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

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

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PZM21 構造式

PZM21 構造式

CAS 番号 : 1997387-43-5

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 在庫あり
Solution
10 mM * 1 mL in DMSO USD 121 在庫あり
Solid
5 mg USD 110 在庫あり
10 mg USD 160 在庫あり
50 mg USD 380 在庫あり
100 mg USD 600 在庫あり
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Based on 4 publication(s) in Google Scholar

PZM21 関連抗体

Top Publications Citing Use of Products

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

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製品説明

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

IC50 & Target

μ Opioid Receptor/MOR

 

体外実験

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].

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

PZM21 関連抗体
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

361.50

分子式

C19H27N3O2S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@@H](C)CC1=CSC=C1)NC[C@@H](N(C)C)CC2=CC=C(O)C=C2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (276.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.57%

COA (244 KB) HNMR (213 KB) LCMS (495 KB)

取扱説明書 (2659 KB)
参考文献
動物実験
[1]

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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7663 mL 13.8313 mL 27.6625 mL 69.1563 mL
5 mM 0.5533 mL 2.7663 mL 5.5325 mL 13.8313 mL
10 mM 0.2766 mL 1.3831 mL 2.7663 mL 6.9156 mL
15 mM 0.1844 mL 0.9221 mL 1.8442 mL 4.6104 mL
20 mM 0.1383 mL 0.6916 mL 1.3831 mL 3.4578 mL
25 mM 0.1107 mL 0.5533 mL 1.1065 mL 2.7663 mL
30 mM 0.0922 mL 0.4610 mL 0.9221 mL 2.3052 mL
40 mM 0.0692 mL 0.3458 mL 0.6916 mL 1.7289 mL
50 mM 0.0553 mL 0.2766 mL 0.5533 mL 1.3831 mL
60 mM 0.0461 mL 0.2305 mL 0.4610 mL 1.1526 mL
80 mM 0.0346 mL 0.1729 mL 0.3458 mL 0.8645 mL
100 mM 0.0277 mL 0.1383 mL 0.2766 mL 0.6916 mL
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PZM21 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PZM211997387-43-5PZM 21PZM-21Opioid ReceptorInhibitorinhibitorinhibit

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製品名:
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製品番号:
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