货号:A190802 同义名: 巴氯酚 / (±)-Baclofen
Baclofen, a gamma-amino-butyric acid derivative, is a selective GABAB agonist with IC50 of 200 nM which used as a skeletal muscle relaxant.
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | GABA receptor ↓ ↑ | GABAA receptor ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Niflumic Acid | ✔ | 98% | |||||||||||||||||
Ginkgolide A |
++
GABA receptor, Ki: 14.5 μM |
98% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC,Autophagy | 97% | ||||||||||||||||
Flumazenil | ✔ | 95% | |||||||||||||||||
Bemegride | ✔ | 98% | |||||||||||||||||
Bicuculline |
+++
GABAA receptor, IC50: 2 μM |
98+% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA-B receptor (GABABR) agonist. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[3]. Intrathecal baclofen infusion is an accepted treatment for spasticity[4]. Baclofen pretreatment (3 mg/kg) not only prolonged the time taken for animals to reach a core body temperature of 40 degrees C[5]. Moreover, repeated pretreatment attenuates baclofen-attributed neurotoxicity in overdose and results in post-discontinuation withdrawal syndrome[6]. In high-dose baclofen participants only, there was a predictive effect of lower baseline heart rate variability and fewer post-test percentage of heavy drinking days. There was a dose-specific rescuing effect of high-dose baclofen on the dynamic modulation of cardiovascular responses to eliciting cues[7]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00814632 | Vulvodynia | Phase 2 | Completed | - | United States, Michigan ... 展开 >> William Beaumont Hospital Royal Oak, Michigan, United States, 48073 收起 << |
NCT01244113 | Cerebral Palsy | Not Applicable | Completed | - | Korea, Republic of ... 展开 >> Severance Hospital Seoul, Korea, Republic of, 120-752 收起 << |
NCT02771925 | Alcohol Dependence | Phase 4 | Unknown | May 2018 | India ... 展开 >> Dyanand Medical College and Hospital Recruiting Ludhiana, Punjab, India, 141001 Contact: Sandeep Singh Sidhu, MD,DM +919814025085 sandeepsidhu1963@gmail.com Contact: Omesh Goyal, MD,DM +919914821155 goyalomesh@yahoo.co.in Principal Investigator: Sandeep Singh Sidhu, MD,DM 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.68mL 0.94mL 0.47mL |
23.40mL 4.68mL 2.34mL |
46.80mL 9.36mL 4.68mL |
CAS号 | 1134-47-0 |
分子式 | C10H12ClNO2 |
分子量 | 213.661 |
别名 | 巴氯酚 ;(±)-Baclofen |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 4 mg/mL(18.72 mM),配合低频超声,水浴加热至45℃,并调节pH至4,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 2 mg/mL(9.36 mM),配合低频超声助溶 0.1 M HCL: 10 mg/mL(46.8 mM),配合低频超声助溶 |
动物实验配方 |