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AZD 3988

Potent and selective DGAT-1 inhibitor CAS# 892489-52-0

AZD 3988

Catalog No. BCC5621----Order now to get a substantial discount!

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AZD 3988: 5mg $184 In Stock
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Chemical structure

AZD 3988

3D structure

Chemical Properties of AZD 3988

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.
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 AZD 3988

DescriptionPotent 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

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AZD 3988 Molarity Calculator

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Preparing Stock Solutions of AZD 3988

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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References on AZD 3988

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.

Description

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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