BAY38-7271
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- CAS號:
- 212188-60-8
- 英文名:
- (R)-3-(2-(hydroxymethyl)-2,3-dihydro-1H-inden-4-yloxy)phenyl 4,4,4-trifluorobutane-1-sulfonate
- 英文別名:
- 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
- 中文別名:
- 化合物 T14504;化合物 BAY 38-7271;(R)-3-(2-(羥甲基)-2,3-二氫-1H-茚-4-氧基)苯基 4,4,4-三氟丁烷-1-磺酸鹽
- CBNumber:
- CB22502634
- 分子式:
- C20H21F3O5S
- 分子量:
- 430.4379496
- MOL File:
- 212188-60-8.mol
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BAY38-7271化學(xué)性質(zhì)
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沸點:
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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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儲存條件:
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Store at -20°C
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酸度系數(shù)(pKa):
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14.81±0.10(Predicted)
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BAY38-7271性質(zhì)、用途與生產(chǎn)工藝
bay38 -7271 (KN 38-7271)是由化學(xué)家Wayne E. Kenney最初合成的一種藥物，是拜耳公司開發(fā)的一種大麻素受體激動劑。它具有鎮(zhèn)痛和神經(jīng)保護作用，并被用于科學(xué)研究，建議用于治療創(chuàng)傷性腦損傷。在動物實驗中，它是一種完全的激動劑，與CP 55,940的效力差不多，并且對CB1和CB2受體都有相當(dāng)高的親和力，在CB1處的Ki值為2.91nM，在CB2處為4.24nM。它已經(jīng)被授權(quán)給KeyNeurotek制藥公司進行臨床開發(fā)，并在2008年進入II期臨床試驗，但它的開發(fā)似乎已經(jīng)停止。
BAY 38-7271 是一個選擇性、高效的大麻素受體 CB1/CB2 激動劑，對人重組 CB1 和 CB2 作用的 Ki 值分別為 1.85 nM 和 5.96 nM。BAY 38-7271 具有很強的神經(jīng)保護特性。
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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
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS編號 | 包裝 | 價格 |
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| 2025/05/22 | HY-119744 | BAY38-7271
BAY 38-7271 | 212188-60-8 | 1 mg | 5400元 |
| 2023/03/20 | HY-119744 | BAY38-7271
BAY 38-7271 | 212188-60-8 | 5mg | 5800元 |
212188-60-8, BAY38-7271 相關(guān)搜索:
- Pharmaceutical intermediate
- 抑制劑
- C20H21F3O5S
- 化合物 BAY 38-7271
- 化合物 T14504
- (R)-3-(2-(羥甲基)-2,3-二氫-1H-茚-4-氧基)苯基 4,4,4-三氟丁烷-1-磺酸鹽
- 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