Zegocractin [1713240-67-5]
Référence HY-101942-10mg
Conditionnement : 10mg
Marque : MedChemExpress
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CM-4620 est un inhibiteur de canal calcique activé par le calcium (canal CRAC), avec des IC50s de 119 nM et 895 nM pour Orai1/STIM1 et Orai2/STIM1 canaux, respectivement.
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.
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Zegocractin Chemical Structure
CAS No. : 1713240-67-5
This product is a controlled substance and not for sale in your territory.
Based on 10 publication(s) in Google Scholar
| Description |
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]. |
IC50 & Target |
IC50: 119 nM (Orai 1/STIM1), 895 nM (Orai 1/STIM1)[1] |
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| 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. |
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| 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. |
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| Essai clinique |
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| Masse moléculaire |
421.76 |
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| Formule |
C19H11ClF3N3O3 |
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| CAS No. |
1713240-67-5 |
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| Unlabeled CAS |
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| Appearance |
Solid |
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| Color |
White to off-white |
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| 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 |
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| Livraison | Room temperature in continental US; may vary elsewhere. |
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| Stockage |
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| Solvant et solubilité |
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
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.
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 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:
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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.
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| Pureté et documentation |
Purity: 99.93% |
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| Références |
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 |