Tracazolate hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tracazolate Hydrochloride 是 GABAA 受体的调节剂，具有抗焦虑和抗惊厥活性。

Tracazolate hydrochloride is a modulator of the GABAA receptor with anxiolytic and anticonvulsant activity. Tracazolate hydrochloride potentiates α1β1γ2s and α1β3γ2 with EC50s of 13.2 μM and 1.5 μM.(In Vitro):Tracazolate hydrochloride (10 μM) enhanced the sensitivity of α1β2δ-containing GABAA receptors and increased the maximum current amplitude in oocytes . Tracazolate hydrochloride inhibited α1β1ε, α1β3ε, α1β3, and α6β3γ with EC50s of 4.0 μM, 1.2 μM, 2.7 μM, and 1.1 μM. Tracazolate hydrochloride interacted with γ-aminobutyric acid GABAA receptors, adenosine receptors, and phosphodiesterases .

Tracazolate (ICI 136753) hydrochloride inhibits α1β1ε (EC50=4.0 μM) and α1β3ε (EC50=1.2 μM), α1β3 (EC50=2.7 μM) and α6β3γ (EC50=1.1 μM). Replacement of Ser265 within the β1 subunit with Asn (the β3 counterpart) increases the sensitivity of tracazolate, whereas the opposite mutation (Asnβ3 to Ser) decreases the sensitivity to Tracazolate. Tracazolate hydrochloride interacts with γ-aminobutyric acid GABAA receptors, adenosinereceptors, and phosphodiesterases.Tracazolate hydrochloride (10?μM) increases the maximum current amplitude and enhances the sensitivity of α1β2δ-containing GABAA receptors in oocytes.

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Tracazolate (hydrochloride)

Others

Other Targets

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1135210-68-2

340.85

C16H25ClN4O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (366.73 mM)

Cl.CCCCNc1c(C(=O)OCC)c(C)nc2n(CC)ncc12

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(-20℃)

With Ice Pack

≥ 2 years