Zegocractin (Synonyms: CM-4620)

Name: Zegocractin
Brand: MedChemExpress
SKU: HY-101942
Rating: 5.0 (17 reviews)

Cat. No.: HY-101942 Purity: 99.96%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 1713240-67-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Zegocractin:

Zegocractin (Standard) Get quote

17 Publications Citing Use of MCE Zegocractin

Bio/Physico-chemical Assay

Cell Imaging/Staining

Others

Histological Imaging/Staining

: Zegocractin purchased from MedChemExpress. Usage Cited in: Cell Rep. 2026 Jan 22;45(2):116903. [Abstract]; Schematic of drug treatment experiments. Whole blood from healthy donors (n = 3) was incubated in 6-well suspension culture plates with 5 μM sorafenib, 1 μM BVD-523, 5 μM Zegocractin (CM4620), or DMSO control for 1 h prior to being sheared for 2 h. DMSO-treated blood samples under static conditions were used as controls. PBMCs were isolated for scRNA-seq.

: Zegocractin purchased from MedChemExpress. Usage Cited in: Cell Rep. 2026 Jan 22;45(2):116903. [Abstract]; Feature maps of IL8 expression in classical monocytes across five conditions: static, shear stress, sorafenib + shear, BVD-523 + shear, and Zegocractin (CM4620) + shear, respectively.

: Zegocractin purchased from MedChemExpress. Usage Cited in: Cell Rep. 2026 Jan 22;45(2):116903. [Abstract]; Violin plots show that BVD-523 and Zegocractin (CM4620) downregulated shear stress-induced IL8 expression in monocytes by 29.8% (adjusted p = 0.0001) and 35.4% (adjusted p = 1.16 × 10−18), respectively, as compared to DMSO sheared samples.

: Zegocractin purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Feb 1;22(1):92. [Abstract]; TUNEL assay labelling dying cells (magenta) in rd1 and wild-type (wt) retinal explant cultures. DAPI (grey) was used as a nuclear counterstain. Untreated (Untr.) wt and rd1 retina were compared to retina treated with 50 µM CNGC inhibitor (L-cis diltiazem), 20 µM Zegocractin (CM4620), 40 µM NCX inhibitor (SN-6), 100 µM L-type VGCC inhibitor (D-cis diltiazem), 10 µM T-type VGCC inhibitor (TTA-A2), and 15 µM α2δ subunit VGCC ligand (DS5565). Scatter plot showing percent TUNEL-positive cells in outer nuclear layer (ONL).

: Zegocractin purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Feb 1;22(1):92. [Abstract]; PAR staining (black) was performed in rd1 and wt retinal explant cultures. Untreated wt and rd1 retina were compared to drug-treated retina as in A. Untr. wt: n = 6; Untr. rd1: 17; BAPTA rd1: 7; L-cis rd1: 7; Zegocractin (CM4620) rd1: 10; SN-6 rd1: 8; D-cis rd1: 8; TTA-A2 rd1: 8; DS5565 rd1: 8; NA-184 rd1: 9.

: Zegocractin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Mar 8;14(1):1286. [Abstract]; Time courses of Ca²⁺ current-densities after whole-cell break-in of Orai1 A137Bpa, Orai1 L174Bpa and Orai1 A254Azi exposed to UV-light (15 s) compared to STIM1/Orai1 currents activated by passive store-depletion. After maximal activation the Orai1 channel blocker Zegocractin (CM-4620, 10 µM) was applied.

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Description

IC₅₀ & Target

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

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

421.76

Formula

C₁₉H₁₁ClF₃N₃O₃

CAS No.

1713240-67-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NC=C(C2=C(Cl)C=C(OC(F)(F)O3)C3=C2)N=C1)C4=C(C)C=CC=C4F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (237.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3710 mL	11.8551 mL	23.7102 mL
5 mM	0.4742 mL	2.3710 mL	4.7420 mL
10 mM	0.2371 mL	1.1855 mL	2.3710 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (4.93 mM); Suspended solution; Need ultrasonic and warming

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.93 mM); Suspended solution; Need ultrasonic and warming

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 70% PEG300 30% (20% SBE-β-CD in Saline)
Solubility: 10 mg/mL (23.71 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (273 KB) SDS (392 KB)

COA (248 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3710 mL	11.8551 mL	23.7102 mL	59.2754 mL
	5 mM	0.4742 mL	2.3710 mL	4.7420 mL	11.8551 mL
	10 mM	0.2371 mL	1.1855 mL	2.3710 mL	5.9275 mL
	15 mM	0.1581 mL	0.7903 mL	1.5807 mL	3.9517 mL
	20 mM	0.1186 mL	0.5928 mL	1.1855 mL	2.9638 mL
	25 mM	0.0948 mL	0.4742 mL	0.9484 mL	2.3710 mL
	30 mM	0.0790 mL	0.3952 mL	0.7903 mL	1.9758 mL
	40 mM	0.0593 mL	0.2964 mL	0.5928 mL	1.4819 mL
	50 mM	0.0474 mL	0.2371 mL	0.4742 mL	1.1855 mL
	60 mM	0.0395 mL	0.1976 mL	0.3952 mL	0.9879 mL
	80 mM	0.0296 mL	0.1482 mL	0.2964 mL	0.7409 mL
	100 mM	0.0237 mL	0.1186 mL	0.2371 mL	0.5928 mL

Zegocractin Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zegocractin1713240-67-5CM-4620CM4620CM 4620CRAC ChannelCalcium release-activated channelsCa2+ release-activated Ca2+ channelsInhibitorinhibitorinhibit

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Zegocractin (Synonyms: CM-4620)

Customer Review

Other Forms of Zegocractin:

Zegocractin Related Antibodies

17 Publications Citing Use of MCE Zegocractin

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Zegocractin Related Antibodies

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Complete Stock Solution Preparation Table

Zegocractin Related Classifications

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