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AR-C141990 | AR-C141990 : Inhibitor of SLC16A1
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
SLC16A1
  • Ki:4.8 nM
  • IC50:3.2 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: Exhibits approximately 10-fold selectivity for MCT1 over MCT2 and ...

Potency
Cellular
In Vitro

SLC16A1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2006.01.024

In Vivo Validations

Rat
Dose:
Route of delivery: Intravenous, Oral
Plasma half life: 0.7 h
Systemic clearance: 67 mL/min/Kg
Fb : 60%
Bioavailability: 3%

DOI Reference: 10.1111/j.1432-2277.2012.01579.x

Chemical Information

Molecular Formula C26H28N4O4S
SMILEs CC(C)Cn1c(=O)n(C)c(=O)c2c(C(=O)N3CC[C@@H](O)C3)c(Cc3ccnc4ccccc34)sc21
InChI InChI=1S/C26H28N4O4S/c1-15(2)13-30-25-22(23(32)28(3)26(30)34)21(24(33)29-11-9-17(31)14-29)20(35-25)12-16-8-10-27-19-7-5-4-6-18(16)19/h4-8,10,15,17,31H,9,11-14H2,1-3H3/t17-/m1/s1
Molecular weight 492.18 Da
AlogP 0.0
HBond acceptors 8
HBond donors 1
Atoms 63

Vendors

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Expert Reviews

by SERP
(on 17 Oct 2023 )
Cellular Use Rating
In Model Organisms
This is a potent inhibitor of MCT1 with weaker (by approximately 10-fold) activity against MCT2. The specific on-target activity and possible off-targets have not been exhaustively characterized, but based...
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