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PZM21
🥰Excellent
Catalog No. T4386Cas No. 1997387-43-5
PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).
PZM21
🥰Excellent
Purity: 99.59%
Catalog No. T4386Cas No. 1997387-43-5
PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $39 | In Stock | |
| 2 mg | $55 | In Stock | |
| 5 mg | $89 | In Stock | |
| 10 mg | $129 | In Stock | |
| 25 mg | $215 | In Stock | |
| 50 mg | $313 | In Stock | |
| 100 mg | $496 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $98 | In Stock |
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Purity:99.59%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 highly selective μOR activator with significant Gi activation and minimal activation of β-arrestin-2, differentiating it from morphine by demonstrating greater efficacy in the affective aspect of pain relief compared to the reflexive aspect, without causing respiratory depression or exhibiting morphine-like addictive qualities in mice at equivalent analgesic doses. In a mouse hotplate assay, PZM21 achieved a maximal effect of 87% for pain relief 15 minutes post-administration of the highest dose [1]. Furthermore, PZM21 exerts a durable analgesic effect on central nervous system (CNS)-mediated pain without the typical opioid-induced side effects of respiratory depression and constipation [2]. |
| Molecular Weight | 361.5 |
| Formula | C19H27N3O2S |
| Cas No. | 1997387-43-5 |
| Smiles | C[C@@H](Cc1ccsc1)NC(=O)NC[C@H](Cc1ccc(O)cc1)N(C)C |
| Relative Density. | 1.169 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 27.5 mg/mL (76.07 mM)  | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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