AZD 3988

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Cat.No. 4837 - AZD 3988 | C23H22F2N4O4 | CAS No. 892489-52-0
Description: Potent and selective DGAT-1 inhibitor
Chemical Name: trans-4-[-[[[5-[(3,4-Difluorophenyl)amino]-1,3,4-oxadiazol-2-yl]carbonyl]amino]phenyl]cyclohexaneacetic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Compound Libraries

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Technical Data

M. Wt 456.44
Formula C23H22F2N4O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 892489-52-0
PubChem ID 11676786
InChI Key ZGBGPEDJXCYQPH-UHFFFAOYSA-N
Smiles O=C(NC3=CC=[C@@]([C@H]4CC[C@H](CC(O)=O)CC4)C=C3)C1=NN=C(NC2=CC(F)=C(F)C=C2)O1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.64 100
1eq. NaOH 4.56 10 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 456.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.19 mL 10.95 mL 21.91 mL
5 mM 0.44 mL 2.19 mL 4.38 mL
10 mM 0.22 mL 1.1 mL 2.19 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the biological activity of the product.

McCoull et al (2012) Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes. Bioorg.Med.Chem.Lett. 22 3873 PMID: 22608962


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Literature in this Area

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