2

Antiobesity agents CAS# 942999-61-3

DGAT-1 inhibitor 2

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Chemical structure

DGAT-1 inhibitor 2

3D structure

Chemical Properties of DGAT-1 inhibitor 2

Cas No. 942999-61-3 SDF Download SDF
PubChem ID 16202164 Appearance Powder
Formula C24H28N4O3 M.Wt 420.5
Type of Compound N/A Storage Desiccate at -20°C
Synonyms DGAT-1 inhibitor
Solubility DMSO : 25 mg/mL (59.45 mM; Need ultrasonic)
Chemical Name 2-[4-[4-(4-amino-7,7-dimethylpyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]-1-bicyclo[2.2.2]octanyl]acetic acid
SMILES CC1(C(=NC2=C(N=CN=C2O1)N)C3=CC=C(C=C3)C45CCC(CC4)(CC5)CC(=O)O)C
Standard InChIKey VGPKUACRBMPJLF-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H28N4O3/c1-22(2)19(28-18-20(25)26-14-27-21(18)31-22)15-3-5-16(6-4-15)24-10-7-23(8-11-24,9-12-24)13-17(29)30/h3-6,14H,7-13H2,1-2H3,(H,29,30)(H2,25,26,27)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of DGAT-1 inhibitor 2

DescriptionDGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents. IC50 value: Target: DGAT-1 Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) is one of two known DGAT enzymes that catalyze the final step in triglyceride synthesis. Findings from genetically modified mice as well as pharmacological studies suggest that inhibition of DGAT1 is a promising strategy for the treatment of obesity and type 2 diabetes.

References:
[1]. Matsuda D, Tomoda H. DGAT inhibitors for obesity. Curr Opin Investig Drugs. 2007 Oct;8(10):836-41. [2]. Birch, Alan M.; Birtles, Susan; Buckett, Linda K. et al. Discovery of a Potent, Selective, and Orally Efficacious Pyrimidinooxazinyl Bicyclooctaneacetic Acid Diacylglycerol Acyltransferase-1 Inhibitor. Journal of Medicinal Chemistry (2009), 52(6), 1558-15 [3]. King AJ, Judd AS, Souers AJ. Inhibitors of diacylglycerol acyltransferase: a review of 2008 patents. Expert Opin Ther Pat. 2010 Jan;20(1):19-29. [4]. Cao J, Zhou Y, Peng H et al. Targeting Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases. J Biol Chem. 2011 Dec 2;286(48):41838-51.

DGAT-1 inhibitor 2 Dilution Calculator

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DGAT-1 inhibitor 2 Molarity Calculator

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Preparing Stock Solutions of DGAT-1 inhibitor 2

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3781 mL 11.8906 mL 23.7812 mL 47.5624 mL 59.453 mL
5 mM 0.4756 mL 2.3781 mL 4.7562 mL 9.5125 mL 11.8906 mL
10 mM 0.2378 mL 1.1891 mL 2.3781 mL 4.7562 mL 5.9453 mL
50 mM 0.0476 mL 0.2378 mL 0.4756 mL 0.9512 mL 1.1891 mL
100 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.4756 mL 0.5945 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on DGAT-1 inhibitor 2

Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) is one of two known DGAT enzymes that catalyze the final step in triglyceride synthesis. Findings from genetically modified mice as well as pharmacological studies suggest that inhibition of DGAT1 is a promising strategy for the treatment of obesity and type 2 diabetes. This compound is an effective inhibitor of DGAT-1. Antiobesity agents.

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References on DGAT-1 inhibitor 2

Preclinical pharmacokinetic characterization of 2-(4-(4-(5-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido)-1H-benzo[d]imidazo l-2-yl)phenyl)cyclohexyl) acetic acid, a novel DGAT-1 inhibitor.[Pubmed:24152122]

Xenobiotica. 2014 May;44(5):465-71.

