GSK-7975A [1253186-56-9]
Cat# HY-12507-5mg
Size : 5mg
Brand : MedChemExpress
GSK-7975A is a potent and orally available CRAC channel inhibitor.
For research use only. We do not sell to patients.
GSK-7975A Chemical Structure
CAS No. : 1253186-56-9
This product is a controlled substance and not for sale in your territory.
Based on 8 publication(s) in Google Scholar
Description |
GSK-7975A is a potent and orally available CRAC channel inhibitor. |
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In Vitro |
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. |
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In Vivo |
GSK-7975A inhibits local and systemic features of acute pancreatitis in TLCS-AP, CER-AP, FAEE-AP, in dose- and time-dependent manners. GSK-7975A significantly reduces increases in serum amylase, IL6, and pancreatic MPO levels; lung MPO is reduced significantly by low dose only. GSK-7975A markedly reduces pancreatic histopathology in TLCS-AP, CER-AP, and FAEE-AP[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Molecular Weight |
397.30 |
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Formula |
C18H12F5N3O2 |
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CAS No. |
1253186-56-9 |
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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=NN(CC2=CC=C(O)C=C2C(F)(F)F)C=C1)C3=C(F)C=CC=C3F |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
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. 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:
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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Purity & Documentation |
Purity: 99.79% |
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References |
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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 | 2.5170 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 |