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- 详细信息
- 技术资料
- 保存条件：
-20°C, sealed storage, away from moisture
- 英文名：
ICI 136753 hydrochloride
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1135210-68-2
- 规格：
1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 1 mg | 产品价格： | ￥296.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥740.0 |
| 规格： | 10 mg | 产品价格： | ￥1190.0 |
| 规格： | 25 mg | 产品价格： | ￥2520.0 |
| 规格： | 50 mg | 产品价格： | ￥4000.0 |
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Tracazolate hydrochloride
CAS No. : 1135210-68-2
MCE 国际站：Tracazolate hydrochloride
产品活性：Tracazolate (ICI 136753) hydrochloride 是一种有效的 GABAA 受体调节剂。Tracazolate hydrochloride 对 β3 具有选择性，同时增强 α1β1γ2s (EC50=13.2μM) 和 α1β3γ2 (EC50=1.5 μM)。Tracazolate hydrochloride 的效力 (EC50) 是由受体复合物中的第三亚基 (γ1-3, δ, ε) 的性质决定。Tracazolate hydrochloride 具有抗焦虑和抗惊厥活性。
研究领域：Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点：GABA Receptor
In Vitro: 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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