<Suppliers Price>

CM-4620

Names

[ CAS No. ]:
1713240-67-5

[ Name ]:
CM-4620

[Synonym ]:
Benzamide, N-[5-(6-chloro-2,2-difluoro-1,3-benzodioxol-5-yl)-2-pyrazinyl]-2-fluoro-6-methyl-
N-[5-(6-Chloro-2,2-difluoro-1,3-benzodioxol-5-yl)-2-pyrazinyl]-2-fluoro-6-methylbenzamide
CM-4620

Biological Activity

[Description]:

CM-4620 is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> CRAC Channel
Research Areas >> Neurological Disease

[Target]

IC50: 119 nM (Orai 1/STIM1), 895 nM (Orai 1/STIM1)[1].


[In Vitro]

It is determined that CM-4620 (compound 1) inhibits Orai 1/STIM1 channels with an IC50 of 119 nM, and Orai2/STIM1 channels with an IC50 of 895 nM. It is more potent on Orai1 than Orai2-type CRAC channels. In human PBMCs, CM-4620 potently inhibits release of multiple cytokines which play important roles in T cells (IC50s, IFN γ: 138 nM, IL-4: 879 nM, IL-6: 135 nM, IL-1β: 240 nM, IL-10: 303 nM, TNFα: 225 nM, IL-2: 59 nM, IL-17 120 nM)[1].

[In Vivo]

Mouse PACs are treated with CRAC inhibitors CM-4620 or GSK-7975A and monitored for their rate of Calcium uptake. Both CRAC inhibitors reduce the rate of store-operated Calcium entry into the ER to 50% of controllevels upon treatment with 700 nM of inhibitor. CM-4620 blocks 100% of reuptake at 10 mM[1].

[References]

[1]. ARYL SULFONOHYDRAZIDES. WO2016/138472Al.


[Related Small Molecules]

YM-58483 | GSK-5498A | Synta66 | 4-(3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl)phenylamine | CRAC intermediate 1

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
444.4±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C19H11ClF3N3O3

[ Molecular Weight ]:
421.757

[ Flash Point ]:
222.5±28.7 °C

[ Exact Mass ]:
421.044098

[ LogP ]:
4.93

[ Vapour Pressure ]:
0.0±1.1 mmHg at 25°C

[ Index of Refraction ]:
1.639

[ Storage condition ]:
2-8℃

Related Compounds