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AZD3988

SKU: orb2901624

Description

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.

Images & Validation

Key Properties

CAS Number892489-52-0
MW456.44
Purity>98% (HPLC)
FormulaC23H22F2N4O4
SMILESOC(=O)C[C@H]1CC[C@@H](CC1)c1ccc(NC(=O)c2nnc(Nc3ccc(F)c(F)c3)o2)cc1
TargetTransferase
SolubilityIn Vitro: DMSO : 16.67 mg/mL (36.52 mM; Ultrasonic )

Bioactivity

In Vivo
AZD3988 (compound 53) shows (i. v. , p.o. ; 0.5, 1, 2, 5 mg/kg) has good pharmacokinetics In vivo efficacy. Animal model: Mouse, Rats and Dog. Dosage: 0.5, 1, 2, 5 mg/kg. Administration: IV at 0.5 mg/kg (mouse), 2 mg/kg (rat) and 1 mg/kg (dog) and po at 1 mg/kg (mouse), 5 mg/kg(rat) and 1 mg/kg (dog).
In Vitro
AZD3988 (compound 53) (10 μM) can inhibit DGAT-1 with IC50 values of0. 6 nM (human), 0. 5 nM (rat), 1.1 nM (mouse) and 0.5 nM (HuTu 80 cell), respectively.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Protocol Information