Tertiapin Q，blocker of inward-rectifier r K+ channels (ab120432)
Key features and details
- Potent inward rectifier K+ channel blocker
- CAS Number: 252198-49-5
- Soluble in water
- Form / State: Solid
- Source: Synthetic
概述
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产品名称
Tertiapin Q，blocker of inward-rectifier r K+ channels -
描述
Potent inward rectifier K+ channel blocker -
生物学描述
Potent blocker of inward rectifier K+ channels. Stable analog of the bee venom tertiapin. High affinity for ROMK1 and GIRK1/4 (Ki values are 1.3 and 13.3 nM, respectively). Displays >250-fold selectivity over many other Kir subtypes.
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常规说明
Sold under license granted by the University of Pennsylvania. -
CAS编号
252198-49-5 -
化学结构
性能
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分子量
2452.01 -
分子式
C106H175N35O24S4 -
序列
ALCNCNRIIIPHQCWKKCGKK (Modifications: C-terminal amide; Disulfide bonds: 3-14, 5-18) -
PubChem识别号
92131436 -
存放说明
Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
溶解度概述
Soluble in water -
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 week. 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.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
CC[C@H](C)[C@H]1C(=O)NC(C(=O)N[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H]3CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC3=O)CC4=CNC5=CC=CC=C54)CCCCN)CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N)C(=O)N[C@H](C(=O)N1)CC(=O)N)CC(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)N)CCC(=O)N)CC6=CNC=N6)[C@@H](C)CC)[C@@H](C)CC -
来源
Synthetic
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研究领域
图片
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Chemical Structure - Tertiapin Q, blocker of inward-rectifier r K+ channels (ab120432)2D chemical structure image of ab120432, Tertiapin Q, blocker of inward-rectifier r K+ channels
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Cellular activation - Tertiapin Q, blocker of inward-rectifier r K+ channels (ab120432)Image from Montalbano A, et al. Plos One, 10(10), e0140369. Fig 3,; doi: 10.1371/journal.pone.0140369Tertiapin Q, blocker of inward-rectifier r K+ channels
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 (8)
ab120432 被引用在 8 文献中.
- Djebari S et al. G-Protein-Gated Inwardly Rectifying Potassium (Kir3/GIRK) Channels Govern Synaptic Plasticity That Supports Hippocampal-Dependent Cognitive Functions in Male Mice. J Neurosci 41:7086-7102 (2021). PubMed: 34261700
- Huang Y et al. GIRK1-mediated inwardly rectifying potassium current suppresses the epileptiform burst activities and the potential antiepileptic effect of ML297. Biomed Pharmacother 101:362-370 (2018). PubMed: 29499411
- Berry MH et al. Restoration of patterned vision with an engineered photoactivatable G protein-coupled receptor. Nat Commun 8:1862 (2017). PubMed: 29192252
- Bragança B et al. Ion Fluxes through KCa2 (SK) and Cav1 (L-type) Channels Contribute to Chronoselectivity of Adenosine A1 Receptor-Mediated Actions in Spontaneously Beating Rat Atria. Front Pharmacol 7:45 (2016). PubMed: 27014060
- Montalbano A et al. Pharmacological Characterization of 5-HT1A Autoreceptor-Coupled GIRK Channels in Rat Dorsal Raphe 5-HT Neurons. PLoS One 10:e0140369 (2015). PubMed: 26460748
- Murthy M et al. Role for germline mutations and a rare coding single nucleotide polymorphism within the KCNJ5 potassium channel in a large cohort of sporadic cases of primary aldosteronism. Hypertension 63:783-9 (2014). PubMed: 24420545
- Vilar B et al. Alleviating pain hypersensitivity through activation of type 4 metabotropic glutamate receptor. J Neurosci 33:18951-65 (2013). PubMed: 24285900
- Murthy M et al. Characterization of a novel somatic KCNJ5 mutation delI157 in an aldosterone-producing adenoma. J Hypertens 30:1827-33 (2012). PubMed: 22743686
