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GSK-7975A

Catalog No. T15423 CAS 1253186-56-9

GSK-7975A is a potent and orally available inhibitor of CRAC channel.

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GSK-7975A, CAS 1253186-56-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 336.00
50 mg	In stock	$ 542.00
100 mg	In stock	$ 773.00
1 mL * 10 mM (in DMSO)	In stock	$ 107.00

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Purity: 99.78%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK-7975A is a potent and orally available inhibitor of CRAC channel.
In vitro	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 inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety species and it also 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. GSK-7975A decreases FcεRI-dependent Ca2+ influx and 3 μM GSK-7975A decreases the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50%[1]. 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 also prevents activation of the necrotic cell death pathway in mouse and human pancreatic acinar cells[3].
In vivo	GSK-7975A obviously decreses increases in serum amylase, IL6, and pancreatic MPO levels; lung MPO is reduced significantly by low dose only. 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 markedly decreases pancreatic histopathology in TLCS-AP, CER-AP, and FAEE-AP[3].

Molecular Weight	397.3
Formula	C18H12F5N3O2
CAS No.	1253186-56-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (201.36 mM)

References and Literature

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. 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. 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Orally Active Compound Library Anti-Hypertension Compound Library Metabolism Compound Library Ion Channel Inhibitor Library Calcium Channel Compound Library NO PAINS Compound Library Anti-Cardiovascular Disease Compound Library

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Keywords

GSK-7975A 1253186-56-9 Membrane transporter/Ion channel Metabolism Calcium Channel Ca channels GSK 7975A inhibit Inhibitor Ca2+ channels GSK7975A inhibitor

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