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| (+/-)-BAY K 8644 Basic information |
| Product Name: | (+/-)-BAY K 8644 | | Synonyms: | 1,4-DIHYDRO-2,6-DIMETHYL-5-NITRO-4-[2'-(TRIFLUOROMETHYL)PHENYL]-3-PYRIDINECARBOXYLIC ACID METHYL ESTER;1,4-DIHYDRO-2,6-DIMETHYL-5-NITRO-4-[2-(TRIFLUOROMETHYL)PHENYL]-3-PYRIDINECARBOXYLIC ACID, METHYL ESTER;1,4-DIHYDRO-2,6-DIMETHYL-5-NITRO-4-(2-[TRIFLUOROMETHYL]PHENYL)PYRIDINE-3-CARBOXYLIC ACID METHYL ESTER;(+/-)-BAY K 8644;BAY K-8644 (+/-);3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-diMethyl-5-nitro-4-[2-(trifluoroMethyl)phenyl]-, Methyl ester;methyl 2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-3-carboxylate;(+/-)-BAY K8644 CALCIUM SLOW CHANNEL | | CAS: | 71145-03-4 | | MF: | C16H15F3N2O4 | | MW: | 356.3 | | EINECS: | | Product Categories: | Calcium channel | | Mol File: | 71145-03-4.mol |
| (+/-)-BAY K 8644 Chemical Properties |
| Melting point | 166 °C | | Boiling point | 429.2±45.0 °C(Predicted) | | density | 1.3548 (estimate) | | RTECS | US5655000 | | storage temp. | 2-8°C | | solubility | DMSO: 184 mg/mL | | form | Yellow solid. | | pka | -3.43±0.70(Predicted) | | color | Yellow | | Water Solubility | Soluble in DMSO at 20mg/ml. Also soluble in methanol or ethanol at 60mg/ml. Insoluble in water | | Stability: | Stable. Incompatible with strong oxidizing agents. |
| Hazard Codes | Xi | | Risk Statements | 36/38 | | Safety Statements | 26-36 | | WGK Germany | 3 |
| (+/-)-BAY K 8644 Usage And Synthesis |
| Description | BAY K8644 (71145-03-4) is an L-type Ca2+-channel activator with positive inotropic and vasoconstrictive effects. | | Chemical Properties | yellow powder | | Uses | An active L-type, voltage-gated calcium channel agonist | | Biological Activity | L-type Ca 2+ -channel activator (EC 50 = 17.3 nM). Has positive inotropic, vasoconstrictive and behavioral effects in vivo . Separate enantiomers also available ((4R)-1,4-Dihydro-2,6-dimethyl-5-nitro-4-[2-trifluoromet hyl)phenyl]-3-pyridinecarboxylic acid methyl ester and (4S)-1,4-Dihydro-2,6-dimethyl-5-nitro-4-[2-trifluoromet hyl)phenyl]-3-pyridinecarboxylic acid methyl ester). | | Biochem/physiol Actions | (±)-Bay K8644 is a 1,4-dihydropyridine (DHP) derivative and an agonist for L-type Ca2+ channels. However, it′s enantiomers (-)-BAY k8644 and (+)-BAY k8644 have opposing functionality with respect to Ca2+ channels as high-potency agonist and low-potency antagonist, respectively. (±)-Bay K8644 increases influx of Ca2+ specifically at voltage-gated calcium channels. It constricts blood vessels and heart contraction. | | in vitro | it was demonstrated that bay k 8644 prolonged the mean ca2+ channel opening time in heart myocytes and neurones of spinal ganglia. an experiment using rat heart ventricles demonstrated that bay k 8644, at the final concentration of approximately 1 pm, had strong positive inotropic effect when added to the perfusion fluid. moreover, the addition of bay k 8644 to the chronic ethanol treatment significantly reduced the electrophysiological signs of withdrawal in the isolated hippocampal slices. [2, 3] | | in vivo | study in mice demonstrated that bay k 8644 significantly ameliorated the ethanol withdrawal syndrome. when experimental animals were administered with an acute injection of bay k 8644, the convulsive behavior of mice could be monitored to increase for 2 hours. in addition, bay k 8644 was also reported to ameliorate hypotension in endotoxin-shocked rats. it could lead to a 37% decrease in heart rate of endotoxin-treated rats and 39% decrease in control rats in a dose-dependent manner. [3,4] | | References | 1) Schramm?et al. (1983)?Novel Dihydropyridines with positive inotropic action through activation of Ca2+ channels; Nature,?303?535
2) Yamamoto?et al. (1984)?Bay K8644 Differentiates between potential and receptor operated Ca2+ channels; Eur. J. Pharmacol.?102?555
3) Thomas?et al. (1985)?A dihydropyridine (Bay K 8644) that enhances calcium currents in guinea pig and calf myocardial cells. A new type of positive inotropic agent; Circ. Res.,?56?87
4) Shi?et al. (2009)?Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small molecule compounds; Cell Stem Cell,?3?568 |
| (+/-)-BAY K 8644 Preparation Products And Raw materials |
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