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Submit ReviewCo 101244 hydrochloride
说明： GluN2B-selective NMDA antagonist
别名： PD 174494,Ro 63-1908
化学名： 1-[2-(4-Hydroxyphenoxy)ethyl]-4-[(4-methylphenyl)methyl]-4-piperidinol hydrochloride
纯度： ≥99% (HPLC)
生物活性 for Co 101244 hydrochloride
Co 101244 hydrochloride is a novel, potent and selective antagonist of GluN2B (formally NR2B)-containing NMDA receptors (IC50 values are 0.043, > 100 and > 100 μM for GluN1A/2B (NR1A/2B), GluN1A/2A (NR1A/2A) and GluN1A/2C (NR1A/2C) subunit combinations respectively). Displays neuroprotective effects in vivo and in vitro.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
化合物库 for Co 101244 hydrochloride
Co 101244 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Co 101244 hydrochloride
| 分子量 | 377.91 |
| 公式 | C21H27NO3.HCl |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 193356-17-1 |
| PubChem ID | 6918426 |
| InChI Key | WFFZHKKSIDENAJ-UHFFFAOYSA-N |
| Smiles | Cl.CC1=CC=C(CC2(O)CCN(CCOC3=CC=C(O)C=C3)CC2)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Co 101244 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 37.79 | 100 | |
| DMSO | 18.9 | 50 |
制备储备液 for Co 101244 hydrochloride
以下数据基于产品分子量 377.91。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.65 mL | 13.23 mL | 26.46 mL |
| 5 mM | 0.53 mL | 2.65 mL | 5.29 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.65 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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产品说明书 for Co 101244 hydrochloride
参考文献 for Co 101244 hydrochloride
参考文献是支持产品生物活性的出版物。
Zhou et al (1999) 4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist. J.Med.Chem. 42 2993 PMID: 10425109
Gill et al (2002) Pharmacological characterization of Ro 63-1908 (1-[2-(4-hydroxy-phenoxy)-ethyl]-4-(4-methyl-benzyl)-piperidin-4-ol), a novel subtype-selective N-MthD.-aspartate antagonist. J.Pharmacol.Exp.Ther. 302 940 PMID: 12183650
Higgins et al (2003) Evaluation of the NR2B-selective NMDA receptor antagonist Ro 63-1908 on rodent behaviour: evidence for an involvement of NR2B NMDA receptors in response inhibition. Neuropharmacology 44 324 PMID: 12604092
If you know of a relevant reference for Co 101244 hydrochloride, please let us know.
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关键词: Co 101244 hydrochloride, Co 101244 hydrochloride supplier, selective, NR2B, antagonists, Glutamate, NMDA, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, Co101244, hydrochloride, PD174494, Ro63-1908, GluN2B, PD, 174494, Ro, 63-1908, 2456, Tocris Bioscience
3 篇 Co 101244 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Co 101244 hydrochloride 的部分引用包括：
Mirante et al (2014) Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala. Am J Physiol Renal Physiol 7 62 PMID: 25071439
Peng et al (2008) TRPV1 mediates the uterine capsaicin-induced NMDA NR2B-dependent cross-organ reflex sensitization in anesthetized rats. Neuroscience 295 F1324 PMID: 18632800
Quillinan et al (2015) Region-specific role for GluN2B-containing NMDA receptors in injury to Purkinje cells and CA1 neurons following global cerebral ischemia. J Cell Biol 284 555 PMID: 25450957
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Impact of Co-101244 on current transfer through neutrophil cell membrane.
By
Sergiy Sylantyev on 07/13/2023
分析类型： In Vitro
种属： Human
细胞系/组织： Blood
Co-101244 was used to quantify the input of GluN2B-containing NMDA receptors into electrical current flow through the membrane of human neutrophil. Figure; normalized electrical response of a single neutrophil after application of Co-101244 (bar +Co).
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