CAS NO: | 202821-81-6 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Cas No. | 202821-81-6 |
别名 | BMS-A |
化学名 | 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 |
分子式 | C16H10ClF3N2O3 |
分子量 | 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 |
储存条件 | Store at RT |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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: |