Trequinsin
Trequinsin (HL 725 free base) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin targets PDE3 with an IC50 of <1 nM. Trequinsin enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 79855-88-2
- 分子式: C24H27N3O3
- 分子量:405.50
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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PDE3 <1 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
10 μM
Compound: Trequinsin
|
TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells
TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells
|
[PMID: 12695538] |
| HEK293 | IC50 |
30 μM
Compound: Trequinsin
|
TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP5-expressing HEK293 cells
TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP5-expressing HEK293 cells
|
[PMID: 12695538] |
| Sf21 | IC50 |
12 μM
Compound: 2
|
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells
|
[PMID: 22023548] |
| Sf21 | IC50 |
25.4 μM
Compound: 2
|
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB2 expressed in baculovirus infected insect Sf21 cells
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB2 expressed in baculovirus infected insect Sf21 cells
|
[PMID: 22023548] |
Trequinsin (40 μM; 82 min) induces a high-magnitude increase in intracellular calcium in pooled capacitated human donor sperm, equivalent to 91% of the response evoked by 10 μM Progesterone (HY-N0437)[1].
Trequinsin (0.1-30 μM) induces a concentration-dependent increase in intracellular calcium in capacitated human donor sperm with an EC50 of 3.43 μM, exhibits efficacy equivalent to progesterone at 10 μM, and cross-desensitises with PGE1 but not progesterone[1].
Trequinsin (10 μM; 120 min) significantly and sustainably increases hyperactivated motility in capacitated human donor sperm (80% density gradient centrifugation fraction) without altering total or progressive motility[1].
Trequinsin (10 μM; 120 min) significantly increases progressive motility in poor-motility human donor sperm (40% density gradient centrifugation fraction) under both capacitating and non-capacitating conditions, and increases hyperactivated motility under capacitating conditions[1].
Trequinsin (10 μM; 120 min) increases hyperactivated motility in the majority of capacitated human patient sperm samples, with no effect on total or progressive motility in most cases[1].
Trequinsin (10 μM; 20 min) does not induce premature acrosome reaction in capacitated human donor sperm[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 79855-88-2
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分子量 405.50
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分子式 C24H27N3O3
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SMILES
O=C1N(C(=NC=2C(=CC(=CC2C)C)C)C=C3C=4C=C(OC)C(OC)=CC4CCN13)C
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別名
HL 725 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. McBrinn RC, et al. Novel pharmacological actions of trequinsin hydrochloride improve human sperm cell motility and function. Br J Pharmacol. 2019;176(23):4521-4536. [Content Brief]
[2]. Oquist NL, et al. Inotropic responses to selective (RO 20-1724 and SQ 65,442) and nonselective (trequinsin) inhibitors of cyclic AMP-specific class IV phosphodiesterase in newborn, immature, and adult rabbit myocardium. Pediatr Res. 1992;31(3):300-304. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
- Trequinsin
- 79855-88-2
- HL 725
- HL725
- HL-725
- Phosphodiesterase (PDE)
- intracellular cGMP
- phosphodiesterase inhibitor
- rabbit ventricular papillary muscles
- male infertility
- asthenozoospermia
- sperm potassium channel
- cyclic AMP-specific Class IV phosphodiesterase
- intracellular calcium
- CatSper channel
- cyclic GMP phosphodiesterase
- Inhibitor
- inhibitor
- inhibit