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
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
1eq. NaOH 4.56 10mM with gentle warming
DMSO 45.64 100

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.

Select a batch to recalculate based on the batch molecular weight:
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 products' biological activity.

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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View all Diacylglycerol O-Acyltransferase Inhibitors

Keywords: AZD3988 potent selective diacylglycerol transferases DGAT1 inhibitors inhibits obesity orally bioavailable cell permeable Diacylglycerol O-Acyltransferase

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