1. A novel diacylglyceride acyltransferase-1 (DGAT-1) inhibitor, 2-(4-(4-(5-(2-phenyl-5-(trifluoromethyl) oxazole-4-carboxamido)-1H-benzo[d]imidazol-2-yl)phenyl)cyclohexyl) acetic acid (KR-69232), was synthesized for a potential therapeutic use against several metabolic disorders, such as obesity, insulin resistance, and type II diabetes, characterized by excessive triglycerides (TGs) in the blood. 2. The half-lives against phase I metabolism were measured as 75.3 +/- 20.9 min and over 120 min in rat and human liver microsomes, respectively. In Caco-2 cell monolayers, extremely low permeability (<0.13 x 10(-)(6)cm/s) was seen in the absorptive direction, predicting limited intestinal absorption of KR-69232. This compound was highly bound to rat and human plasma proteins (>99.8%). 3. With the intravenous administration of KR-69232 in rats (1, 2, and 5 mg/kg), non-linear kinetics were observed at the highest dose, with significantly higher systemic clearance, higher volume of distribution, and lower dose-normalized AUC. Following oral administration, it exhibited low bioavailability (<10%) and was absorbed slowly (T(max), 3.8-5.2 h) over the dose range. We also confirmed that considerable KR-69232 remained in the intestine at T(max), demonstrating its limited absorption into the systemic circulation.

Pharmacological characterization of [trans-5'-(4-amino-7,7-dimethyl-2-trifluoromethyl-7H-pyrimido[4,5-b][1,4]oxazin-6 -yl)-2',3'-dihydrospiro(cyclohexane-1,1'-inden)-4-yl]acetic acid monobenzenesulfonate (JTT-553), a novel acyl CoA:diacylglycerol transferase (DGAT) 1 inhibitor.[Pubmed:25747985]

Biol Pharm Bull. 2015;38(2):263-9.

Acyl CoA:diacylglycerol acyltransferase (DGAT) 1 is an enzyme that catalyzes the final step in triglyceride (TG) synthesis. This enzyme is considered to be a potential therapeutic target for obesity and diabetes. Here, results of an investigation of the pharmacological effects of JTT-553 [trans-5'-(4-amino-7,7-dimethyl-2-trifluoromethyl-7H-pyrimido[4,5-b][1,4]oxazin-6 -yl)-2',3'-dihydrospiro(cyclohexane-1,1'-inden)-4-yl]acetic acid monobenzenesulfonate, a novel DGAT1 inhibitor, are reported. To measure the inhibitory activity of JTT-553 against DGAT1, TG synthesis using [(14)C]-labeled oleoyl-CoA was evaluated. Similarly, the inhibitory activity of JTT-553 against DGAT2, an isozyme of DGAT1, and acyl-CoA cholesterol acyltransferase (ACAT) 1, which is highly homologous to DGAT1, were evaluated. JTT-553 selectively inhibited human DGAT1 and showed comparable inhibitory effects on the activity of human, rat, and mouse DGAT. In vivo, JTT-553 suppressed plasma TG and chylomicron TG levels after olive oil loading in Sprague-Dawley (SD) rats. JTT-553 also inhibited TG synthesis in epididymal fat after [(14)C] oleic acid injection in C57BL/6J mice. Food intake was evaluated in SD rats fed 3.1%, 13%, or 35% (w/w) fat diets. In rats fed the 35% fat diet, JTT-553 reduced food intake. This reduction of food intake was observed 2 h after feeding, lasted for 24 h, and correlated with dietary fat content. Furthermore, JTT-553 reduced daily food intake and body weight gain in diet-induced obese rats after 4-week repeated administration. JTT-553 exerted multiple effects on intestinal fat absorption, adipose fat synthesis, and food intake, and consequently induced body weight reduction. Therefore, JTT-553 is expected to be an effective novel therapeutic agent for the treatment of obesity.

Description

DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.

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