MRT-83
Names
[ CAS No. ]:
1263131-92-5
[ Name ]:
MRT-83
[Synonym ]:
Benzamide, N-[[[3-[([1,1'-biphenyl]-4-ylcarbonyl)amino]-4-methylphenyl]amino]iminomethyl]-3,4,5-trimethoxy-
N-{2-Methyl-5-[N'-(3,4,5-trimethoxybenzoyl)carbamimidamido]phenyl}-4-biphenylcarboxamide
Biological Activity
[Description]:
MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range.
[Related Catalog]:
[Target]
Smo[1].
[In Vitro]
MRT-83 displays full antagonist properties with an IC50 (~3 nM) for inhibiting ShhN (3 nM)-induced proliferation of rat GCPs. MRT-83 also blocks SAG (0.01 μM)-induced proliferation of GCPs (IC50 ~6 nM). MRT-83 blocks BC binding to HEK-hSmo cells in a dose-dependent manner with an IC50 of 4.6 nM. MRT-83 abrogates BC binding to cells expressing mouse Smo with an IC50 of 14 nM, which is in good correlation with its IC50 in the Shh-light2 and alkaline phosphatase assays[1].
[In Vivo]
Animals treated with ShhN in the presence of MRT-83 are as healthy as those of the other groups but up-regulation of Ptc transcription in the SVZ of these animals is no longer observed in agreement with a complete inhibition of ShhN-mediated effects (8.7±2.4 Ptc+ cells/section, n=9) and is not different from vehicle-mediated effects. MRT-83 but not MRT-36 antagonizes the up-regulation of Ptc transcription induced by ShhN in vivo in the SVZ of the LV[1].
[Animal admin]
Mice[1] Four groups of six animals received 5 μL of 45% 2-hydroxypropyl-β-cyclodextrin PBS solution containing 0.9 μg of ShhN alone or in the presence of MRT-83 (200 ng) or MRT-36 (110 ng). A control group receive 5 μL of 45% 2-hydroxypropyl-β-cyclodextrin solution alone. All groups are analyzed 48 h after the injection[1]
[References]
[Related Small Molecules]
SAG.HCI
|
Purmorphamine
|
LDE225 (NVP-LDE225,Erismodegib)
|
PF-04449913
|
Jervine
|
LY2940680
|
BMS-833923
|
LEQ506
|
MK-4101
|
PF-5274857
|
Saridegib
Chemical & Physical Properties
[ Density]:
1.2±0.1 g/cm3
[ Molecular Formula ]:
C31H30N4O5
[ Molecular Weight ]:
538.594
[ Exact Mass ]:
538.221619
[ LogP ]:
5.23
[ Index of Refraction ]:
1.608
[ Storage condition ]:
2-8℃