BAY38-7271
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- CAS号:
- 212188-60-8
- 英文名:
- (R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate
- 英文别名:
- KN 38-7271;BAY 38-7271;BAY-38-7071;O-1861 (R-form);BAY 38 7271,BAY 387271;BAY38-7271 CAS NO.212188-60-8;(R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate;(R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate USP/EP/BP;4,4,4-Trifluoro-1-butanesulfonic acid 3-[[(2R)-2,3-dihydro-2-(hydroxymethyl)-1H-inden-4-yl]oxy]phenyl ester;1-Butanesulfonic acid, 4,4,4-trifluoro-,3-[[(2R)-2,3-dihydro-2-(hydroxyMethyl)-1H-inden-4-yl]oxy]phenyl ester
- 中文名:
- BAY38-7271
- 中文别名:
- 化合物 T14504;(R)-3-(2-(羟甲基)-2,3-二氢-1H-茚-4-氧基)苯基 4,4,4-三氟丁烷-1-磺酸盐
- CBNumber:
- CB22502634
- 分子式:
- C20H21F3O5S
- 分子量:
- 430.4379496
- MOL File:
- 212188-60-8.mol
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BAY38-7271化学性质
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沸点:
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527.2±50.0 °C(Predicted)
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密度:
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1.350±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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酸度系数(pKa):
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14.81±0.10(Predicted)
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BAY38-7271性质、用途与生产工艺
bay38 -7271 (KN 38-7271)是由化学家Wayne E. Kenney最初合成的一种药物，是拜耳公司开发的一种大麻素受体激动剂。它具有镇痛和神经保护作用，并被用于科学研究，建议用于治疗创伤性脑损伤。在动物实验中，它是一种完全的激动剂，与CP 55,940的效力差不多，并且对CB1和CB2受体都有相当高的亲和力，在CB1处的Ki值为2.91nM，在CB2处为4.24nM。它已经被授权给KeyNeurotek制药公司进行临床开发，并在2008年进入II期临床试验，但它的开发似乎已经停止。
BAY 38-7271 是一个选择性、高效的大麻素受体 CB1/CB2 激动剂，对人重组 CB1 和 CB2 作用的 Ki 值分别为 1.85 nM 和 5.96 nM。BAY 38-7271 具有很强的神经保护特性。
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CB1
1.85 nM (Ki)
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CB2
5.96 nM (Ki)
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BAY 38-7271 shows only minor interactions at the micromolar range with other binding sites such as adenosine A
3
receptor (IC
50
= 7.5 μM), peripheral GABA
A
benzodiazepine receptor (IC
50
= 971 nM), melatonin ML
1
receptor (IC
50
= 3.3 μM), and at the monoamine transporter (IC
50
= 1.7 μM).
BAY 38-7271 (Ed
50
= 0.02 mg/kg; i.v. and 0.5 mg/kg; i.p.) induces a potent and dose-de-pendent reduction in core body temperature.
BAY 38-7271 has low physical dependence liability and is not essentially different from that of other cannabinoid CB
1
receptor agonists.
BAY 38-7271 (1-1000 ng/kg/h; i.v. infusion; for 4 hours) shows neuroprotective efficacy in the rat SDH model.
BAY 38-7271 also has neuroprotective efficacy in models of transient and permanent occlusion of the middle cerebral artery and brain edema models.
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Animal Model:
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Wistar rat ,TBI rat models (acute subdural hematoma, SDH)
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Dosage:
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1 ng/kg/h, 10 ng/kg/h, 100 ng/kg/h, 1000 ng/kg/h
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Administration:
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Intravenous infusion, for 4 hours
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Result:
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Reduced the mean infarct volume.
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BAY38-7271
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2023/03/20 | HY-119744 | BAY38-7271
BAY 38-7271 | 212188-60-8 | 5mg | 5800元 |
| 2023/03/20 | HY-119744 | BAY38-7271
BAY 38-7271 | 212188-60-8 | 10mg | 9800元 |
212188-60-8, BAY38-7271 相关搜索:
- Pharmaceutical intermediate
- C20H21F3O5S
- 化合物 T14504
- (R)-3-(2-(羟甲基)-2,3-二氢-1H-茚-4-氧基)苯基 4,4,4-三氟丁烷-1-磺酸盐
- 212188-60-8
- BAY 38 7271,BAY 387271
- BAY38-7271 CAS NO.212188-60-8
- (R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate USP/EP/BP
- 4,4,4-Trifluoro-1-butanesulfonic acid 3-[[(2R)-2,3-dihydro-2-(hydroxymethyl)-1H-inden-4-yl]oxy]phenyl ester
- 1-Butanesulfonic acid, 4,4,4-trifluoro-,3-[[(2R)-2,3-dihydro-2-(hydroxyMethyl)-1H-inden-4-yl]oxy]phenyl ester
- BAY-38-7071
- O-1861 (R-form)
- KN 38-7271
- BAY 38-7271
- (R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate