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AZD3988 | Inhibitor of DGAT1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DGAT1
  • IC50:0.6 nM
  • IC50:0.5 nM
  • IC50:1.1 nM
  • IC50:0.5 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - ACAT1 86 nM, ACAT2 600 nM

Potency Assay Off-Target:
Enzymatic Activity
Selectivity Assessment Description:
no significant activity against DGAT-2, the hERG encoded potassium channel (>30 μM), and cytoc ...

Potency
Cellular
In Vitro

DGAT1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.bmcl.2012.04.117

In Vivo Validations

Mouse, Rat, Dog
Dose: 0.5 (M), 2 (R), 1 (D) mg/kg IV, 1 (M), 5 (R), 1 (D) mg/kg PO, Reviewer suggest: 20 mg/Kg (M), 0.5-5 mg/Kg (R)
Route of delivery: Intravenous, Oral
Plasma half life: 4.9 (M), 3.4 (R), 1.8 (D) h (IV), 4.7 (M), 5.8 (R), 5.7 (D) h (PO)
Systemic clearance: 4.6 (M), 1.1 (R), 2.5 (D) mL/min/kg

DOI Reference: 10.1016/j.bmcl.2012.04.117

Orthogonal Probes def

GSK2973980A

Chemical Information

Molecular Formula C23H22F2N4O4
SMILEs O=C(O)C[C@H]1CC[C@H](c2ccc(NC(=O)c3nnc(Nc4ccc(F)c(F)c4)o3)cc2)CC1
InChI InChI=1S/C23H22F2N4O4/c24-18-10-9-17(12-19(18)25)27-23-29-28-22(33-23)21(32)26-16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-20(30)31/h5-10,12-14H,1-4,11H2,(H,26,32)(H,27,29)(H,30,31)/t13-,14-
Molecular weight 456.16 Da
AlogP 0.0
HBond acceptors 8
HBond donors 3
Atoms 55

Vendors

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Expert Reviews

by SERP
(on 18 Dec 2020 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 7 Jan 2021 )
Cellular Use Rating
In Model Organisms
Overall, AZD3988 has very favourable probe properties to study DGAT-1. The probe shows a clear mechanism of action and engages with the target at low nanomolar concentrations, exhibits selectivity for...
by SERP
(on 18 Feb 2021 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria