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Submit ReviewNESS 0327 is an ultra-high affinity and selective CB1 receptor antagonist (Ki = 350 fM). Exhibits >60-fold selectivity for CB1 over CB2 receptors. Antagonizes the inhibitory effects of WIN 55,212-2 (Cat. No. 1038) on electrically evoked contractions in mouse isolated vas deferens ex vivo. Also antagonizes the antinociceptive effect of WIN 55,212-2 in tail-flick and hot plate tests in vivo.
NESS 0327 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 | 489.82 |
公式 | C24H23Cl3N4O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 494844-07-4 |
PubChem ID | 10435654 |
InChI Key | NCXBPZJQQSNIRA-UHFFFAOYSA-N |
Smiles | O=C(NN1CCCCC1)C2=NN(C3=CC=C(Cl)C=C3Cl)C4=C2CCCC5=C4C=CC(Cl)=C5 |
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 | |||
DMSO | 9.8 | 20 |
以下数据基于产品分子量 489.82。 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 |
---|---|---|---|
0.2 mM | 10.21 mL | 51.04 mL | 102.08 mL |
1 mM | 2.04 mL | 10.21 mL | 20.42 mL |
2 mM | 1.02 mL | 5.1 mL | 10.21 mL |
10 mM | 0.2 mL | 1.02 mL | 2.04 mL |
参考文献是支持产品生物活性的出版物。
Ruiu et al (2003) Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor. J.Pharmacol.Exp.Ther. 306 363 PMID: 12663689
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关键词: NESS 0327, NESS 0327 supplier, NESS0327, cannabinoid, receptors, CB1, antagonists, antagonism, ultra, high, affinity, selective, Receptors, 5746, Tocris Bioscience
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.