• USA Home
  • SML2784 - CMPD101 hydrochloride

EMAIL THIS PAGE TO A FRIEND
SML2784 Sigma-Aldrich

CMPD101 hydrochloride

≥98% (HPLC)

Synonym: 3-((4-Methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methylamino)-N-(2-(trifluoromethyl)benzyl)benzamide, 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide hydrochloride, Compound 101 hydrochloride, Cpd101 hydrochloride, Takeda101 hydrochloride

  • CAS Number 1941168-71-3

  • Empirical Formula (Hill Notation) C24H21N6OF3 · HCl

  • Molecular Weight 502.92

Purchase

Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, CI-CZ, Cell Biology
Quality Level   100
assay   ≥98% (HPLC)
form   powder
storage condition   desiccated
color   white to beige
solubility   DMSO: 2 mg/mL, clear
storage temp.   2-8°C
SMILES string   CN1C(CNC2=CC=CC(C(NCC3=CC=CC=C3C(F)(F)F)=O)=C2)=NN=C1C4=CC=NC=C4.Cl

Description

Biochem/physiol Actions

CMPD101 is an active site-targeting, potent and subtype-selective G protein-coupled receptor kinase GRK2 & GRK3 inhibitor (human GRK2/3 IC50 = 54/32 nM with 3 μM ATP and tubulin dimer as substrate; bovine GRK2 IC50 = 290 nM with 0.5 mM ATP and bROS as substrate; no GRK1/5 inhibition at 125 μM). CMPD101 selectively inhibits GPR39 agonist-induced β-arrestin recruitment (by 94% at 10 μM against 30 μM GPR39-C3/50 μM ZnCl2), but not cAMP pathway desensitization in cultures and prevents β-arrestin2-biased D2R ligand UNC9994(1 μg/side bilateral local injection) from blocking NMDAR antagonist PCP (6 mg/kg i.p.)-induced locomotion (60%/12% blockage without/with 0.5 μg CMPD101 co-injection) in mice in vivo.

Safety & Documentation

Safety Information

WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

Please Enter a Lot Number
Protocols & Articles
Peer-Reviewed Papers
15

References

Related Products

Technical Service:

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Bulk Ordering & Pricing:

Need larger quantities for your development, manufacturing or research applications?