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| SKF 96365 HYDROCHLORIDE Basic information |
| Product Name: | SKF 96365 HYDROCHLORIDE | | Synonyms: | 1-[BETA-[3-(4-METHOXYPHENYL)PROPOXY]-4-METHOXYPHENETHYL]-1H-IMIDAZOLE HCL;1-(BETA-[3-(4-METHOXYPHENYL)PROPOXY]-4-METHOXYPHENETHYL)-1H-IMIDAZOLE HYDROCHLORIDE;1-[2-(4-METHOXYPHENYL)-2-[3-(4-METHOXYPHENYL)PROPOXY]ETHYL]-1H-IMIDAZOLE HYDROCHLORIDE;SK AND F 96365;SKF 96365;SKF 96365 HYDROCHLORIDE;SKF-96365, HCl;1-[β-(3-(4-methoxyphenyl)propoxy)-4-methoxyphenethyl]-1h-imidazole hydrochloride | | CAS: | 130495-35-1 | | MF: | C22H27ClN2O3 | | MW: | 402.91 | | EINECS: | | Product Categories: | Calcium channel;Signalling | | Mol File: | 130495-35-1.mol |
| SKF 96365 HYDROCHLORIDE Chemical Properties |
| Melting point | 119 °C | | RTECS | NI6823500 | | storage temp. | Inert atmosphere,Room Temperature | | solubility | H2O: >20 mg/mL | | form | solid | | color | white | | Water Solubility | Soluble to 100mM in water | | 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. | | CAS DataBase Reference | 130495-35-1(CAS DataBase Reference) |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36 | | WGK Germany | 3 |
| SKF 96365 HYDROCHLORIDE Usage And Synthesis |
| Description | SKF-96365 (130495-35-1) is an inhibitor of receptor-mediated calcium entry (RMCE) with IC50‘s of 8.5 μM for ADP stimulated platelets and 11.7 μM for thrombin stimulated platelets. Also inhibits Voltage-gated Ca2+ but not ATP-gated Ca2+ entry.1 It has also been shown to block transient receptor potential canonical type (TRPC) channels2, high-voltage-activated (HVA) L-type channels1, K channels3, sarcoplasmic reticulum Ca-ATPase4 and voltage-gated sodium channels5. SKF-96365 is a potent blocker of LVA T-type Ca channels, in particular Ca(V)3.1 (IC50 = 0.56 μM).6 | | Uses | SKF 96365 Hydrochloride is a novel inhibitor of receptor-mediated calcium entry. | | General Description | Inhibits receptor-mediated Ca2+ entry in stimulated platelets (IC50 = 8-12 μM in intact platelets), neutrophils, and endothelial cells (IC50 = 30 μM for human endothelial cells) at concentrations that do not affect internal Ca2+ release. Also inhibits voltage-gated Ca2+ entry in excitable cells. Inhibits the histamine-induced formation of nitric oxide in human endothelial cells. | | Biological Activity | Store-operated Ca 2+ entry (SOCE) inhibitor that inhibits STIM1. Also inhibits TRP channels, voltage-gated Ca 2+ channels and potassium channels. | | Biochem/physiol Actions | SKF-96365 with an alkylated imidazole ring is a selective inhibitor of receptor-mediated Ca2+?entry and voltage-gated Ca2+?entry . SKF-96365 mediated depolarization of smooth cardiac muscle membrane and had no impact on the acetylcholine (ACh)-induced depolarization. It is an inhibitor for SOCE (store-operated calcium entry). It also inhibits Homer1 protein expression. SKF-96365 elicits protective functionality in 1-methyl-4-phenylpyridinium(MPP) mediated cytotoxicity. | | References | 1) Merritt et al.,(1990) SKF96365, a novel inhibitor of receptor-mediated calcium entry; Biochem. J. 271 515
2) Kiselyov et al., (1998) Functional interaction between InsP3 receptors and store-operated Htrp3 channels; Nature, 396 478
3) Schwarz et al., (1994) Multiple effects of SKF96365 on ionic currents and intracellular calcium in human endothelial cells; Cell Calcium, 15 45
4) Mason et al., (1993) Inhibition of Ca2+ transport pathways in thymic lymphocytes by econazole, miconazole and SKF96365; Am. J. Physiol., 264 C654
5) Hong et al. (1994) Inhibition of the sodium channel by SKF96365, an inhibitor of the receptor-operated calcium channel, in mouse diaphragm; J. Biomed. Sci., 1 172
6) 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 |
| SKF 96365 HYDROCHLORIDE Preparation Products And Raw materials |
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