GSK-7975A

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 5mg
ArtNr HY-12507-5mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
CAS
1253186-56-9
MWt
397.2988
Formula
C18H12F5N3O2
Solubility
DMSO
Clinical_Information
No Development Reported
Pathway
Membrane Transporter/Ion Channel
Target
Calcium Channel
Biological Activity
GSK-7975A is a potent and orally available CRAC channel inhibitor.
In Vitro: GSK-7975A reduces FcepsilonRI-dependent Ca2+ influx and 3 uM GSK-7975A reduces the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFalpha) 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].
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].
Menge: 5mg
Lieferbar: In stock
Listenpreis: 166,79 €
Preis: 166,79 €
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