Zegocractin
Based on 17 publication(s) in Google Scholar
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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- Pureté: 99.96%
- CAS No.: 1713240-67-5
- Formule: C19H11ClF3N3O3
- Masse moléculaire:421.76
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Publications Citing Use of MedChemExpress (MCE) Zegocractin
More- Nat Aging. 2023 Jul;3(7):796-812. [Abstract]
- Nat Commun. 2023 Mar 8;14(1):1286. [Abstract]
- Cell Commun Signal. 2024 Feb 1;22(1):92. [Abstract]
- Cell Rep. 2026 Jan 22;45(2):116903. [Abstract]
- J Med Chem. 2025 Apr 17. [Abstract]
- J Invest Dermatol. 2024 Apr;144(4):811-819.e4. [Abstract]
- Life Sci. 2021 Sep 1:280:119699. [Abstract]
- Am J Physiol Cell Physiol. 2025 Apr 29. [Abstract]
- Pancreatology. 2024 Jun;24(4):528-537. [Abstract]
- PLoS One. 2024 Jan 23;19(1):e0296065. [Abstract]
- Biochem Biophys Res Commun. 2025 Mar 19:753:151510. [Abstract]
- Patent. US20250312336A1.
- Patent. US20250230435A1.
- Elife. 2023 Dec 6:12:RP88874. [Abstract]
- bioRxiv. 2023 Sep 17:2023.09.15.557802. [Abstract]
- bioRxiv. 2023 Jun 6.
- Humboldt university. 2023 Jan 27.
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Activité biologique
IC50: 119 nM (Orai 1/STIM1), 895 nM (Orai 1/STIM1)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1713240-67-5
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Appearance Solid
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Masse moléculaire 421.76
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Formule C19H11ClF3N3O3
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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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Synonyms
CM-4620
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (17)
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Journal Impact Factor
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Most Recent
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Nat Aging
2023 Jul;3(7):796-812. PMID: 37277641 -
Nat Commun
2023 Mar 8;14(1):1286. PMID: 36890174
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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Cell Commun Signal
T-type voltage-gated channels, Na+/Ca2+-exchanger, and calpain-2 promote photoreceptor cell death in inherited retinal degeneration. [Abstract]2024 Feb 1;22(1):92. PMID: 38303059
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.
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Cell Rep
A shear stress-responsive pathway in monocytes drives cardiopulmonary bypass-induced inflammation via spectrin/RAF1/store-operated calcium entry. [Abstract]2026 Jan 22;45(2):116903. PMID: 41579376
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.
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J Med Chem
A Novel Compound 3a-M1, from Metabolites of Sinomenine Derivative 3a, Exerts Potent Anti-Aplastic Anemia Activity via IP3R/ORAI-Mediated CTL Ferroptosis. [Abstract]2025 Apr 17. PMID: 40243551 -
J Invest Dermatol
GNAQ/GNA11 mosaicism causes aberrant calcium signalling susceptible to targeted therapeutics. [Abstract]2024 Apr;144(4):811-819.e4. PMID: 37802293 -
Life Sci
The role of STIM1/ORAI1 channel in the analgesic effect of grain-sized moxibustion on inflammatory pain mice model. [Abstract]2021 Sep 1:280:119699. PMID: 34102196 -
Am J Physiol Cell Physiol
Orai channel pharmacological manipulation reduces metabolic flexibility in cardiac fibroblasts. [Abstract]2025 Apr 29. PMID: 40298968 -
Pancreatology
Deletion of myeloid-specific Orai1 calcium channel does not affect pancreatic tissue damage in experimental acute pancreatitis. [Abstract]2024 Jun;24(4):528-537. PMID: 38637233 -
PLoS One
Side-by-side comparison of published small molecule inhibitors against thapsigargin-induced store-operated Ca2+ entry in HEK293 cells. [Abstract]2024 Jan 23;19(1):e0296065. PMID: 38261554 -
Biochem Biophys Res Commun
2025 Mar 19:753:151510. PMID: 39986091 -
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Elife
Sustained store-operated calcium entry utilizing activated chromatin state leads to instability in iTregs. [Abstract]2023 Dec 6:12:RP88874. PMID: 38055613 -
bioRxiv
Trogocytosis of cancer-associated fibroblasts promotes pancreatic cancer growth and immune suppression via phospholipid scramblase anoctamin 6 (ANO6). [Abstract]2023 Sep 17:2023.09.15.557802. PMID: 37745612 -
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Solvant et solubilité
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
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 |
|---|---|---|---|---|---|
| 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
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