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PZM21
CAS No. 1997387-43-5
PZM21( PZM21 | PZM-21 | PZM 21 )
Catalog No. M18199 CAS No. 1997387-43-5
PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 87 | In Stock |
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| 10MG | 151 | In Stock |
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| 25MG | 267 | In Stock |
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| 50MG | 462 | In Stock |
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| 100MG | 672 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NamePZM21
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NoteResearch use only, not for human use.
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Brief DescriptionPZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).
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DescriptionPZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. PZM21 is an experimental opioid analgesic drug that is being researched for the treatment of pain. It is a functionally selective μ-opioid receptor agonist which produces μ-opioid receptor mediated G protein signaling, with potency and efficacy similar to morphine, but with less β-arrestin 2 recruitment. In tests on mice, PZM21 was slightly less potent than morphine or TRV130 as an analgesic, but also had significantly reduced adverse effects, with less constipation than morphine, and very little respiratory depression, even at high doses.
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In VitroPZM21 has no detectable κOR or nociceptin receptor agonist activity-it is actually an 18 nM κOR antagonist-while it is a 500-fold weaker δOR agonist, making it a selective μOR agonist.At hERG, PZM21 has an IC50 of between 2 and 4 μM, 500- to 1,000-fold weaker than its potency as a μOR agonist. Signalling by PZM21 and other μOR agonists appears to be mediated primarily by the heterotrimeric G protein Gi/o, as its effect on cAMP levels is eliminated by pertussis toxin and no activity is observed in a calcium release assay .
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In VivoPZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. PZM21 is efficacious for the affective component of analgesia versus the reflexive component and is devoid of respiratory depression in mice at equi-analgesic doses. PZM21 displays dose-dependent analgesia in a mouse hotplate assay, with a per cent maximal possible effect (% MPE) of 87% reached 15 min after administration of the highest dose of drug tested .PZM21 has a long-lasting analgesic effect on CNS mediated-pain responses, but does not cause respiratory depression and constipation, two key side effects of opioid agonists.
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SynonymsPZM21 | PZM-21 | PZM 21
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PathwayOthers
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TargetOther Targets
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Recptorμ-opioid receptor
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Research AreaNeurological Disease
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Indication——
Chemical Information
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CAS Number1997387-43-5
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Formula Weight361.5
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Molecular FormulaC19H27N3O2S
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 72 mg/mL; 199.17 mM
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SMILESOc1ccc(cc1)C[C@@H](CNC(=O)N[C@@H](C)Cc2ccsc2)N(C)C
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Chemical Name1-[(2S)-2-(Dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-[(2S)-1-(thiophen-3-yl)propan-2-yl]urea
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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