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PZM21

Catalog No. T4386   CAS 1997387-43-5

PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).

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PZM21 Chemical Structure
PZM21, CAS 1997387-43-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 44.00
5 mg In stock $ 97.00
10 mg In stock $ 168.00
25 mg In stock $ 297.00
50 mg In stock $ 513.00
100 mg In stock $ 747.00
1 mL * 10 mM (in DMSO) In stock $ 116.00
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Purity: 99.59%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).
Targets&IC50 μ opioid receptor:1.8 nM (EC50)
In vitro 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 [1].
In vivo PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. Unlike morphine, PZM21 is more efficacious for the affective component of analgesia versus the reflexive component and is devoid of both respiratory depression and morphine-like reinforcing activity 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 [1].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 [2].
Molecular Weight 361.5
Formula C19H27N3O2S
CAS No. 1997387-43-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27.5 mg/mL (76.07 mM)

TargetMolReferences and Literature

1. Manglik A, et al. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Sep 8;537(7619):185-190. 2. Kostic M, et al. Biasing Opioid Receptors and Cholesterol as a Player in Developmental Biology.

Related compound libraries

This product is contained In the following compound libraries:
ReFRAME Related Library NO PAINS Compound Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Neurotransmitter Receptor Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Anti-Parkinson's Disease Compound Library

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Keywords

PZM21 1997387-43-5 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor Inhibitor PZM 21 inhibit PZM-21 inhibitor

 

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