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Purity: ≥98%
(R)-(+)-Bay-K-8644, the R-isomer of Bay-K-8644, is a novel and potent a calcium channel inhibitor/blocker that inhibits Ba2+ currents (IBa) (IC50=975 nM). (+/-)-Bay K 8644, a conventional racemic mixture of Bay K 8644, is widely used as an L-type Ca(2+) channel agonist.
| Targets |
(R)-(+)-Bay-K-8644 is a conventional racemic combination that is frequently employed as an L-type Ca2+ channel agonist (Bay K 8644). With (R)-(+)-Bay-K-8644 functioning as an antagonist and S(-)-Bay K 8644 working as an agonist, each optical isomer has opposing effects on IBa. Ba2+ current (IBa) is inhibited by (R)-(+)-Bay-K-8644 (IC50=975 nM). Applying (R)-(+)-Bay-K-8644 (0.5 μM) suppressed IBa to 71±10% of control. when (R)-(+)-Bay-K-8644IBa is present[1]. An inhibitor of calcium channels is (R)-(+)-Bay-K-8644 [2].
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| ln Vitro |
(R)-(+)-Bay-K-8644 is a conventional racemic combination that is frequently employed as an L-type Ca2+ channel agonist (Bay K 8644). With (R)-(+)-Bay-K-8644 functioning as an antagonist and S(-)-Bay K 8644 working as an agonist, each optical isomer has opposing effects on IBa. Ba2+ current (IBa) is inhibited by (R)-(+)-Bay-K-8644 (IC50=975 nM). Applying (R)-(+)-Bay-K-8644 (0.5 μM) suppressed IBa to 71±10% of control. when (R)-(+)-Bay-K-8644IBa is present[1]. An inhibitor of calcium channels is (R)-(+)-Bay-K-8644 [2].
In intact mouse urinary bladder smooth muscle (UBSM) strips, application of (R)-(+)-Bay-K-8644 (1 µM) significantly reduced the frequency of Ca²⁺ sparklets (small, discrete membrane-localized Ca²⁺ elevations) from 0.20 ± 0.08 Hz/mm² to 0.034 ± 0.021 Hz/mm². [1] The amplitude of the remaining Ca²⁺ sparklets in the presence of (R)-(+)-Bay-K-8644 (1 µM) was not significantly different from control (0.08 ± 0.004 F/F₀ vs. control 0.08 ± 0.002 F/F₀). [1] When UBSM strips were exposed to both the sarcoplasmic reticulum Ca²⁺-ATPase inhibitor cyclopiazonic acid (CPA, 10 µM) and (R)-(+)-Bay-K-8644 (1 µM), a significant decrease in Ca²⁺ sparklet frequency was also observed (0.15 ± 0.03 Hz/mm² vs. control 0.34 ± 0.08 Hz/mm²), and the sparklet amplitude remained unaffected. This indicates that CPA-induced sparklet activity is also dependent on VGCCs. [1] |
| Cell Assay |
The study utilized intact smooth muscle strips from the urinary bladder of male C57BL/6 mice (6-10 weeks old). Strips were loaded with the fluorescent Ca²⁺ indicator Oregon Green BAPTA-1 AM (10 µM) for 70 minutes at 35°C. [1]
Ca²⁺ sparklets were imaged using Total Internal Reflection Fluorescence (TIRF) microscopy. The strip was placed serosal side down on a coverslip, perfused with oxygenated Krebs solution at 25°C, and gently weighted to position cells within the evanescent field. Images were captured at 150 Hz. [1] For drug application, (R)-(+)-Bay-K-8644 (1 µM) was dissolved in DMSO as a stock solution and diluted in Krebs solution on the day of use. A minimum exposure period of 15 minutes was allowed before imaging. Ca²⁺ sparklets were detected and analyzed using automated (LC Pro plugin for ImageJ) and manual methods, with criteria including a minimum duration of 3 frames, a signal 2.5 standard deviations above baseline, and a peak amplitude of at least 0.05 F/F₀. Frequency was normalized to cell membrane area within the TIRF zone. [1] |
| References |
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| Additional Infomation |
(R)-Bay-K-8644 is a methyl 2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-3-carboxylic acid ester with an (R) configuration at position 4. It is the enantiomer of (S)-Bay-K-8644. It is a dihydropyridine derivative and, unlike nifedipine, is a calcium channel agonist. This compound promotes the influx of Ca2+ through partially activated voltage-dependent Ca2+ channels, resulting in vasoconstriction and positive inotropic effects. It is primarily used as a research tool. (R)-(+)-Bay-K-8644 has been used as a pharmacological tool to inhibit L-type voltage-gated calcium channels (VGCCs) and to investigate its role in the generation of Ca2+ sparks in bladder smooth muscle. [1]
This study indicates that Ca²⁺ spark (which can be inhibited by (R)-(+)-Bay-K-8644) represents a form of storage-operated calcium influx (SOCE) that can occur via voltage-gated calcium channel (VGCC) complexes in excitable cells, especially after pharmacological depletion of the reservoir using CPA. [1] Here, the enantiomer (R)-(+)-Bay-K-8644 is described as an inhibitor, while its enantiomer (S)-(-)-Bay-K-8644 is generally considered an L-type channel agonist. [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 # |
98791-67-4
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| Related CAS # |
Bay K 8644;71145-03-4;(S)-(-)-Bay-K-8644;98625-26-4
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| PubChem CID |
6604881
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
429.2±45.0 °C at 760 mmHg
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| Flash Point |
213.4±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.543
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| LogP |
2.39
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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 |
1
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| SMILES |
CC1=C([C@H](C(=C(N1)C)[N+](=O)[O-])C2=CC=CC=C2C(F)(F)F)C(=O)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; Bay-K 8644 (R)-(-)-; (R)-(-)-Bay-K-8644; Bay-K-8644 (S)-(-)-; (R)-(-)-Bay K-8644; (-)-BAY-R-5417; (-)-BAY-K-8644; (-)-BAY R-5417; BAYK 8644; BAYK8644; 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 : ≥ 300 mg/mL (~841.99 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.02 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 25.0 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. Solubility in Formulation 2: 2.5 mg/mL (7.02 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 ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. (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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