GSK-7975A

SKU: orb1308255

Description

GSK-7975A is a cell-permeable, selective CRAC channel blocker suitable for oral administration in research. It is widely used in vitro and in vivo to investigate calcium signaling in immune cells, with applications in studying T-cell activation and related inflammatory pathways.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1253186-56-9
• MW: 397.3
• Purity: 99.78% (May vary between batches)
• Formula: C₁₈H₁₂F₅N₃O₂
• SMILES: Oc1ccc(Cn2ccc(NC(=O)c3c(F)cccc3F)n2)c(c1)C(F)(F)F
• Target: Calcium Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (8.31 mM);DMSO:80 mg/mL (201.36 mM)

Bioactivity

• 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.
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• 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%. 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. GSK-7975A also prevents activation of the necrotic cell death pathway in mouse and human pancreatic acinar cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CRAC channel, CalciumChannel, Ca2+ channels, Calcium Channel, Ca channels, Inhibitor, GSK7975A, GSK-7975A, GSK 7975A, inhibit

Compound Identifiers

PubChem CID

59547990