1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. PZM21


Cat. No.: HY-101386 Purity: 99.45%
Handling Instructions

PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.

For research use only. We do not sell to patients.

PZM21 Chemical Structure

PZM21 Chemical Structure

CAS No. : 1997387-43-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 429 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
10 mg USD 780 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2340 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3180 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
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PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM[1][2][3].

IC50 & Target

EC50: 1.8 nM (μ opioid receptor)[1]

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 [1].

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 [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







O=C(N[[email protected]@H](C)CC1=CSC=C1)NC[[email protected]@H](N(C)C)CC2=CC=C(O)C=C2


Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 72 mg/mL (199.17 mM)

*"≥" means soluble, but saturation unknown.

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7663 mL 13.8313 mL 27.6625 mL
5 mM 0.5533 mL 2.7663 mL 5.5325 mL
10 mM 0.2766 mL 1.3831 mL 2.7663 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    PZM21 is dissolved in 100% DMSO and further diluted in saline containing 1% DMSO[3].

Animal Administration

Mice: PZM21 is dissolved in 0.9% sodium chloride. Mice are injected with PZM21 (10 mg/kg; 20 mg/kg; or 40 mg/kg). After injection of drug, the analgesic effect expressed as percentage maximum possible effect (%MPE) is measured at 15, 30, 60, 90 and 120 min after drug treatment[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Purity: 99.45%

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