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Submit ReviewTertiapin-Q
说明： Selective blocker of inward-rectifier K+ channels
纯度： ≥95% (HPLC)
生物活性 for Tertiapin-Q
Tertiapin-Q is a high affinity blocker for inward-rectifier K+ channels. Tertiapin-Q is a stable derivative of the bee venom toxin tertiapin. Tertiapin-Q binds to ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels with high affinity (Ki values are 1.3 and 13.3 nM respectively) and is selective over Kir2.1 channels. Tertiapin-Q improves heart rate and atrioventricular conduction in a mouse model of bradycardia. Derivative Tertiapin LQ (Cat. No. 4339) also available.
许可信息
Sold under license granted by the University of Pennsylvania
技术数据 for Tertiapin-Q
| 分子量 | 2452 |
| 公式 | C106H175N35O24S4 |
| 序列 |
ALCNCNRIIIPHQCWKKCGKK (Modifications: Disulfide bridges: 3-14, 5-18, Lys-21 = C-terminal amide) |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 910044-56-3 |
| PubChem ID | 90479782 |
| InChI Key | GMZAXHIZSCRCHM-MIPBWYARSA-N |
| Smiles | [H]N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC3=CNC=N3)NC(=O)[C@@H]3CCCN3C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC3=CNC4=C3C=CC=C4)NC2=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Tertiapin-Q
| 溶解性 | Soluble to 2 mg/ml in water |
产品说明书 for Tertiapin-Q
参考文献 for Tertiapin-Q
参考文献是支持产品生物活性的出版物。
Jin et al (1999) Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q. Biochemistry 38 14294 PMID: 10572004
Jin and Lu (1999) Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels. Biochemistry 38 14286 PMID: 10572003
Bidaud et al (2020) Inhibition of G protein-gated K + channels by tertiapin-Q rescues sinus node dysfunction and atrioventricular conduction in mouse models of primary bradycardia Sci.Rep. 10 9835 PMID: 32555258
If you know of a relevant reference for Tertiapin-Q, please let us know.
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关键词: Tertiapin-Q, Tertiapin-Q supplier, Potent, selective, blockers, inward-rectifier, K+, channels, Potassium, KIR, Channels, venoms, Inward, rectifier, 1316, Tocris Bioscience
10 篇 Tertiapin-Q 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Tertiapin-Q 的部分引用包括：
Llamosas et al (2017) Inactivation of GIRK channels weakens the pre- and postsynaptic inhibitory activity in dorsal raphe neurons. Physiol Rep 5 PMID: 28196855
Choisy et al (2012) Acute desensitization of acetylcholine and endothelin-1 activated inward rectifier K+ current in myocytes from the cardiac atrioventricular node. Biochem Biophys Res Commun 423 496 PMID: 22683635
Choisy et al (2012) Modulation by endothelin-1 of spontaneous activity and membrane currents of atrioventricular node myocytes from the rabbit heart. PLoS One 7 e33448 PMID: 22479400
Workman et al (2015) Rapid antidepressants stimulate the decoupling of GABAB receptors from GIRK/Kir3 channels through increased protein stability of 14-3-3η. Mol Psychiatry 20 298 PMID: 25560757
Marcott et al (2014) Phasic DA release drives rapid activation of striatal D2-receptors. Neuron 84 164 PMID: 25242218
Patel et al (2020) Structural Determinants Mediating Tertiapin Block of Neuronal Kir3.2 Channels. Biochemistry 59 836 PMID: 31990535
Chu et al (2013) Effects of stresscopin on rat hypothalamic paraventricular nucleus neurons in vitro. PLoS One 8 e53863 PMID: 23349753
Yi et al (2011) Sperm GIRK2-containing K+ inward rectifying channels participate in sperm capacitation and fertilization. Syst Biol Reprod Med 57 296 PMID: 22054410
Aguilar-Sanchez et al (2019) Transmural Autonomic Regulation of Cardiac Contractility at the Intact Heart Level. Front Physiol 10 773 PMID: 31333477
Stott et al (2015) Contribution of Kv7 channels to natriuretic peptide mediated vasodilation in normal and hypertensive rats. Hypertension 65 676 PMID: 25547342
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Tertiapin-Q 的评论
平均评分: 5 (基于 2 条评论。)
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Works as expected..
By
Anonymous on 05/26/2020
种属： Mouse
细胞系/组织： Bed nucleus of the stria terminalis
We performed ex-vivo slice physiology and pre-incubated the slices in tertiapin-Q (200 nM). Pre-incubation blocked inward rectifying channels.
Tertiapin-Q is a very potent Kir channel blocker even at low concentrations.
By
Anonymous on 10/31/2018
分析类型： In Vitro
种属： Human
The product shows great Kir channel blocking properties even at very small cocentrations, the data was reproducible every time.
