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1G244 | 1G244 : Inhibitor of DPP8, DPP9
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
DPP8
  • IC 50:14 nM
  • Ki:0.9 nM DPP8
  • IC50:2.7 uM
  • IC50:320 nM
DPP9
  • IC 50:53 nM
  • Ki:4.2 nM
  • IC50:2.7 uM
Inhibitor
up to 8 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selective over: DPP4 >100,000, FAP >100,000, DPP2 >100,000

Potency
Cellular
In Vitro

DPP8

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.2229

DPP9

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.2229

In Vivo Validations

Rat
Dose: 1, 10, 30 mg/Kg, 1.1 (IV), 2.2 (PO) mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 7 (IV), 1 (PO) h
Systemic clearance: 23.4 (IV) ml/min/Kg

Reference: --

Chemical Information

Molecular Formula C29H30F2N4O2
SMILEs N[C@@H](CC(=O)N1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)C(=O)N1Cc2ccccc2C1
InChI InChI=1S/C29H30F2N4O2/c30-24-9-5-20(6-10-24)28(21-7-11-25(31)12-8-21)34-15-13-33(14-16-34)27(36)17-26(32)29(37)35-18-22-3-1-2-4-23(22)19-35/h1-12,26,28H,13-19,32H2/t26-/m0/s1
Molecular weight 504.23 Da
AlogP 3.4582
HBond acceptors 6
HBond donors 2
Atoms 67

Vendors

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Expert Reviews

by SERP
(on 18 Mar 2024 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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