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Submit ReviewPotent, non-competitive excitatory amino acid transporter (EAAT) blocker. Preferentially inhibits glutamate-induced [3H]D-aspartate release (IC50 = 1.2 μM) rather than [3H]L-glutamate uptake (IC50 = 16.9 μM). Moderately selective; displays no affinity for NMDA and metabotropic glutamate receptors, and low affinity for AMPA and kainate receptors (IC50 values are 35 and 45 μM respectively).
分子量 | 172.14 |
公式 | C6H8N2O4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 227619-65-0 |
PubChem ID | 90488748 |
InChI Key | RDIJEATTYWWNKA-ACIRMZHZSA-N |
Smiles | OC1=NO[C@@]2([H])[C@@]([H])1CN[C@@H]2[C@@](O)=O.OC3=NO[C@]4([H])[C@]([H])3CN[C@H]4C(O)=O |
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.
参考文献是支持产品生物活性的出版物。
Conti et al (1999) Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists. J.Med.Chem. 42 4099 PMID: 10514280
Funicello et al (2004) Dissociation of [3H]glutamate uptake from glutamate-induced [3H]D-Aspartate release by 3-hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole-4-carboxylic acid and 3-hydroxy-4,5,6,6a-tetrahydro-3aH-pyrro Mol.Pharmacol. 66 522 PMID: 15322243
Conti et al (1999) Synthesis of new bicyclic analogues of glutamic acid. Tetrahedron 55 5623
关键词: (±)-HIP-B, (±)-HIP-B supplier, Potent, non-competitive, EAAT, inhibitors, inhibits, Excitatory, Amino, Acid, Transporters, GLAST, GLT-1, Glutamate, Monoamine, Neurotransmitter, 2218, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.