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BI-9627 | BI-9627 : Antagonist of SLC9A1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
SLC9A1
  • IC50:6 nM
  • EC50:31 nM
  • EC50:138 nM
Antagonist
up to 5 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Solute carrier family 9 isoform selectivity: > 30-fold selective versus SLC9A2 (IC50 = 231 nM) and > ...

Potency
Cellular
In Vitro

SLC9A1

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm300601d

In Vivo Validations

Rat
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Systemic clearance: 5.7 %QH
Tmax: 3.2 h
Bioavailability: 73%
Volume of Distribution at Steady-State: 0.76 L/kg
Target engagement assay: Efficacious in a rat model of coronary artery ligation at 150 ppm in chow.

DOI Reference: 10.1021/jm300601d

Dose:
Target engagement assay: Efficacious in a rat model of coronary artery ligation at 150 ppm in chow.

DOI Reference: 10.1124/jpet.114.217091

Dog
Dose: 1 mg/Kg IV, 5 mg/Kg PO
Route of delivery: Intravenous, Oral
Systemic clearance: 13 %QH
Tmax: 6.2 h
Bioavailability: 33%
Volume of Distribution at Steady-State: 1.4 L/Kg

DOI Reference: 10.1021/jm300601d

Negative Control Compounds

BI 0054
Notes: pHi change assay: SLC9A1 IC50 > 10 µM; SLC9A2 and SLC9A3 IC50 > 10 µM; hPSA assay: IC50 > 10 µM; Clean GPCR scan with the closest hit on SLC6A3 (pKi = 6.1)

Orthogonal Probes def

d9A-2

Chemical Information

Molecular Formula C16H19F3N4O2
SMILEs CC(=O)N1CCC(c2ccc(C(=O)NC(=N)N)cc2C(F)(F)F)CC1
InChI InChI=1S/C16H19F3N4O2/c1-9(24)23-6-4-10(5-7-23)12-3-2-11(14(25)22-15(20)21)8-13(12)16(17,18)19/h2-3,8,10H,4-7H2,1H3,(H4,20,21,22,25)
Molecular weight 356.15 Da
AlogP 2.05457
HBond acceptors 6
HBond donors 4
Atoms 44

Vendors

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Expert Reviews

by SERP
(on 1 Feb 2022 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 9 Feb 2022 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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