GSK-7975A
Based on 12 publication(s) in Google Scholar
GSK-7975A is a potent and orally available CRAC channel inhibitor.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.83%
- CAS No.: 1253186-56-9
- Formule: C18H12F5N3O2
- Masse moléculaire:397.30
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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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Immunology/Inflammation Compound Library
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Neuronal Signaling Compound Library
HY-L013
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Orally Active Compound Library
HY-L061
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Neuroprotective Compound Library
HY-L070
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Calcium Channel Blocker Library
HY-L117
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Antihypertensive Compound Library
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
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Ion Channel Compound Library
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) GSK-7975A
More- Eur J Pharmacol. 2025 Sep 15:1003:177900. [Abstract]
- Front Pharmacol. 2022 Feb 23;13:816133. [Abstract]
- Front Pharmacol. 2021 Jul 14:12:684538. [Abstract]
- Biosci Rep. 2019 Jul 2;39(7):BSR20190516. [Abstract]
- Front Physiol. 2021 Mar 9:12:639857. [Abstract]
- J Cell Physiol. 2021 Sep;236(9):6548-6558. [Abstract]
- Exp Biol Med. 2019 Oct;244(14):1193-1201. [Abstract]
- Biochem Biophys Res Commun. 2025 Sep 19:785:152676. [Abstract]
- bioRxiv. 2024 Dec 23:2024.12.23.629519. [Abstract]
- Heliyon. 2024 Jul 6;10(14):e33994. [Abstract]
- Res Sq. 2024 Jun 11.
- University of Pennsylvania. 2019 Jun.
Voir tous les produits spécifiques à Isoform Calcium Channel
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Activité biologique
GSK-7975A reduces FcεRI-dependent Ca2+ influx and 3 μM GSK-7975A reduces the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50%[1]. GSK-7975A inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety species. GSK-7975A completely inhibits calcium influx through CRAC channels. This leads to inhibition of the release of mast cell mediators and T-cell cytokines from multiple human and rat preparations. Mast cells from guinea-pig and mouse preparations are not inhibited by GSK-7975A; however cytokine release is fully blocked from T-cells in a mouse preparation[2]. GSK-7975A inhibits toxin-induced activation of ORAI1 and/or activation of Ca2+ currents after Ca2+ release, in a concentration-dependent manner, in mouse and human pancreatic acinar cells (inhibition >90% of the levels observed in control cells). GSK-7975A also prevents activation of the necrotic cell death pathway in mouse and human pancreatic acinar cells[3].
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.
Chemical Information
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CAS No. 1253186-56-9
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Appearance Solid
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Masse moléculaire 397.30
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Formule C18H12F5N3O2
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Color White to off-white
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SMILES
O=C(NC1=NN(CC2=CC=C(O)C=C2C(F)(F)F)C=C1)C3=C(F)C=CC=C3F
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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 (12)
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Journal Impact Factor
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Most Recent
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Eur J Pharmacol
Novel mechanisms of metformin-induced vasorelaxation of mesenteric arterioles via endothelium-dependent hyperpolarization to treat murine colitis. [Abstract]2025 Sep 15:1003:177900. PMID: 40617384 -
Front Pharmacol
Ca2+-Permeable Channels/Ca2+ Signaling in the Regulation of Ileal Na+/Gln Co-Transport in Mice. [Abstract]2022 Feb 23;13:816133. PMID: 35281933 -
Front Pharmacol
