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SKF96365 TRP Channel inhibitor

Cat.No.S7999

SKF96365, originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels.
SKF96365 TRP Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 402.91

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Quality Control

Batch: Purity: 99.54%
99.54

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (198.55 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 80 mg/mL

Ethanol : 80 mg/mL

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 402.91 Formula

C22H26N2O3.HCl

Storage (From the date of receipt)
CAS No. 130495-35-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC=C(C=C1)CCCOC(CN2C=CN=C2)C3=CC=C(C=C3)OC.Cl

Mechanism of Action

Targets/IC50/Ki
TRPC
In vitro
SKF-96365 exhibits protective activity against MPP+ injury in PC12 cells and significantly inhibits apoptotic cell death in PC12 cells after MPP+ administration. SKF-96365 does not exert effects on necrotic cell death induced by MPP+ insult in PC12 cells. Because of its non-selective activity, SKF-96365 has been demonstrated to have effects on multiple other Ca2+ channels: it not only blocks high-voltage-activated (HVA) Ca2+ channels at typically utilized test concentrations, but also potently inhibits low-voltage -activated (LVA) T-type Ca2+ channels in HEK293 cells. The exact effect of SKF-96365 on intracellular calcium homeostasis might dependent on cell types and experimental models used.
In vivo
SKF-96365 treatment inhibited the calcium/calmodulin-dependent protein kinase IIγ (CaMKIIγ)/AKT signaling cascade in vitro and in vivo.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/26803057/

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