(±)-Bay K 8644 (Synonyms: SQ 28,873) |
| Katalog-Nr.GC15015 |
(±)-Bay K 8644 ((±)-(±)-Bay K 8644) ist ein Racemat, das aus zwei Isomeren (R)-(+)-Bay-K-8644 und (S)-(-)-Bay besteht -K-8644.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 71145-03-4
Sample solution is provided at 25 µL, 10mM.
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EC50: Acting as a L-type Ca2+ channel activator with EC50 of 17.3 nM .
The advent of calcium channel activators makes it possible to increase the amount of ACh released from the nerve terminals during their activation. Being applied as a Ca2+ channel activator, BAY K 8644 generally exhibits positive inotropic and vasoconstrictor effects on heart and smooth muscle. [1]
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]
Clinical trial: So far, no clinical trial has been conducted.
References:
[1]Greenberg DA, Cooper EC and Carpenter C. Calcium channel 'agonist' BAY K 8644 inhibits calcium antagonist binding to brain and PC12 cell membranes. Brain Res. 1987. 305: 3658.
[2]Doledal V and Tucek S. Failure of the calcium channel activator, Bay K 8644, to increase the release of acetylcholine from nerve terminals in brain and diaphragm. Br. J. Pharmac. 1987. 91: 475-9.
[3]Whittington MA, Butterworth AR, Dolin SJ, Patch TL and Little HJ. The effects of chronic treatment with the dihydropyridine, Bay K 8644, on hyperexcitability due to ethanol withdrawal, in vivo and in vitro. Br. J. Pharmacol. 1992. 105: 285-92.
[4] Ives N, King JW, Chernow B and Roth BL. BAY k 8644, a calcium channel agonist, reverses hypotension in endotoxin-shocked rats. Eur J Pharmacol. 1986. 130: 169-175.
| Cell experiment [1]: | |
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Cell lines |
Guinea Pig and Calf Myocardial Cells |
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Preparation method |
Soluble to 100 mM in ethanol. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
280 nM, 5 minutes |
|
Applications |
Bay k 8644 increased twitch tension in guinea pig atria without changing the time course of tension development. Bay k 8644 increased the action potential duration of calf ventricular muscle and Purkinje fibers. Bay k 8644 increased strontium currents and altered the time- and voltage-dependence of channel opening. |
| Animal experiment [2]: | |
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Animal models |
Male Sprague-Dawley rats |
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Dosage form |
Intraperitoneal administration, 0.5-4 mg/kg |
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Application |
Intraperitoneal administration of BAY K 8644 (0.5-4 mg/kg) induced an increase in blood pressure associated with bradycardia, increased tail-flick latency in response to radiant heat, decreased locomotion, induced muscle contraction, postural changes and also reduced reflex activity. BAY K 8644 (4 mg/kg, i.p.) significantly increased homovanillic acid and 3,4-dihydroxyphenylacetic acid concentrations in the cortex and striatum. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Thomas G, Chung M, Cohen C J. A dihydropyridine (Bay k 8644) that enhances calcium currents in guinea pig and calf myocardial cells. A new type of positive inotropic agent[J]. Circulation research, 1985, 56(1): 87-96. [2]. Bourson A, Moser P C, Gower A J, et al. Central and peripheral effects of the dihydropyridine calcium channel activator BAY K 8644 in the rat[J]. European journal of pharmacology, 1989, 160(3): 339-347. |
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| Cas No. | 71145-03-4 | SDF | |
| Überlieferungen | SQ 28,873 | ||
| Chemical Name | methyl 2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-3-carboxylate | ||
| Canonical SMILES | CC1=C(C(C(=C(N1)C)[N+](=O)[O-])C2=CC=CC=C2C(F)(F)F)C(=O)OC | ||
| Formula | C16H15F3N2O4 | M.Wt | 356.3 |
| Löslichkeit | 50mg/mL in DMSO, 50mg/mL in DMF, 50mg/mL in ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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