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Submit ReviewSKF 96365 hydrochloride
Description: TRPC channel inhibitor; also inhibits store-operated Ca2+ entry
Chemical Name: 1-[2-(4-Methoxyphenyl)-2-[3-(4-methoxyphenyl)propoxy]ethyl-1H-imidazole hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for SKF 96365 hydrochloride
SKF 96365 hydrochloride is a store-operated Ca2+ entry (SOCE) inhibitor that inhibits STIM1. Also blocks TRPC channels, voltage-gated Ca2+ channels and potassium channels.
Technical Data for SKF 96365 hydrochloride
| M. Wt | 402.92 |
| Formula | C22H26N2O3.HCl |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 130495-35-1 |
| PubChem ID | 104955 |
| InChI Key | FWLPKVQUECFKSW-UHFFFAOYSA-N |
| Smiles | Cl.COC1=CC=C(CCCOC(CN2C=CN=C2)C2=CC=C(OC)C=C2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SKF 96365 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 8.06 | 20 with gentle warming |
Preparing Stock Solutions for SKF 96365 hydrochloride
The following data is based on the product molecular weight 402.92. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 12.41 mL | 62.05 mL | 124.09 mL |
| 1 mM | 2.48 mL | 12.41 mL | 24.82 mL |
| 2 mM | 1.24 mL | 6.2 mL | 12.41 mL |
| 10 mM | 0.25 mL | 1.24 mL | 2.48 mL |
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Product Datasheets for SKF 96365 hydrochloride
References for SKF 96365 hydrochloride
References are publications that support the biological activity of the product.
Merritt et al (1990) SK&F96365, a novel inhibitor of receptor-mediated calcium entry. Biochem.J. 271 515 PMID: 2173565
Varnai et al (2009) STIM and Orai: the long-awaited constituents of store-operated calcium entry. TiPS 30 118 PMID: 19187978
Singh et al (2010) The transient receptor potential channel antagonist SKF96365 is a potent blocker of low-voltage-activated T-type calcium channels. Br.J.Pharmacol. 160 1464 PMID: 20590636
If you know of a relevant reference for SKF 96365 hydrochloride, please let us know.
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Keywords: SKF 96365 hydrochloride, SKF 96365 hydrochloride supplier, STIM1-mediated, Ca2+, influx, inhibitos, receptor-mediated, entry, Store, Operated, Calcium, Channels, STIM-Orai, Signaling, Signalling, Agents, General, SKF96365, hydrochloride, TRPC, 1147, Tocris Bioscience
14 Citations for SKF 96365 hydrochloride
Citations are publications that use Tocris products. Selected citations for SKF 96365 hydrochloride include:
Shin et al (2008) Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells. J Neuroinflammation 105 746 PMID: 18174329
Alkhani et al (2014) Contribution of TRPC3 to store-operated calcium entry and inflammatory transductions in primary nociceptors. Proc Natl Acad Sci U S A 10 43 PMID: 24965271
Soltoff and Lannon (2013) Activation of ERK1/2 by store-operated calcium entry in rat parotid acinar cells. PLoS One 8 e72881 PMID: 24009711
Szikra et al (2009) Calcium homeostasis and cone signaling are regulated by interactions between calcium stores and plasma membrane ion channels. PLoS One 4 e6723 PMID: 19696927
Hildebrand et al (2009) Functional coupling between mGluR1 and Cav3.1 T-type calcium channels contributes to parallel fiber-induced fast calcium signaling within Purkinje cell dendritic spines. J Neurosci 29 9668 PMID: 19657020
Sahu et al (2019) Peptide/Receptor Co-evolution Explains the Lipolytic Function of the Neuropeptide TLQP-21. Cell Rep 28 2567 PMID: 31484069
Ben-Mabrouk and Tryba (2010) Substance P modulation of TRPC3/7 channels improves respiratory rhythm regularity and ICAN-dependent pacemaker activity. Mol Pain 31 1219 PMID: 20345918
Kyriazis et al (2010) Stress-induced switch in Numb isoforms enhances Notch-dependent expression of subtype-specific transient receptor potential channel. J Biol Chem 285 6811 PMID: 20038578
Fu and Pol (2010) Kisspeptin directly excites anorexigenic proopiomelanocortin neurons but inhibits orexigenic neuropeptide Y cells by an indirect synaptic mechanism. J Neurosci 30 10205 PMID: 20668204
Kubota et al (2014) mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways. PLoS One 9 e106316 PMID: 25181481
Hutchins et al (2013) Calcium release-dependent actin flow in the leading process mediates axophilic migration. Biochem J 33 11361 PMID: 23843509
Huang et al (2004) Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons. J Neurosci 24 4551 PMID: 15140926
Lim et al (2001) NAADP+ initiates the Ca2+ response during fertilization of starfish oocytes. FASEB J 15 2257 PMID: 11641253
Moneer et al (2003) Nitric oxide co-ordinates the activities of the capacitative and non-capacitative Ca2+-entry pathways regulated by vasopressin. Eur J Neurosci 370 439 PMID: 12459038
Do you know of a great paper that uses SKF 96365 hydrochloride from Tocris? Please let us know.
Reviews for SKF 96365 hydrochloride
Average Rating: 4.7 (Based on 3 Reviews.)
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It can inhibit TRPC1 channel.
By
Yuyang Sun on 05/30/2022
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HSG
Used SKF to test TRPC1 channel; it can inhibit the Tg induced SOCE entry.
Tested for store operated calcium entry inhibiting activity.
By
ANANTH KUMAR KAMMALA on 01/30/2021
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Mast cells LAD2
SKF96365 HCL was used to study the Invitro Calcium mobilization assay, cytokine assay in human mast cells (LAD2), and Invivo mast cell-dependent inflammation studies. SKF96365 at a concentration of 30,50 and 100uM has inhibited the calcium mobilization via the MRGPRX2 pathway and reduced the inflammation in mast cell dependent invivo paw edema and rosacea experiments. SKF965365 HCL is the best compound to study the store-operated calcium entry assays.
a Store-operated channel blocker.
By
Anonymous on 05/02/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: microglia
SKF96365 at 20 microM blocks intracellular calcium influx through a store-operated channel in microglia culture.