CMPD101

Cat. No. 5642

CMPD101 C24H21F3N6O [865608-11-3]

Price and Availability

For CMPD101 pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Chemical Name: 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide

Biological Activity

Potent and selective GRK2/3 inhibitor (IC50 values are 32 and 54 nM for GRK3 and GRK2, respectively). Exhibits selectivity for GRK2/3 over GRK1/5. Reduces DAMGO-induced desensitization and internalization of μ-opioid receptors.

Technical Data

M.Wt:
466.46
Formula:
C24H21F3N6O
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
865608-11-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Lowe et al (2015) Role of G protein-coupled receptor kinases 2 and 3 in μ-opioid receptor desensitization and internalization. Mol.Pharmacol. 88 347. PMID: 26013542.

Thal et al (2011) Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol.Pharmacol. 80 294. PMID: 21596927.

If you know of a relevant reference for CMPD101 please let us know.

Citations are publications that use Tocris products.

Do you know of a great paper that uses CMPD101 from Tocris? If so please let us know.

View Related Products by Target

View Related Products by Product Action

Keywords: CMPD101, supplier, potent, selective, GRK2, GRK3, inhibitors, inhibits, receptors, GPCRs, desensitization, kinases, Tocris Bioscience, G Protein (Heterotrimeric) Inhibitor products

Quick Order

Find multiple products by catalog number

divider line

Cancer Research Product Guide

Cancer Research Product Guide

Our Cancer Research Guide highlights over 750 products for cancer research. Request copy or view PDF today.

divider line

Pain Research Product Guide

Pain Research Product Guide

Our Pain guide highlights over 280 products for Pain research. Request copy or view PDF today.

divider line

New Products in this Area

TAT-Gap19

Cx43 hemichannel blocker

WL 47 - dimer

High affinity caveolin-1 ligand

Sign-up for new product e-alerts
divider line

Bio-Techne Events

WCI 2017

13th World Congress on Inflammation

July 8 - 12, 2017

London, UK