MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.

Product information

CAS Number: 1263131-92-5

Molecular Weight: 538.59

Formula: C31H30N4O5

Chemical Name: N-[2-methyl-5-({[(3,4,5-trimethoxyphenyl)formamido]methanimidoyl}amino)phenyl]-[1,1'-biphenyl]-4-carboxamide

Smiles: CC1C=CC(=CC=1NC(=O)C1C=CC(=CC=1)C1C=CC=CC=1)NC(=N)NC(=O)C1=CC(OC)=C(OC)C(=C1)OC

InChiKey: BKTMNLKJWHVZRN-UHFFFAOYSA-N

InChi: InChI=1S/C31H30N4O5/c1-19-10-15-24(33-31(32)35-30(37)23-16-26(38-2)28(40-4)27(17-23)39-3)18-25(19)34-29(36)22-13-11-21(12-14-22)20-8-6-5-7-9-20/h5-18H,1-4H3,(H,34,36)(H3,32,33,35,37)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

Products are for research use only. Not for human use.