PZM21

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Cat.No. 7218 - PZM21 | C19H27N3O2S | CAS No. 1997387-43-5
Description: Selective μ receptor agonist
Chemical Name: N-[(2S)-2-(Dimethylamino)-3-(4-hydroxyphenyl)propyl]-N'-[(1S)-1-methyl-2-(3-thienyl)ethyl]urea
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (5)

Biological Activity for PZM21

PZM21 is a selective μ receptor agonist (EC50 = 4.6 nM). PZM21 has been reported to exhibit bias for the Gi signaling pathway over arrestin-3. The compound exhibits 500-fold selectivity for μ over δ receptors and no detectable activity at κ or nociceptin receptors and a panel of 316 other GPCRs. PZM21 induces analgesia in a mouse hot plate assay, but not a tail-flick assay and exhibits no significant conditioned place preference response in in vivo assays. CNS penetrant.

Technical Data for PZM21

M. Wt 361.5
Formula C19H27N3O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1997387-43-5
PubChem ID 121596705
InChI Key MEDBIJOVZJEMBI-YOEHRIQHSA-N
Smiles C[C@H](NC(NC[C@@H](N(C)C)CC1=CC=C(C=C1)O)=O)CC2=CSC=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PZM21

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.15 100
ethanol 36.15 100

Preparing Stock Solutions for PZM21

The following data is based on the product molecular weight 361.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.77 mL 13.83 mL 27.66 mL
5 mM 0.55 mL 2.77 mL 5.53 mL
10 mM 0.28 mL 1.38 mL 2.77 mL
50 mM 0.06 mL 0.28 mL 0.55 mL

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References for PZM21

References are publications that support the biological activity of the product.

Manglik et al (2016) Structure-based discovery of opioid analgesics with reduced side effects. Nature 537 185 PMID: 27533032

Hill et al (2018) The novel μ-opioid receptor agonist PZM21 depresses respiration and induces tolerance to antinociception. Br.J.Pharmacol. 175 2653 PMID: 29582414


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Keywords: PZM21, PZM21 supplier, selective, mu, opioid, receptor, agonist, μ, analgesic, brain, penetrant, Mu, Opioid, Receptors, 7218, Tocris Bioscience

Citations for PZM21

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Literature in this Area

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