Role of Serosal TRPV4-Constituted SOCE Mechanism in Secretagogues-Stimulated Intestinal Epithelial Anion Secretion. [Abstract]2021 Jul 14:12:684538. PMID: 34335254 -
Biosci Rep
CaMKII/proteasome/cytosolic calcium/cathepsin B axis was present in tryspin activation induced by nicardipine. [Abstract]2019 Jul 2;39(7):BSR20190516. PMID: 31221819 -
Front Physiol
Cyclopiazonic Acid-Induced Ca2+ Store Depletion Initiates Endothelium-Dependent Hyperpolarization-Mediated Vasorelaxation of Mesenteric Arteries in Healthy and Colitis Mice. [Abstract]2021 Mar 9:12:639857. PMID: 33767636 -
J Cell Physiol
Effects of various calcium transporters on mitochondrial Ca2+ changes and oocyte maturation. [Abstract]2021 Sep;236(9):6548-6558. PMID: 33704771 -
Exp Biol Med
Glucagon-like peptide-1 receptor pathway inhibits extracellular matrix production by mesangial cells through store-operated Ca2+ channel. [Abstract]2019 Oct;244(14):1193-1201. PMID: 31510798 -
Biochem Biophys Res Commun
Glucose transports in the ileum: mechanism, regulation and physiological role of ileal glucose absorption. [Abstract]2025 Sep 19:785:152676. PMID: 41005286 -
bioRxiv
Angiotensin II elicits robust calcium oscillations coordinated within juxtaglomerular cell clusters to suppress renin secretion. [Abstract]2024 Dec 23:2024.12.23.629519. PMID: 39763801 -
Heliyon
N,N,N',N'-Tetrakis(2-pyridylmethyl)ethylenediamine induces endothelium-dependent hyperpolarization-mediated vasorelaxation via store-operated calcium entry mechanism in healthy and intestinal inflammatory mice. [Abstract]2024 Jul 6;10(14):e33994. PMID: 39108891 -
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Solvant et solubilité
DMSO : ≥ 90 mg/mL (226.53 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: ≥ 2.5 mg/mL (6.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Protocole
Mice: Acute pancreatitis is induced in C57BL/6J mice by ductal injection of taurolithocholic acid 3-sulfate or intravenous' administration of cerulein or ethanol and palmitoleic acid. Some mice then are given GSK-7975A, which inhibit ORAI1, at different time points to assess local and systemic effects. Sampling of GSK-7975A is at 1, 2, 4, 10, and 22 hours after osmotic minipump insertion from 3 mice/time point. Immediately after humane killing, blood is collected into a heparinized tube, diluted 1:1 with sterile water, and the pancreas is removed and homogenized. Standards and study samples (50 μL from blood and 100 μL from pancreas) are extracted by protein precipitation and centrifuged. Supernatants are dried under heated nitrogen (40°C). Levels of GSK-7975A and GSK-6288B are determined[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ashmole I, et al. CRACM/Orai ion channel expression and function in human lung mast cells. J Allergy Clin Immunol. 2012 Jun;129(6):1628-35.e2. [Content Brief]
[2]. Rice LV, et al. Characterization of selective Calcium-Release Activated Calcium channel blockers in mast cells and T-cells from human, rat, mouse and guinea-pig preparations. Eur J Pharmacol. 2013 Mar 15;704(1-3):49-57. [Content Brief]
[3]. Wen L, et al. Inhibitors of ORAI1 Prevent Cytosolic Calcium-Associated Injury of Human Pancreatic Acinar Cells and Acute Pancreatitis in 3 Mouse Models. Gastroenterology. 2015 Aug;149(2):481-92.e7. [Content Brief]
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 | 2.5170 mL | 12.5849 mL | 25.1699 mL | 62.9247 mL |
| 5 mM | 0.5034 mL | 2.5170 mL | 5.0340 mL | 12.5849 mL | |
| 10 mM | 0.2517 mL | 1.2585 mL | 2.5170 mL | 6.2925 mL | |
| 15 mM | 0.1678 mL | 0.8390 mL | 1.6780 mL | 4.1950 mL | |
| 20 mM | 0.1258 mL | 0.6292 mL | 1.2585 mL | 3.1462 mL | |
| 25 mM | 0.1007 mL | 0.5034 mL | 1.0068 mL | 2.5170 mL | |
| 30 mM | 0.0839 mL | 0.4195 mL | 0.8390 mL | 2.0975 mL | |
| 40 mM | 0.0629 mL | 0.3146 mL | 0.6292 mL | 1.5731 mL | |
| 50 mM | 0.0503 mL | 0.2517 mL | 0.5034 mL | 1.2585 mL | |
| 60 mM | 0.0419 mL | 0.2097 mL | 0.4195 mL | 1.0487 mL | |
| 80 mM | 0.0315 mL | 0.1573 mL | 0.3146 mL | 0.7866 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2517 mL | 0.6292 mL |
GSK-7975A Related Classifications
HY-12507 Related Classifications
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