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Submit ReviewTrequinsin hydrochloride is a highly potent inhibitor of cGMP-inhibited phosphodiesterase (PDE3; IC50 = 250 pM). Potently inhibits arachidonic acid-induced aggregation of human platelets (IC50 = 50 pM). Orally active antihypertensive agent; reduces systemic blood pressure in both normotensive and hypertensive animal models. Also activates CatSper channels, increases intracellular Ca2+ and cGMP levels, and decreases potassium channel activity in sperm.
Trequinsin hydrochloride 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 | 441.95 |
公式 | C24H27N3O3.HCl |
储存 | Desiccate at RT |
纯度 | ≥97% (HPLC) |
CAS Number | 78416-81-6 |
PubChem ID | 3060974 |
InChI Key | DTCZZBVPTHVXFA-UHFFFAOYSA-N |
Smiles | Cl.COC1=C(OC)C=C2C(CCN3C(=O)N(C)C(\C=C23)=N\C2=C(C)C=C(C)C=C2C)=C1 |
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 | 44.2 | 100 | |
ethanol | 44.2 | 100 |
以下数据基于产品分子量 441.95。 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 |
---|---|---|---|
1 mM | 2.26 mL | 11.31 mL | 22.63 mL |
5 mM | 0.45 mL | 2.26 mL | 4.53 mL |
10 mM | 0.23 mL | 1.13 mL | 2.26 mL |
50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
参考文献是支持产品生物活性的出版物。
Ruppert and Weithmann (1982) HL 725, an extremely potent inhibitor of platelet phosphodiesterase and induced platelet aggregation in vitro. Life Sci. 31 2037 PMID: 6294426
Lal et al (1984) Trequinsin, a potent new antihypertensive vasodilator in the series of 2-(arylimino)-3-alkyl-9,10-dimethoxy-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-ones. J.Med.Chem. 27 1470 PMID: 6492077
Agarwal et al (1987) Role of plasma adenosine in the antiplatelet action of HL 725, a potent inhibitor of cAMP phosphodiesterase: species differences. Thromb.Res. 47 191 PMID: 2821650
McBrinn et al (2019) Novel pharmacological actions of Trequinsin Hydrochloride improve human sperm cell motility and function. Br.J.Pharmacol. PMID: 31368510
If you know of a relevant reference for Trequinsin hydrochloride, please let us know.
关键词: Trequinsin hydrochloride, Trequinsin hydrochloride supplier, Ultrapotent, inhibitors, inhibits, PDE3, Phosphodiesterases, HL725, Catsper, activators, activates, sperm, motility, HL-725, Other, Calcium, Channels, 2337, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Trequinsin hydrochloride 的部分引用包括:
McBrinn et al (2019) Novel pharmacological actions of Trequinsin Hydrochloride improve human sperm cell motility and function. Br.J.Pharmacol. 176 4521 PMID: 31368510
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