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Biological Activity for AZD 3988
AZD 3988 is a 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.
Sold with the permission of AstraZeneca UK Ltd.
Compound Libraries for AZD 3988
Technical Data for AZD 3988
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AZD 3988
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|1eq. NaOH||4.56||10 with gentle warming|
Preparing Stock Solutions for AZD 3988
The following data is based on the product molecular weight 456.44. Batch specific molecular weights may vary from batch to batch due to the degree 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|
References for AZD 3988
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
If you know of a relevant reference for AZD 3988, please let us know.
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3 Citations for AZD 3988
Citations are publications that use Tocris products. Selected citations for AZD 3988 include:
Mahoney et al (2019) A chemical biology screen identifies a vulnerability of neuroendocrine cancer cells to SQLE inhibition. Nat Commun 10 96 PMID: 30626880
Benedikt M et al (2019) A Novel Role for Triglyceride Metabolism in Foxp3 Expression. Front Immunol 10 1860 PMID: 31456800
Andris et al (2022) Oxidative stress from DGAT1 oncoprotein inhibition in melanoma suppresses tumor growth when ROS defenses are also breached. Cell Rep 39 110995 PMID: 35732120
Do you know of a great paper that uses AZD 3988 from Tocris? Please let us know.
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