BMS 191011 (Synonyms: BMS-A) |
| カタログ番号GC14239 |
BMS 191011 (BMS-A) は、強力な BKCa チャネル オープナー (大コンダクタンス Ca2+- 活性化カリウム チャネル) です。
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Cas No.: 202821-81-6
Sample solution is provided at 25 µL, 10mM.
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BMS 191011 is a maxi-K channel opener [1].
Maxi-K channels consist of a pore-forming α subunit and a regulatory β subunit. Maxi-K channels are of a high Ca2+ sensitivity [2].
Bath application of BMS-191011 at a concentration of 20 μM strongly reduced the calcium transients. This effect was associated with bursts of bAPs (100 Hz) recorded from Fmr1-/y dendrites without affecting those recorded from wild-type dendrites. This treatment decreased dendritic calcium transients of Fmr1-/y neurons to baseline levels of wild-type neurons [3]. In normoxia, BMS-191011 significantly induced cell death. This effect was indicted by the increases in propidium iodide (PI) uptake by 9.4 ± 2.4 and 16.8 ± 2.1% at 12 and 24 h treatments, respectively. At 12 h and then 24 h, the cellular [ATP] was decreased to 83.4 ± 3.1 and further to 72.3 ± 2.8%. During hypoxia, these effects were increased by ~2-fold in all time points and measurements. PI uptake was increased to 15.1 ± 1.8 at 12 h and then 40.7 ± 1.7% at 24 h. Cellular [ATP] was decreased to 77.8 ± 1.9 at 12 h and then to 43.3 ± 3.4% at 24 h [4].
In male Wistar rats of 8 to 10 weeks old, an i.v. administration with BMS-191011 at 10-100 µg/kg/min increased the retinal arteriol diameter, whereas it did not significantly affect mean arterial pressure and heart rate. Intravitreal injection of iberiotoxin at a dose of 20 pmol/eye significantly attenuated the vasodilator responses of retinal arterioles to BMS-191011 [5]. BMS-191011 demonstrated efficacy as an opener of the cloned large-conductance Ca2+-activated potassium (maxi-K) channel in in vivo stroke models [6].
References:
[1]. Hewawasam P, Ding M, Chen N, et al. Synthesis of water-soluble prodrugs of BMS-191011: a maxi-K channel opener targeted for post-stroke neuroprotection. Bioorganic & medicinal chemistry letters, 2003, 13(10): 1695-1698.
[2]. Valverde MA, Rojas P, Amigo J, et al. Acute activation of Maxi-K channels (hSlo) by estradiol binding to the β subunit. Science, 1999, 285(5435): 1929-1931.
[3]. Zhang Y, Bonnan A, Bony G, et al. Dendritic channelopathies contribute to neocortical and sensory hyperexcitability in Fmr1-/y mice. Nature neuroscience, 2014, 17(12): 1701-1709.
[4]. Gu XQ, Pamenter ME, Siemen D, et al. Mitochondrial but not plasmalemmal BK channels are hypoxia-sensitive in human glioma. Glia, 2014, 62(4): 504-513.
[5]. Mori A, Suzuki S, Sakamoto K, et al. BMS-191011, an opener of large-conductance Ca2+-activated potassium channels, dilates rat retinal arterioles in vivo. Biological and Pharmaceutical Bulletin, 2011, 34(1): 150-152.
[6]. Romine JL, Martin SW, Meanwell NA, et al. 3-[(5-Chloro-2-hydroxyphenyl) methyl]-5-[4-(trifluoromethyl) phenyl]-1, 3, 4-oxadiazol-2 (3 H)-one, BMS-191011: Opener of Large-Conductance Ca2+-Activated Potassium (Maxi-K) Channels, Identification, Solubility, and SAR. Journal of medicinal chemistry, 2007, 50(3): 528-542.
| Cas No. | 202821-81-6 | SDF | |
| 同義語 | BMS-A | ||
| Chemical Name | 3-(5-chloro-2-hydroxybenzyl)-5-(4-(trifluoromethyl)phenyl)-1,3,4-oxadiazol-2(3H)-one | ||
| Canonical SMILES | ClC1=CC=C(C(CN2N=C(C3=CC=C(C(F)(F)F)C=C3)OC2=O)=C1)O | ||
| Formula | C16H10ClF3N2O3 | M.Wt | 370.71 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.3 mg/ml,Ethanol: 3 mg/ml | Storage | Store at RT |
| 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6975 mL | 13.4876 mL | 26.9753 mL |
| 5 mM | 0.5395 mL | 2.6975 mL | 5.3951 mL |
| 10 mM | 0.2698 mL | 1.3488 mL | 2.6975 mL |
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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.
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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