SKF-96365 (hydrochloride)

SKF-96365 (hydrochloride) - Names and Identifiers

Name	1-(2-(4-methoxyphenyl)-2-(3-(4-methoxyphenyl)propoxy)ethyl)-1H-imidazole hydrochloride
Synonyms	SKF 96365 SKF-96365, HCl SK AND F 96365 SKF 96365 HYDROCHLORIDE SKF-96365 (hydrochloride) 1-[BETA-[3-(4-METHOXYPHENYL)PROPOXY]-4-METHOXYPHENETHYL]-1H-IMIDAZOLE HCL 1-[β-(3-(4-methoxyphenyl)propoxy)-4-methoxyphenethyl]-1h-imidazole hydrochloride 1-(BETA-[3-(4-METHOXYPHENYL)PROPOXY]-4-METHOXYPHENETHYL)-1H-IMIDAZOLE HYDROCHLORIDE 1-(2-(4-methoxyphenyl)-2-(3-(4-methoxyphenyl)propoxy)ethyl)-1H-imidazole hydrochloride 1-[2-(4-METHOXYPHENYL)-2-[3-(4-METHOXYPHENYL)PROPOXY]ETHYL]-1H-IMIDAZOLE HYDROCHLORIDE
CAS	130495-35-1

SKF-96365 (hydrochloride) - Physico-chemical Properties

Molecular Formula	C22H27ClN2O3
Molar Mass	402.91
Melting Point	119 °C
Water Solubility	Soluble to 100mM in water
Solubility	Soluble in DMSO, not in water
Appearance	solid
Color	white
Storage Condition	Inert atmosphere,Room Temperature
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
Use	SKF-96365 is a selective TRPC channel blocker. SKF-96365 activates cytoprotective autophagy to delay apoptosis in colorectal cancer cells through inhibition of the calcium/CaMKIIγ/AKT-mediated pathway. SKF-96365 strongly inhibits voltage-gated sodium current in rat ventricular myocytes. SKF 96365 inhibits glioblastoma cell growth by enhancing reverse mode of the Na(+) /Ca(2+) exchanger and increasing intracellular Ca(2+). SKF-96365 attenuates toxin-induced neuronal injury through opposite regulatory effects on Homer1a and Homer1b/c in cultured rat mesencephalic cells.
Target	TRP
In vitro study	SKF-96365 has anti-injury activity against MPP injury in PC12 cells, which can significantly inhibit apoptotic cell death after MPP application. SKF-96365 had no effect on the necrotic cell death induced by MPP. Because of the non-selective activity, SKF-96365 plays a lease on a variety of calcium ion channels: It not only inhibits high voltage activated calcium channels, but also effectively inhibits low voltage activated T-type calcium channels in HEK293 cells. SKF-96365 the specific effect on intracellular calcium homeostasis is determined by cell type and experimental model.
In vivo study	In in vitro and in vivo experiments, SKF-96365 treatment inhibited the calcium/calmodulin-dependent protein kinase II gamma (CaMKII gamma)/AKT signaling cascade.

SKF-96365 (hydrochloride) - Risk and Safety

Hazard Symbols	Xi - Irritant
Risk Codes	36/37/38 - Irritating to eyes, respiratory system and skin.
Safety Description	S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing.
WGK Germany	3
RTECS	NI6823500

SKF-96365 (hydrochloride) - Reference

Reference

1: Cheng H, Curtis AE, Fellingham C, Hancox JC. Multiple ion channel block by the cation channel inhibitor SKF-96365 in myocytes from the rabbit atrioventricular node. Physiol Rep. 2016 Jun;4(11). pii: e12819. doi: 10.14814/phy2.12819. PubMed PMID: 27288059.
2: Jing Z, Sui X, Yao J, Xie J, Jiang L, Zhou Y, Pan H, Han W. SKF-96365 activates cytoprotective autophagy to delay apoptosis in colorectal cancer cells through inhibition of the calcium/CaMKIIγ/AKT-mediated pathway. Cancer Lett. 2016 Mar 28;372(2):226-38. doi: 10.1016/j.canlet.2016.01.006. Epub 2016 Jan 20. PubMed PMID: 26803057.
3: Liu H, Yang L, Chen KH, Sun HY, Jin MW, Xiao GS, Wang Y, Li GR. SKF-96365 blocks human ether-à-go-go-related gene potassium channels stably expressed in HEK 293 cells. Pharmacol Res. 2016 Feb;104:61-9. doi: 10.1016/j.phrs.2015.12.012. Epub 2015 Dec 12. PubMed PMID: 26689773.
4: Bencze M, Behuliak M, Vavřínová A, Zicha J. Broad-range TRP channel inhibitors (2-APB, flufenamic acid, SKF-96365) affect differently contraction of resistance and conduit femoral arteries of rat. Eur J Pharmacol. 2015 Oct 15;765:533-40. doi: 10.1016/j.ejphar.2015.09.014. Epub 2015 Sep 16. PubMed PMID: 26384458.
5: Chen KH, Liu H, Yang L, Jin MW, Li GR. SKF-96365 strongly inhibits voltage-gated sodium current in rat ventricular myocytes. Pflugers Arch. 2015 Jun;467(6):1227-36. doi: 10.1007/s00424-014-1565-4. Epub 2014 Jul 15. PubMed PMID: 25017106.
6: Song M, Chen D, Yu SP. The TRPC channel blocker SKF 96365 inhibits glioblast

SKF-96365 (hydrochloride) - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	2.482 ml	12.41 ml	24.819 ml
5 mM	0.496 ml	2.482 ml	4.964 ml
10 mM	0.248 ml	1.241 ml	2.482 ml
5 mM	0.05 ml	0.248 ml	0.496 ml

Last Update：2024-01-02 23:10:35

SKF-96365 (hydrochloride) - Cell Experiment

To investigate whether SKF-96365 could protect PC12 cells from injury induced by MPP+ insult, cultured PC12 cells are pretreated with SKF-96365 in different concentrations (1 µM, 10 µM or 50 µM) 30 min before MPP+ addition. The cells viability is measured 24 h after MPP+ insult by using the cell proliferation reagent WST-1. (Only for Reference) Cell lines: PC12 cells

Last Update：2023-08-16 21:32:38

SKF-96365 (hydrochloride) - Reference Information

biological activity	SKF96365, originally considered to be a calcium channel blocker, is currently used as a TRPC channel blocker and is widely used in medical diagnosis.
target	TargetValue TRPC ()
Target	Value
in vitro study	SKF-96365 has anti-damage activity to MPP injury in PC12 cells, and can significantly inhibit apoptotic cell death after MPP is applied. SKF-96365 has no effect on the necrotic cell death induced by MPP. Because of its non-selective activity, SKF-96365 lease a variety of calcium channels: it not only inhibits high-voltage activated calcium channels, but also effectively inhibits low-voltage activated T-type calcium channels in HEK293 cells. The specific effect of SKF-96365 on intracellular calcium homeostasis is determined by cell type and experimental model.
In vivo research	In in vitro experiments, SKF-96365 treatment can inhibit calcium/calmodulin-dependent protein kinase II γ(CaMKII γ)/AKT signal cascade reaction.

Last Update：2024-04-10 22:29:15