PZM21
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
100mg | $780 | In Stock |
250mg | $1450 | In Stock |
500mg | $2175 | In Stock |
Cat #: V8817 CAS #: 1997387-43-5 Purity ≥ 98%
Description: PZM21 is a novel, potent and selective Gi activator with exceptional selectivity for μ opioid receptor (μOR) and minimal β-arrestin-2 recruitment with an EC50 of 1.8 nM.
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Molecular Weight (MW) | 361.50 |
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Molecular Formula | C19H27N3O2S |
CAS No. | 1997387-43-5 |
Protocol | In Vitro | PZM21 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 Vivo | PZM21 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 |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.7663 mL | 13.8313 mL | 27.6625 mL | 55.3250 mL |
5mM | 0.5533 mL | 2.7663 mL | 5.5325 mL | 11.0650 mL |
10mM | 0.2766 mL | 1.3831 mL | 2.7663 mL | 5.5325 mL |
20mM | 0.1383 mL | 0.6916 mL | 1.3831 mL | 2.7663 mL |
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