Bioactivity | AZD3988 is an orally active diacylglycerol acyl transferase-1 (DGAT-1) inhibitor. AZD3988 has excellent DGAT-1 (human) potency with an IC50 value of 0. 6 nM. AZD3988 can be used for the research of metabolic diseases such as diabetes, obesity[1]. | ||||||||||||
Target | IC50: 0.6 nM (h DGAT-1), 0.5 nM (Rat DGAT-1), 1.1 nM (Mouse DGAT-1) | ||||||||||||
Invitro | AZD3988 (compound 53) (10 μM) can inhibit DGAT-1 with IC50 values of 0. 6 nM (human), 0. 5nM (rat), 1.1 nM (mouse) and 0.5 nM (HuTu 80 cell), respectively[1]. | ||||||||||||
In Vivo | AZD3988 (compound 53) shows (i.v., p.o.; 0.5, 1, 2, 5 mg/kg) has good pharmacokinetics in vivo efficacy[1]. Animal Model: | ||||||||||||
Name | AZD3988 | ||||||||||||
CAS | 892489-52-0 | ||||||||||||
Formula | C23H22F2N4O4 | ||||||||||||
Molar Mass | 456.44 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. McCoull W, et al. Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3873-8. |