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Submit ReviewOrg 25543 hydrochloride is a potent and selective glycine transporter type 2 (GlyT2) inhibitor (IC50 = 16 nM for hGlyT2). Displays no activity at GlyT1 or 56 other common biological targets (≥ 100 μM), in a glycine uptake assay in CHO cells. Ameliorates mechanical allodynia after partial sciatic nerve ligation injury in mice.
Org 25543 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 448.98 |
公式 | C24H32lN2O4.HCl |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 495076-64-7 |
PubChem ID | 10095215 |
InChI Key | NIPQJILJYQVZJR-UHFFFAOYSA-N |
Smiles | O=C(NCC2(N(C)C)CCCC2)C1=CC(OC)=C(OCC3=CC=CC=C3)C(OC)=C1.Cl |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 8.98 | 20 | |
DMSO | 44.9 | 100 |
以下数据基于产品分子量 448.98。 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 | 2.23 mL | 11.14 mL | 22.27 mL |
5 mM | 0.45 mL | 2.23 mL | 4.45 mL |
10 mM | 0.22 mL | 1.11 mL | 2.23 mL |
50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
参考文献是支持产品生物活性的出版物。
Caulfield et al (2001) The first potent and selective inhibitors of the glycine transporter type 2. J.Med.Chem. 44 2679 PMID: 11495577
Morita et al (2008) Spinal antiallodynia action of glycine transporter inhibitors in neuropathic pain models in mice. J.Pharmacol.Exp.Ther. 326 633 PMID: 18448867
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