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ChemicalBook Optimization Suppliers |
| 名前: |
Ascent Scientific |
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4401179829988 |
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customerservice@ascentscientific.co.uk |
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| 化学名: | | | 英語化学名: | UCPH-101 | | 别名: | UCPH-101;2-Amino-5,6,7,8-tetrahydro-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-4H-chromene-3-carbonitrile;4H-1-Benzopyran-3-carbonitrile, 2-aMino-5,6,7,8-tetrahydro-4-(4-Methoxyphenyl)-7-(1-naphthalenyl)-5-oxo-;2-Amino-4-(4-methoxy-phenyl)-7-naphthalen-1-yl-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile;UCPH-101; UCPH 101; UCPH101;CS-2757;2-amino-4-(4-methoxyphenyl)-7-(naphthalene-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile;inhibit,UCPH101,UCPH-101,Inhibitor | | CAS番号: | 1118460-77-7 | | 分子式: | C27H22N2O3 | | 分子量: | 422.48 | | EINECS: | | | カテゴリ情報: | Glutamate | | Mol File: | 1118460-77-7.mol |  |
| 融点 | 194.0-197.2 °C | | 沸点 | 703.5±60.0 °C(Predicted) | | 比重(密度) | 1.32±0.1 g/cm3(Predicted) | | 貯蔵温度 | Keep in dark place,Inert atmosphere,2-8°C | | 溶解性 | Soluble in DMSO (up to 10 mg/ml). | | 外見 | solid | | 酸解離定数(Pka) | 3.23±0.60(Predicted) | | 色 | Off-white | | 安定性： | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| | UCPH-101 Usage And Synthesis |
| 説明 | UCPH-101 is a noncompetitive inhibitor of excitatory amino acid transporter 1 (EAAT1), which takes up extracellular glutamate in the central nervous system. UCPH-1 is selective for EAAT1 over EAAT2 and EAAT3 with IC50 values of 0.66, >300, and >300 μM, respectively, in a radioligand uptake assay using HEK293 cells transfected with the human transporter. It selectively inhibits anion currents in tsA201 cells expressing human EAAT1 (Kd = 0.34 μM) over rat EAAT4 and mouse EAAT5 at concentrations up to 10 μM. UCPH-101 is orally bioavailable in rats at a dose of 10 mg/kg but does not cross the blood-brain barrier. | | 使用 | UCPH 101 is a subtype-selective inhibitor of human excitatory amino acid transporter subtype 1. | | IC 50 | EAAT1 | | 貯蔵 | Store at +4°C | | 参考文献 | 1) Jensen?et al.?(2009),?Discovery of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1; J. Med. Chem.,?52?912
2) Erichsen?et al.?(2010),?Structure-Activity Relationship Study of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101); J. Med. Chem.,?53?7180
3) Corbetta?et al.?(2019),?Altered function of the glutamate-aspartate transporter GLAST, a potential therapeutic target in glioblastoma; Int. J. Cancer,?144?2539 |
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