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Submit ReviewPK-THPP is a potent TASK-3 channel blocker (IC50 = 35 and 300 nM for TASK-3 and TASK-1 respectively). Increases breathing rate and induces respiratory alkalosis in rats.
PK-THPP is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 468.59 |
公式 | C29H32N4O2 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 1332454-07-5 |
PubChem ID | 53464059 |
InChI Key | CJZGRIRZVHNUSM-UHFFFAOYSA-N |
Smiles | O=C(C1=CC=C(C2=CC=CC=C2)C=C1)N(C3)CCC4=C3C(N5CCC(C(CCC)=O)CC5)=NC=N4 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 23.43 | 50 | |
1eq. HCl | 9.37 | 20 温和加热 |
以下数据基于产品分子量 468.59。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.27 mL | 21.34 mL | 42.68 mL |
2.5 mM | 0.85 mL | 4.27 mL | 8.54 mL |
5 mM | 0.43 mL | 2.13 mL | 4.27 mL |
25 mM | 0.09 mL | 0.43 mL | 0.85 mL |
参考文献是支持产品生物活性的出版物。
Cotten (2013) TASK-1 (KCNK3) and TASK-3 (KCNK9) tandem pore potassium channel antagonists stimulate breathing in isoflurane-anesthetized rats. Anesth.Analg. 116 810 PMID: 23460565
Coburn et al (2012) Discovery of a pharmacologically active antagonist of the two-pore-domain potassium channel K2P9.1 (TASK-3). ChemMedChem 7 123 PMID: 21916012
If you know of a relevant reference for PK-THPP, please let us know.
关键词: PK-THPP, PK-THPP supplier, potent, TASK3, channels, blockers, TWIK, related, acid, sensitive, K+, two, pore, potassium, K2P9.1, subfamily, member, 9, Two-P, Potassium, Channels, 5338, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PK-THPP 的部分引用包括:
Veldkamp et al (2018) Neurokinin-3 receptor activation selectively prolongs atrial refractoriness by inhibition of a background K+ channel. Nat Commun 9 4357 PMID: 30341287
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平均评分: 4 (Based on 1 Review.)
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A very potent K2p channel blocker which was used to figure out the blocking activity as concentration of the blocker molecule increased. PK-THPP is a great antagonist molecule which shows channel obstructing properties which is concentration dependent.