Flunarizine dot 2HClA calcium channel protein inhibitor

Flunarizine • 2HCl (CAS 30484-77-6)

Flunarizine andbull 2HCl | CAS 30484-77-6 is rated 5.0 out of 5 by 1.
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Application: A calcium channel protein inhibitor
CAS Number: 30484-77-6
Purity: ≥99%
Molecular Weight: 477.4
Molecular Formula: C26H26F2N2·2HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Flunarizine • 2HCl, a calcium channel protein inhibitor and antagonist, has been shown to inhibit contraction of isolated murine caudal artery preparations. Mechanistic studies suggest that this compound inhibits prostaglandin-induced and Serotonin • HCl (sc-201146) induced components of the contraction via reduction in the amounts of TXB2 (Thromboxane B2) (sc-201452) and ALK-1, and an increase in production of HETE. Experiments on rabbit sino-atrial nodes and isolated guinea-pig papillary muscles have reported that Flunarizine • 2HCl depressed the slow action potentials of K+-depolarized papillary muscle. Additionally, studies indicate that Flunarizine • 2HCl selectively suppresses Ca2+ influx through the cell membrane of sino-atrial nodes.


References

1. De Clerck, F., et al. 1983. Biochem. Pharmacol. 32: 765-771. PMID: 6404280
2. Kotake, H., et al. 1988. Res. Commun. Chem. Pathol. Pharmacol. 62: 147-160. PMID: 3251331
3. Takahashi, K., et al. 1991. J. Pharmacol. Exp. Ther. 256: 169-175. PMID: 1846413

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/mL), ethanol (5 mg/mL warm), methanol, 0.1N HCI, and chloroform/methanol (9:1) (50 mg/mL). Insoluble in water, and dilute aqueous base..
Storage :
Store at -20° C
Melting Point :
251-255° C
IC50 :
Sodium channel protein type III alpha subunit: IC50 = 290 nM (rat); Sodium channel protein type V alpha subunit: IC50 = 350 nM (rat); Voltage-gated T-type calcium channel alpha-1H subunit: IC50 = 2200 nM (rat); Sodium channel protein type VIII alpha subunit : IC50 = 290 nM (rat); Voltage-gated T-type calcium channel alpha-1G subunit: IC50 = 2200 nM (rat)
Ki Data :
Sodium channel protein type II alpha subunit: Ki= 53 nM (rat); Sodium channel protein type VIII alpha subunit: Ki= 53 nM (rat); Sodium channel protein type III alpha subunit: Ki= 53 nM (rat); Sodium channel protein type I alpha subunit: Ki= 53 nM (rat)
pK Values :
pKb: 6.99
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
TK9187000
PubChem CID :
5282407
Merck Index :
14: 4144
MDL Number :
MFCD00058198
EC Number :
250-216-6
Beilstein Registry :
4284243
SMILES :
C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F.Cl.Cl

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Takahashi et al Takahashi et al. (PubMed ID 1846413) showed that Flunarizine 2HCl blocked T-type Ca++ channel in rat isolated hippocampal CA1 pyramidal neurons. -SCBT Publication Review
Date published: 2015-06-26
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