| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Cannabinoid receptor 2 (CB2).
|
|---|---|
| ln Vitro |
MDA19 has an approximately 70-fold higher affinity for the human CB1 receptor and a 4-fold higher affinity for the human CB(2) receptor compared to the human CB1 receptor (K(i) = 43.3 +/- 10.3 vs 162.4 +/- 7.6 nM). periods. K(i) = 16.3 +/- 2.1 vs. 1130 +/- 574 nM for rat CB2 vs. rat CB1 receptor. MDA19 functioned as an agonist at rat CB1 receptors, human CB1 and CB2 receptors, and inversely as an agonist at rat CB2 receptors in guanosine triphosphate (GTP)gamma[(35)S] functional tests. In the 3',5'-cyclic adenosine monophosphate (cAMP) experiment, MDA19 functioned as an agonist at the rat CB1 receptor but did not exhibit any functional activity at the rat CB(2) receptor. In the test for extracellular signal-regulated kinase 1 and 2.
MDA19 binds to human CB2 with Ki of 43.3 nM and activates CB2 with EC50 of 63.4 nM for functional activation. It shows 14-fold selectivity for CB2 over CB1 in cell-based functional assays (EC50 CB2 = 63.4 nM vs. CB1 = 867 nM). Interestingly, it acts as an inverse agonist at rat CB2 receptors in cell-based functional assays. |
| ln Vivo |
Rat CB2 receptors are agonistically activated by MDA19. MDA19, but not CB2(-/-) mice, dose-dependently reduces the tactile allodynia caused by spinal nerve ligation or paclitaxel in rats and CB2(+/+) mice. This suggests that the CB2 receptor mediates the role of MDA19. In rats, MDA19 has no effect on locomotor activity.
MDA19 attenuates tactile allodynia in a rat model of neuropathic pain without affecting locomotor capacity. By targeting CB2 receptors, MDA19 modulates immune cell activity and inflammatory responses without eliciting the psychoactive effects associated with CB1 activation. |
| Enzyme Assay |
CB1 and CB2 receptor binding affinity is measured using radioligand binding assays. Membrane preparations from cells expressing human or rat CB1/CB2 receptors are incubated with [³H]-CP-55,940 or other radiolabeled cannabinoid ligands and varying concentrations of MDA19. Specific binding is determined to calculate Ki values.
|
| Cell Assay |
CB2 receptor functional activity is assessed in cells expressing human or rat CB2 receptors. Cells are treated with MDA19, and downstream signaling (e.g., cAMP inhibition, ERK phosphorylation) is measured. EC50 values for receptor activation are determined. For inverse agonist activity, constitutive receptor activity is measured.
|
| Animal Protocol |
MDA19 is evaluated in rat models of neuropathic pain (e.g., chronic constriction injury or spinal nerve ligation). MDA19 is administered via intraperitoneal or oral routes. Mechanical allodynia and thermal hyperalgesia are assessed using von Frey filaments and paw withdrawal latency tests. Locomotor activity is monitored in open field tests.
|
| ADME/Pharmacokinetics |
MDA19 has molecular weight 349.43 and formula C21H23N3O2. It is soluble in DMSO and stable at +4°C. As a CB2-selective agonist, it is primarily used in preclinical studies of pain and inflammation. Detailed PK parameters are available in primary research publications.
|
| Toxicity/Toxicokinetics |
Preclinical toxicity data for MDA19 are limited. It does not affect rat locomotor activity at analgesic doses, suggesting a lack of CNS side effects associated with CB1 activation. Standard toxicological assessments would be required for clinical development.
|
| References |
|
| Additional Infomation |
MDA19 is a research tool for studying CB2 receptor biology, pain mechanisms, and immune modulation. It has no approved therapeutic applications. Its mechanism involves selective activation of CB2 receptors, which modulates inflammatory and neuropathic pain pathways without psychoactive effects. It is used primarily in preclinical pain research.
|
| Molecular Formula |
C21H23N3O2
|
|---|---|
| Molecular Weight |
349.434
|
| Exact Mass |
349.179
|
| CAS # |
1048973-47-2
|
| PubChem CID |
135743701
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Index of Refraction |
1.607
|
| LogP |
4.99
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
26
|
| Complexity |
476
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ICNRTDOKKSWDRL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H23N3O2/c1-2-3-4-10-15-24-18-14-9-8-13-17(18)19(21(24)26)22-23-20(25)16-11-6-5-7-12-16/h5-9,11-14,26H,2-4,10,15H2,1H3
|
| Chemical Name |
N-(1-hexyl-2-hydroxyindol-3-yl)iminobenzamide
|
| Synonyms |
MDA19; MDA 19; MDA-19
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~14.29 mg/mL (~40.90 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.43 mg/mL (4.09 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 1.43 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2862 mL | 1.4309 mL | 2.8618 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
