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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.
| 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].
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| 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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| References |
[1]. W Schreibmayer, et al. Kinetic modulation of guinea-pig cardiac L-type calcium channels by fendiline and reversal of the effects of Bay K 8644. Br J Pharmacol. 1992 May;106(1):151-6.
[2]. G A Rae, et al. Interactions of calcium antagonists and the calcium channel agonist Bay K 8644 on neurotransmission of the mouse isolated vas deferens. Br J Pharmacol. 1989 Feb;96(2):333-40. [3]. H Satoh, et al. Bay K 8644 increases resting Ca2+ spark frequency in ferret ventricular myocytes independent of Ca influx: contrast with caffeine and ryanodine effects. Circ Res. 1998 Dec 14-28;83(12):1192-204. [4]. J P Gomez, et al. Effects of Bay K 8644 on L-type calcium current from newborn rat cardiomyocytes in primary culture. J Mol Cell Cardiol. 1996 Oct;28(10):2217-29. [5]. N Ives,et al. BAY k 8644, a calcium channel agonist, reverses hypotension in endotoxin-shocked rats. Eur J Pharmacol. 1986 Nov 4;130(3):169-75. |
| Molecular Formula |
C16H15N2O4F3
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|---|---|
| Molecular Weight |
356.2965
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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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| SMILES |
O=C(C1=C(C)NC(C)=C([N+]([O-])=O)C1C2=CC=CC=C2C(F)(F)F)OC
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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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| 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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