XE-991 dihydrochloride，KCNQ channel blocker; blocks M current (ab120089)
Key features and details
- Potent, selective KCNQ channel blocker; blocks M current
- CAS Number: 122955-13-9
Soluble in water to 100 mM
- Form / State: Solid
- Source: Synthetic
概述
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产品名称
XE-991 dihydrochloride，KCNQ channel blocker; blocks M current -
描述
Potent，selective KCNQ channel blocker; blocks M current -
生物学描述
Potent and selective blocker of KCNQ voltage-gated potassium channels. Blocks M current. (IC50 values are 0.98 μM (M-current), 0.71 μM (KCNQ 2), 0.75 μM (KCNQX 1), >100 μM (Kv1.2) and >43 μM (Kv4.3). Potent pulmonary vasoconstrictor. Cognitive enhancer following oral administration in vivo.
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CAS编号
122955-13-9 -
化学结构
性能
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化学名称
10,10-Bis(4-pyridinylmethyl)-9(10H)-anthracenone dihydrochloride
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分子量
449.40 -
分子式
C26H20N2O.2HCl -
PubChem识别号
45073462 -
存放说明
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
溶解度概述
Soluble in water to 100 mM
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处理
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Refer to SDS for further information.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
C1=CC=C2C(=C1)C(=O)C3=CC=CC=C3C2(CC4=CC=NC=C4)CC5=CC=NC=C5.Cl.Cl -
来源
Synthetic
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研究领域
图片
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Chemical Structure - XE-991 dihydrochloride, KCNQ channel blocker; blocks M current (ab120089)2D chemical structure image of ab120089, XE-991 dihydrochloride, KCNQ channel blocker; blocks M current
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Functional Studies - XE-991 dihydrochloride, KCNQ channel blocker; blocks M current (ab120089)Image from Glasgow SD et al., PLoS One. 2013;8(3):e58901. Fig 7(A).; doi: 10.1371/journal.pone.0058901. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/To assess the effects of blockade of muscarine-dependent K+ current, IM, under voltage clamp conditions, and to determine if carbachol, CCh, acts through the blockade of an additional conductance other than IM, voltage ramps were performed in ACSF containing TTX (0.5 µM), ZD7288 (50 µM), prior to and during sequential addition of XE-991 (10 µM) and CCh (50 µM) (n=9). Application of XE-991 in the presence of TTX and ZD7288 resulted in a significant increase in current required to hold neurons at −60 mV (−18.1±6.6 pA; N–K: p<0.05).
Bath application of XE-991 (10 µM; white bar) resulted in an inward current in cells held at −60 mV indicating that the cells express IM, and the subsequent perfusion with CCh (50 µM) resulted in an additional inward current, suggesting that CCh blocks a second K+ conductance (*: p<0.05).
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Functional Studies - XE-991 dihydrochloride, KCNQ channel blocker; blocks M current (ab120089)Image from Petrovic MM et al., PLoS One. 2012;7(2):e30402. Fig 1(B,C).; doi: 10.1371/journal.pone.0030402. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/Left - Theta burst stimulation (TBP) does not induce long-term potentiation (LTP) under control conditions. Coincident TBP of subthreshold excitatory post-synaptic potentials (EPSPs) and somatic action potentials induced no change in EPSC amplitude in the test (black circles) or control (white circles) pathways. The arrow indicates the timing of the TBP protocol. Example voltage traces show the initial burst of 5 coincident EPSPs and action potentials and a single test burst of 5 subthreshold EPSPs. Example current traces from a single experiment illustrating the mean EPSC response during the baseline (1) and at 30–35 minutes (2) in the test and control pathways.Right - TBP does induce LTP in the presence of the Kv7 channel inhibitor XE-991 (ab120089). In the presence of XE-991 (10 µM), coincident TBP of subthreshold EPSPs and somatic action potentials induced pathway-specific LTP.
实验方案
To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.
文献 (30)
ab120089 被引用在 30 文献中.
- Simkin D et al. Dyshomeostatic modulation of Ca2+-activated K+ channels in a human neuronal model of KCNQ2 encephalopathy. Elife 10:N/A (2021). PubMed: 33544076
- Kania A et al. RLN3/RXFP3 Signaling in the PVN Inhibits Magnocellular Neurons via M-like Current Activation and Contributes to Binge Eating Behavior. J Neurosci 40:5362-5375 (2020). PubMed: 32532885
- Sahu G et al. Junctophilin Proteins Tether a Cav1-RyR2-KCa3.1 Tripartite Complex to Regulate Neuronal Excitability. Cell Rep 28:2427-2442.e6 (2019). PubMed: 31461656
- Soh H et al. Deletion of KCNQ2/3 potassium channels from PV+ interneurons leads to homeostatic potentiation of excitatory transmission. Elife 7:N/A (2018). PubMed: 30382937
- Mani BK et al. Kv7.5 Potassium Channel Subunits Are the Primary Targets for PKA-Dependent Enhancement of Vascular Smooth Muscle Kv7 Currents. Mol Pharmacol 89:323-34 (2016). PubMed: 26700561