SKF 96365 HYDROCHLORIDE
Synonym(s):1-[β-(3-(4-Methoxyphenyl)propoxy)-4-methoxyphenethyl]-1H-imidazole hydrochloride;1-[β-[3-(4-Methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole, HCl;1-[2-(4-Methoxyphenyl)-2-[3-(4-methoxyphenyl)propoxy]ethyl]imidazole;SKF-96365, Hydrochloride - CAS 130495-35-1 - Calbiochem
- CAS NO.:130495-35-1
- Empirical Formula: C22H27ClN2O3
- Molecular Weight: 402.91
- MDL number: MFCD00236407
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 15:53:33
What is SKF 96365 HYDROCHLORIDE?
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
The Uses of SKF 96365 HYDROCHLORIDE
SKF 96365 Hydrochloride is a novel inhibitor of receptor-mediated calcium entry.
What are the applications of Application
SK&F 96365 is a calcium channel protein and Stim 1 inhibitor
Definition
ChEBI: SKF-96365 hydrochloride is the hydrochloride salt of SKF-96365. It is a TRP channel blocker. It has a role as a TRP channel blocker, an apoptosis inducer, an autophagy inducer, a GABA antagonist, an antineoplastic agent, a calcium channel blocker and a platelet aggregation inhibitor. It contains a SKF-96365 free base(1+).
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.
storage
Store at RT
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
Properties of SKF 96365 HYDROCHLORIDE
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) |
Safety information for SKF 96365 HYDROCHLORIDE
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P304+P340:IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P405:Store locked up. |
Computed Descriptors for SKF 96365 HYDROCHLORIDE
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