AZD 3988Potent and selective DGAT-1 inhibitor CAS# 892489-52-0 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 892489-52-0 | SDF | Download SDF |
| PubChem ID | 23648867 | Appearance | Powder |
| Formula | C23H22F2N4O4 | M.Wt | 456.44 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO and to 10 mM in 1eq. NaOH with gentle warming | ||
| Chemical Name | 2-[4-[4-[[5-(3,4-difluoroanilino)-1,3,4-oxadiazole-2-carbonyl]amino]phenyl]cyclohexyl]acetic acid | ||
| SMILES | C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)NC(=O)C3=NN=C(O3)NC4=CC(=C(C=C4)F)F | ||
| Standard InChIKey | NGEBYTLALFOQKI-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C23H22F2N4O4/c24-18-10-9-17(12-19(18)25)27-23-29-28-22(33-23)21(32)26-16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-20(30)31/h5-10,12-14H,1-4,11H2,(H,26,32)(H,27,29)(H,30,31) | ||
| 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. |
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| 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. |
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| 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. | ||
| Description | Potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50 = 0.6 nM). Exhibits selectivity for DGAT-1 over DGAT-2, Kv11.1 (hERG) and cytochrome P450 enzymes. Suppresses triacylglyceride (TAG) plasma excursion and adipose tissue TAG synthesis in rats. Reduces body weight of diet-induced obese rats. Cell permeable and orally bioavailable. |
AZD 3988 Dilution Calculator
AZD 3988 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1909 mL | 10.9543 mL | 21.9087 mL | 43.8174 mL | 54.7717 mL |
| 5 mM | 0.4382 mL | 2.1909 mL | 4.3817 mL | 8.7635 mL | 10.9543 mL |
| 10 mM | 0.2191 mL | 1.0954 mL | 2.1909 mL | 4.3817 mL | 5.4772 mL |
| 50 mM | 0.0438 mL | 0.2191 mL | 0.4382 mL | 0.8763 mL | 1.0954 mL |
| 100 mM | 0.0219 mL | 0.1095 mL | 0.2191 mL | 0.4382 mL | 0.5477 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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Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.[Pubmed:22608962]
Bioorg Med Chem Lett. 2012 Jun 15;22(12):3873-8.
A novel series of DGAT-1 inhibitors was discovered from an oxadiazole amide high throughput screening (HTS) hit. Optimisation of potency and ligand lipophilicity efficiency (LLE) resulted in a carboxylic acid containing clinical candidate 53 (AZD3988), which demonstrated excellent DGAT-1 potency (0.6 nM), good pharmacokinetics and pre-clinical in vivo efficacy that could be rationalised through a PK/PD relationship.
AZD3988 is a diacylglycerol acyl transferase-1 (DGAT-1) inhibitor with IC50s of 6, 5, 11 nM for human, rat, mouse, respectively.
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