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
製品の概要
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製品名
XE-991 dihydrochloride, KCNQ channel blocker; blocks M current -
製品の詳細
Potent, selective KCNQ channel blocker; blocks M current -
生理活性の詳細
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 番号
122955-13-9 -
構造式
製品の特性
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体系名
10,10-Bis(4-pyridinylmethyl)-9(10H)-anthracenone dihydrochloride
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分子量
449.40 -
分子式
C26H20N2O.2HCl -
PubChem 登録番号
45073462 -
保存方法
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
溶解性
Soluble in water to 100 mM
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使用に関する注意
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 線形表記
C1=CC=C2C(=C1)C(=O)C3=CC=CC=C3C2(CC4=CC=NC=C4)CC5=CC=NC=C5.Cl.Cl -
由来
Synthetic
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研究分野
画像
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2D chemical structure image of ab120089, XE-991 dihydrochloride, KCNQ channel blocker; blocks M current
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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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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.
プロトコール
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.
参考文献 (30)
ab120089 は 30 報の論文で使用されています。
- 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