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Submit ReviewPZM21 is a selective μ receptor agonist (EC50 = 4.6 nM). PZM21 has been reported to exhibit bias for the Gi signaling pathway over arrestin-3. The compound exhibits 500-fold selectivity for μ over δ receptors and no detectable activity at κ or nociceptin receptors and a panel of 316 other GPCRs. PZM21 induces analgesia in a mouse hot plate assay, but not a tail-flick assay and exhibits no significant conditioned place preference response in in vivo assays. CNS penetrant.
PZM21 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 | 361.5 |
公式 | C19H27N3O2S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1997387-43-5 |
PubChem ID | 121596705 |
InChI Key | MEDBIJOVZJEMBI-YOEHRIQHSA-N |
Smiles | C[C@H](NC(NC[C@@H](N(C)C)CC1=CC=C(C=C1)O)=O)CC2=CSC=C2 |
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 | 36.15 | 100 | |
ethanol | 36.15 | 100 |
以下数据基于产品分子量 361.5。 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 |
---|---|---|---|
1 mM | 2.77 mL | 13.83 mL | 27.66 mL |
5 mM | 0.55 mL | 2.77 mL | 5.53 mL |
10 mM | 0.28 mL | 1.38 mL | 2.77 mL |
50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
参考文献是支持产品生物活性的出版物。
Manglik et al (2016) Structure-based discovery of opioid analgesics with reduced side effects. Nature 537 185 PMID: 27533032
Hill et al (2018) The novel μ-opioid receptor agonist PZM21 depresses respiration and induces tolerance to antinociception. Br.J.Pharmacol. 175 2653 PMID: 29582414
If you know of a relevant reference for PZM21, please let us know.
关键词: PZM21, PZM21 supplier, selective, mu, opioid, receptor, agonist, μ, analgesic, brain, penetrant, Mu, Opioid, Receptors, 7218, 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!
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