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Purity: ≥98%
BAYK 8644 [(+/-)-Bay K-8644] is a novel and potent L-type Ca2+ channel activator with an EC50 of 17.3 nM. (+/-)-Bay K 8644, a conventional racemic mixture of Bay K 8644, is widely used as an L-type Ca(2+) channel agonist.
| Targets |
When Bay K 8644 (1 μM) was applied to 2-day-old newborn rat ventricular cardiomyocytes, the cells' L-type calcium current density increased. A greater rise in the L-type calcium current density of Bay K 8644 in 2-day-cultured cells compared to 7-day-cultured cells can be attributed to variations in the phosphorylation levels of calcium channels at each developmental stage [4].
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| ln Vitro |
When Bay K 8644 (1 μM) was applied to 2-day-old newborn rat ventricular cardiomyocytes, the cells' L-type calcium current density increased. A greater rise in the L-type calcium current density of Bay K 8644 in 2-day-cultured cells compared to 7-day-cultured cells can be attributed to variations in the phosphorylation levels of calcium channels at each developmental stage [4].
BAY K 8644 (1 μM) alone increased the peak L-type calcium channel current (\(I_{Ca(peak)}\)) to 293.0 ± 107.9% of control in guinea-pig ventricular myocytes. [1] In the presence of 30 μM fendiline, 1 μM BAY K 8644 further reduced \(I_{Ca(peak)}\) to 1.0 ± 1.6% of control, instead of stimulating it, indicating a paradoxical inhibitory effect. [1] The pure agonist enantiomer (4S)-BAY K 8644 (1 μM) also caused further inhibition of \(I_{Ca(peak)}\) to 4.7 ± 1.1% of control in the presence of fendiline. [1] In contrast, in the presence of other calcium channel blockers (nifedipine, verapamil, diltiazem), 1 μM BAY K 8644 produced the expected agonist effect and increased \(I_{Ca(peak)}\). [1] |
| ln Vivo |
In endotoxin-treated hypotensive rats, a single dose of Bay K 8644 as little as 10 μg/kg dramatically raised mean arterial pressure (MAP), but had no impact on normal rats. Additionally, endotoxin-treated rats' heart rates decreased by 37% and control rats' heart rates decreased by 39% in response to Bay K 8644 [5].
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| Cell Assay |
The whole-cell patch-clamp technique was used to record L-type calcium channel currents (\(I_{Ca}\)) from isolated guinea-pig ventricular myocytes. Cells were superfused with choline-based physiological salt solution and intracellular pipette solution containing CsCl, EGTA, MgCl₂, CaCl₂, HEPES, and K-ATP. Voltage pulses were applied from a holding potential of -90 mV, with a prepulse to -40 mV for 100 ms, followed by a test pulse to +10 mV for 250 ms at 5 s intervals. Currents were low-pass filtered and digitized for analysis. [1]
Steady-state inactivation (\(f_{\infty}\)) was determined using a double-pulse protocol: conditioning prepulses from -80 mV to +10 mV (20 s) followed by a test pulse to +10 mV. \(I_{Ca(peak)}\) values were plotted against prepulse potential and fitted to a Boltzmann equation to calculate \(f_{\infty}\). [1] Time constants of activation and inactivation were obtained by fitting single exponential functions to the rising and decaying phases of \(I_{Ca}\) traces elicited by step depolarizations from -10 to +30 mV. [1] |
| References |
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| Additional Infomation |
2,6-Dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-3-carboxylic acid methyl ester is a pentasubstituted dihydropyridine with methoxycarbonyl, 2-(trifluoromethyl)phenyl, and nitro substituents at positions 3, 4, and 5, respectively, and two methyl substituents at positions 2 and 6. It is a dihydropyridine, methyl ester, C-nitro compound belonging to the (trifluoromethyl)benzene class of compounds. Unlike nifedipine, this dihydropyridine derivative is a calcium channel agonist. This compound promotes Ca2+ influx through partially activated voltage-dependent calcium channels, thereby producing vasoconstriction and positive inotropic effects. It is primarily used as a research tool. BAY K 8644 is a racemic mixture of (4S)-Bay K 8644 (agonist) and (4R)-Bay K 8644 (antagonist). [1]
In the presence of fendiline, the paradoxical inhibition of (ICa) by BAY K 8644 is thought to be caused by an allosteric interaction between fendiline and the dihydropyridine agonist site on the L-type calcium channel. [1] This study suggests that diphenylalkylamines like fendiline may act at different sites than classical calcium channel blockers. [1] |
| Molecular Formula |
C16H15N2O4F3
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|---|---|
| Molecular Weight |
356.2965
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| Exact Mass |
356.098
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| CAS # |
71145-03-4
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| Related CAS # |
(S)-(-)-Bay-K-8644;98625-26-4;(R)-(+)-Bay-K-8644;98791-67-4
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| PubChem CID |
2303
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.37g/cm3
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| Boiling Point |
404.3ºC at 760 mmHg
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| Flash Point |
198.3ºC
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| Index of Refraction |
1.545
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| LogP |
4.199
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
634
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZFLWDHHVRRZMEI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H15F3N2O4/c1-8-12(15(22)25-3)13(14(21(23)24)9(2)20-8)10-6-4-5-7-11(10)16(17,18)19/h4-7,13,20H,1-3H3
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| Chemical Name |
methyl 2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-3-carboxylate
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| Synonyms |
(+/-)-Bay K-8644; BAYK 8644; (+/-)-Bay-K-8644; BAYK8644; (+/-)-Bay K 8644; BAYK-8644.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~233.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.84 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (4.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8066 mL | 14.0331 mL | 28.0662 mL | |
| 5 mM | 0.5613 mL | 2.8066 mL | 5.6132 mL | |
| 10 mM | 0.2807 mL | 1.4033 mL | 2.8066 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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