A μ-opioid receptor agonist
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PZM21

Item No. 20576

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-N'-[(1S)-1-methyl-2-(3-thienyl)ethyl]-urea
CAS Number
1997387-43-5
Molecular Formula
C19H27N3O2S
Formula Weight
361.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 1 mg/mlEthanol: 10 mg/mlEthanol:PBS (pH 7.2) (1:4): 0.2 mg/ml
λmax
229, 281 nm
SMILES
OC1=CC=C(C[C@H](N(C)C)CNC(N[C@@H](C)CC2=CSC=C2)=O)C=C1
InChi Code
InChI=1S/C19H27N3O2S/c1-14(10-16-8-9-25-13-16)21-19(24)20-12-17(22(2)3)11-15-4-6-18(23)7-5-15/h4-9,13-14,17,23H,10-12H2,1-3H3,(H2,20,21,24)/t14-,17-/m0/s1
InChi Key
MEDBIJOVZJEMBI-YOEHRIQHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

    $128

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    10 mg

    $181

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    25 mg

    $270

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    Product Description

    PZM21 is a μ-opioid receptor agonist (Ki = 1.1 nM).1 It is selective for μ- over κ- and δ-opioid receptors (Kis = 18 and 506 nM, respectively). PZM21 induces Gi/o signaling (EC50 = 4.6 nM in HEK293T cells expressing human receptors) but has no detectable activity in a β-arrestin2 recruitment assay. In vivo, PZM21 (10, 20, and 40 mg/kg) induces analgesia in the hot plate test and reduces formalin-induced paw licking in mice when administered at a dose of 40 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Manglik, A., Lin, H., Aryal, D.K., et al. Structure-based discovery of opioid analgesics with reduced side effects. Nature 537(7619), 185-190 (2016).