Overview
Lyophilized Powder yes
Source Synthetic
MW: 356.3
Purity: >99% (HPLC)
Form Lyophilized powder.
Effective concentration 1-100 µM.
Structure
Chemical name (4R)-1,4-Dihydro-2,6-dimethyl-5-nitro-4-[2-trifluoromethyl)phenyl]-3-pyridinecarboxylic acid methyl ester.
Molecular formula C16H15 F3N2O4.
CAS No.: 98791-67-4
Activity (R)(+)-Bay K8644 is an L-type Ca2+-channel blocker1.
References-Activity
- Franckowiak, G. et al. (1985) Eur. J. Pharmacol. 114, 223.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
Storage of solutions Up to four weeks at 4°C or three months at -20°C.
Our bioassay
Alomone Labs (R)(+)-Bay K8644 inhibits L-type CaV channels heterologously expressed in Xenopus oocytes.A. Time course of CaV1.2 (co-expressed with α2δ1 and β1 auxiliary subunits) peak current amplitude, elicited by 100 ms voltage ramp from holding potential of -100 mV to +50 mV, delivered every 10 seconds. Application of 1, 10 and 100 µM (R)(+)-Bay K8644 (#B-352) inhibits the CaV1.2 current (indicated by the horizontal bar). B. Representative current traces before and during application of 1, 10 and 100 µM (R)(+)-Bay K8644 as indicated.
Scientific background
L-type Ca2+ channels possess binding sites for at least three distinct organic drug types: dihydropyridines (DHP), phenylalkylamines (PAA), and benzothiazepines (BTZ). These binding sites are known to reside in the α1 subunit of the channel.
(R)(+)-Bay K8644 is a DHP L-type Ca2+-channel blocker with negative inotropic and vasodilatatory effects in vivo. (R)(+)-Bay K8644 shows opposite effects to (S)(-)-Bay K8644. The action of the of (R)(+)-Bay K8644 was studied in rat tail artery and guinea pig ileal longitudinal smooth muscle using pharmacologic and radioligand binding assays. (R)(+)-Bay K8644 inhibited the responses to KCI-induced depolarization with IC50 values of 16.1-25.6 nM1.
Target L-type Ca2+ channels
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
Citations
