Overview
Lyophilized Powder yes
Source Synthetic
MW: 356.3
Purity: >99% (HPLC)
Effective concentration 1-5 μM.
Structure
Chemical name 1,4-Dihydro-2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl) phenyl]-3-pyridinecarboxylic acid, methyl ester.
Molecular formula C16H15F3N2O4.
CAS No.: 71145-03-4
Activity (±)-Bay K8644 is a dihydropyridine that acts as an L-type, voltage-gated Ca2+ channel agonist. The (-)-enantiomer has strong Ca2+ channel agonist properties, whereas the (+)-enantiomer has weak Ca2+ channel antagonist activity. The net activity of the racemic mix is L-type channel opening. In the presence of this agonist, channels tend to open for longer periods causing a large increase in the channel microscopic response1-4. (±)-Bay K8644 is also an inhibitor (by increasing the inactivation) of a Shaker KV channel5.
References-Activity
- Hess, P. et al. (1984) Nature 311, 538.
- Nowycky, M.C. et al. (1985) Proc. Natl. Acad. Sci. U.S.A. 82, 2178.
- Bechem, M. and Hoffmann, H. (1993) Pflugers Arch. 424, 343.
- Triggle, D.J. and Rampe, D. (1989) Trends Pharmacol. Sci. 10, 507.
- Avdonin, V. et al. (1997) J. Gen. Physiol. 109, 169.
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 Ethanol, methanol or DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to four weeks at 4°C or three months at -20°C.
Our bioassay
Alomone Labs (±)-Bay K8644 increases L-type Ca2+ currents expressed in Xenopus oocytes.Left: I-V relation before (squares) and during (circles) bath perfusion of 5 μM (±)-Bay K8644 (#B-350). Right: An example of current response to 200 ms depolarization to +20mV (from holding potential of -100 mV) before (black) and during (pink) perfusion of (±)-Bay K8644.
Alomone Labs (±)-Bay K8644 modulates the phosphorylation of ERK1/2 MAPK in Jurkat T cells.Cells were preincubated with or without EGTA or Nifedipine for 20 min then stimulated with (±)-Bay K8644 (#B-350) or with Ionomycin for 10 min. The cell proteins were blotted and probed with anti-phospho ERK1/2 (upper panel) or with anti-ERK1/2 (lower panel).
Scientific background
(±)-Bay K8644 is an opener of all L-type channels (CaV1 family). In the presence of this agonist, channels tend to open for longer periods causing a large increase in the channel macroscopic response.
The net activity of the racemic mix is that of the (-)-enantiomer agonistic activity.
(±)-Bay K8644 is a widely used L-type Ca2+ channel activator in various neuronal, muscle, endocrine, thyroid and other cell types.1-3
Target L-type Ca2+ channels
Lyophilized Powder
For research purposes only, not for human use
Last Update: 05/09/2024
Specifications
Citations
Citations
