130495-35-1 Usage
Uses
Used in Pharmaceutical Research:
SKF 96365 HYDROCHLORIDE is used as a research tool for studying the role of calcium signaling in various cellular processes. Its ability to inhibit receptor-mediated calcium entry and voltage-gated calcium channels makes it a valuable compound for investigating the mechanisms underlying calcium-dependent cellular functions.
Used in Platelet Aggregation Studies:
SKF 96365 HYDROCHLORIDE is used as an inhibitor of platelet aggregation, particularly in the context of ADP and thrombin-stimulated platelets. Its IC50 values of 8.5 μM for ADP-stimulated platelets and 11.7 μM for thrombin-stimulated platelets make it a useful compound for studying platelet activation and aggregation mechanisms.
Used in Endothelial Cell Research:
SKF 96365 HYDROCHLORIDE is used as an inhibitor of histamine-induced nitric oxide formation in human endothelial cells. This application aids in understanding the role of calcium signaling in endothelial cell function and the regulation of vascular tone.
Used in Ion Channel Research:
SKF 96365 HYDROCHLORIDE is used as a potent blocker of low-voltage-activated (LVA) T-type Ca channels, specifically Ca(V)3.1, with an IC50 of 0.56 μM. This application is valuable for studying the function and regulation of T-type calcium channels in various cell types.
Used in Drug Development:
SKF 96365 HYDROCHLORIDE is used as a starting point for the development of new drugs targeting calcium channels and related pathways. Its diverse inhibitory effects on various calcium channels and other ion channels make it a promising candidate for the development of therapeutic agents for conditions involving dysregulated calcium signaling.
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
Check Digit Verification of cas no
The CAS Registry Mumber 130495-35-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,0,4,9 and 5 respectively; the second part has 2 digits, 3 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 130495-35:
(8*1)+(7*3)+(6*0)+(5*4)+(4*9)+(3*5)+(2*3)+(1*5)=111
111 % 10 = 1
So 130495-35-1 is a valid CAS Registry Number.
InChI:InChI=1/C22H26N2O3.ClH/c1-25-20-9-5-18(6-10-20)4-3-15-27-22(16-24-14-13-23-17-24)19-7-11-21(26-2)12-8-19;/h5-14,17,22H,3-4,15-16H2,1-2H3;1H
