Home / Pharmacology / Enzymes / GTPases / Heterotrimeric G-protein GTPases / Heterotrimeric G-protein GTPase Inhibitors / CMPD101

CMPD101

Cat. No. 5642 7 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective GRK2/3 inhibitor
Chemical Name: 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations (7)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for CMPD101

CMPD101 is a 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 for CMPD101

M. Wt 466.46
Formula C24H21F3N6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 865608-11-3
PubChem ID 11677079
InChI Key WFOVEDJTASPCIR-UHFFFAOYSA-N
Smiles CN1C(CNC2=CC(C(NCC3=CC=CC=C3C(F)(F)F)=O)=CC=C2)=NN=C1C4=CC=NC=C4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for CMPD101

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.65 100
ethanol 46.65 100

Preparing Stock Solutions for CMPD101

The following data is based on the product molecular weight 466.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.14 mL 10.72 mL 21.44 mL
5 mM 0.43 mL 2.14 mL 4.29 mL
10 mM 0.21 mL 1.07 mL 2.14 mL
50 mM 0.04 mL 0.21 mL 0.43 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets for CMPD101

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References for CMPD101

References are publications that support the biological activity of the product.

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

Okawa et al (2017) Design, synthesis, and evaluation of the highly selective and potent G-protein-coupled receptor kinase 2 (GRK2) inhibitor for the potential treatment of heart failure. J.Med.Chem. 60 6942 PMID: 28699740

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

View Related Products by Target

View Related Products by Product Action

View all Heterotrimeric G-protein GTPase Inhibitors

Keywords: CMPD101, CMPD101 supplier, potent, selective, GRK2, GRK3, inhibitors, inhibits, receptors, GPCRs, desensitization, kinases, Heterotrimeric, G-protein, GTPases, 5642, Tocris Bioscience

7 Citations for CMPD101

Citations are publications that use Tocris products. Selected citations for CMPD101 include:

Francesco Luigi et al (2023) Subcellular location defines GPCR signal transduction. Sci Adv 9 eadf6059 PMID: 37075112

Reyes-Alcaraz et al (2018) Conformational signatures in β-arrestin2 reveal natural biased agonism at a G-protein-coupled receptor. Commun Biol 1 128 PMID: 30272007

Joshua et al (2021) Mechanisms of differential desensitization of metabotropic glutamate receptors. Cell Rep 35 109050 PMID: 33910009

Dominique et al (2021) Biological characterization of ligands targeting the human CC chemokine receptor 8 (CCR8) reveals the biased signaling properties of small molecule agonists. Biochem Pharmacol 188 114565 PMID: 33872569

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

Reviews for CMPD101

There are currently no reviews for this product. Be the first to review CMPD101 and earn rewards!

Have you used CMPD101?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review