1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. MDA 19

MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity.

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MDA 19

MDA 19 Chemische Struktur

CAS. Nr. : 1048973-47-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

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Beschreibung

MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity[1][2].

Cellular Effect
Cell Line Type Value Description References
CHO EC50
63.4 nM
Compound: 33, MDA19
Agonist activity at human CB2 receptor expressed in CHO cells by [35S]GTPgammaS assay
Agonist activity at human CB2 receptor expressed in CHO cells by [35S]GTPgammaS assay
[PMID: 18666769]
CHO EC50
867 nM
Compound: 33, MDA19
Agonist activity at human CB1 receptor expressed in CHO cells by [35S]GTPgammaS assay
Agonist activity at human CB1 receptor expressed in CHO cells by [35S]GTPgammaS assay
[PMID: 18666769]
In Vitro

MDA19 displayed 4-fold-higher affinity at the human CB(2) than at the human CB1 receptor (K(i) = 43.3 +/- 10.3 vs 162.4 +/- 7.6 nM) and nearly 70-fold-higher affinity at the rat CB2 than at the rat CB1 receptor (K(i) = 16.3 +/- 2.1 vs 1130 +/- 574 nM). In guanosine triphosphate (GTP)gamma[(35)S] functional assays, MDA19 behaved as an agonist at the human CB1 and CB2 receptors and at the rat CB1 receptor but as an inverse agonist at the rat CB2 receptor. In 3',5'-cyclic adenosine monophosphate (cAMP) assays, MDA19 behaved as an agonist at the rat CB1 receptor and exhibited no functional activity at the rat CB(2) receptor. In extracellular signal-regulated kinases 1 and 2 activation assays.

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

In Vivo

MDA19 behaved as an agonist at the rat CB2 receptor. MDA19 attenuated tactile allodynia produced by spinal nerve ligation or paclitaxel in a dose-related manner in rats and CB2(+/+) mice but not in CB2(-/-) mice, indicating that CB2 receptors mediated the effects of MDA19. MDA19 did not affect rat locomotor activity.

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

Molekulargewicht

349.43

Formel

C21H23N3O2

CAS. Nr.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N/N=C1C(N(CCCCCC)C2=C\1C=CC=C2)=O)C3=CC=CC=C3

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 14.29 mg/mL (40.90 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 2.8618 mL 14.3090 mL 28.6180 mL
5 mM 0.5724 mL 2.8618 mL 5.7236 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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

In Vivo:

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    90% (20% SBE-β-CD in Saline)

    Solubility: 1.43 mg/mL (4.09 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.43 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.43 mg/mL (4.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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.
Reinheit & Dokumentation
Verweise

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 2.8618 mL 14.3090 mL 28.6180 mL 71.5451 mL
5 mM 0.5724 mL 2.8618 mL 5.7236 mL 14.3090 mL
10 mM 0.2862 mL 1.4309 mL 2.8618 mL 7.1545 mL
15 mM 0.1908 mL 0.9539 mL 1.9079 mL 4.7697 mL
20 mM 0.1431 mL 0.7155 mL 1.4309 mL 3.5773 mL
25 mM 0.1145 mL 0.5724 mL 1.1447 mL 2.8618 mL
30 mM 0.0954 mL 0.4770 mL 0.9539 mL 2.3848 mL
40 mM 0.0715 mL 0.3577 mL 0.7155 mL 1.7886 mL
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  • 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.

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