Zegocractin_product_DataBase

Bioactivity

Zegocractin (CM-4620) is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively[1].

Target

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

Invitro

It is determined that Zegocractin (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, Zegocractin 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 Zegocractin 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. Zegocractin blocks 100% of reuptake at 10 mM[1].

Name

Zegocractin

CAS

1713240-67-5

Formula

C19H11ClF3N3O3

Molar Mass

421.76

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

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

PeptideDB

Zegocractin

CAS: 1713240-67-5 F: C19H11ClF3N3O3 W: 421.76