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Submit ReviewPB 28 dihydrochloride is a high affinity σ2 receptor agonist (Ki values are 0.8 and 15.2 nM for σ2 and σ1 receptors respectively) that displays minimal affinity at other receptors. Inhibits electrically evoked twitch in guinea pig bladder and ileum (EC50 values are 2.62 and 3.96 μM respectively). Displays antiproliferative and cytotoxic effects in SK-N-SH neuroblastoma and C6 glioma cells.
分子量 | 443.5 |
公式 | C24H38N2O.2HCl |
储存 | Desiccate at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 172907-03-8 |
PubChem ID | 46861545 |
InChI Key | DSRBJOQIBXACIV-UHFFFAOYSA-N |
Smiles | COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3.Cl.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 | 8.87 | 20 温和加热 |
以下数据基于产品分子量 443.5。 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 | 11.27 mL | 56.37 mL | 112.74 mL |
1 mM | 2.25 mL | 11.27 mL | 22.55 mL |
2 mM | 1.13 mL | 5.64 mL | 11.27 mL |
10 mM | 0.23 mL | 1.13 mL | 2.25 mL |
参考文献是支持产品生物活性的出版物。
Berardi et al (1996) New σ and 5-HT1A receptor ligands: ω-(tetralin-1-yl)-n-alkylamine derivatives. J.Med.Chem. 39 176 PMID: 8568804
Colabufo et al (2003) A new method for evaluating σ2 ligand activity in the isolated guinea-pig bladder. Naunyn-Schmied.Arch.Pharmacol. 368 106
Colabufo et al (2004) Antiproliferative and cytotoxic effects of some σ2 agonists and σ1 antagonists in tumour cell lines. Naunyn-Schmied.Arch.Pharmacol. 370 106
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关键词: PB 28 dihydrochloride, PB 28 dihydrochloride supplier, High, affinity, σ2, sigma2, agonists, Receptors, PB28, dihydrochloride, Sigma2, 2562, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PB 28 dihydrochloride 的部分引用包括:
Rennekamp et al (2016) σ1 receptor ligands control a switch between passive and active threat responses. Nat Chem Biol 12 552 PMID: 27239788
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Cell viability MTT assay. Sigma-2 receptor ligand PB28 at low concentration (1-10uM) promotes cellular viability in the presence of toxin paraquat, while high concentration (100uM) kills cells.