MDA 19
Based on 2 publication(s) in Google Scholar
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.80%
- CAS 番号: 1048973-47-2
- 分子式: C21H23N3O2
- 分子量:349.43
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 MDA 19
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
63.4 nM
Compound: 33, MDA19
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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
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[PMID: 18666769] |
| CHO | EC50 |
867 nM
Compound: 33, MDA19
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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
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[PMID: 18666769] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1048973-47-2
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性状 Solid
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分子量 349.43
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分子式 C21H23N3O2
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Color Light yellow to yellow
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SMILES
O=C(N/N=C1C(N(CCCCCC)C2=C\1C=CC=C2)=O)C3=CC=CC=C3
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別名
BZO-HEXOXIZID
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Biol Direct
MDA19, a novel CB2 agonist, inhibits hepatocellular carcinoma partly through inactivation of AKT signaling pathway. [Abstract]2019 May 3;14(1):9. PMID: 31053086 -
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
Please enter the basic information of animal experiments:
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-
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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データシート (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Diaz, Philippe; Xu, Jijun; Astruc-Diaz, Fanny et al. Design and Synthesis of a Novel Series of N-Alkyl Isatin Acylhydrazone Derivatives that Act as Selective Cannabinoid Receptor 2 Agonists for the Treatment of Neuropathic Pain. Journal of Medicinal Chemistry (2008), 51(16), 4932-4947. [Content Brief]
[2]. Xu JJ, Diaz P, Astruc-Diaz F et al. Pharmacological characterization of a novel cannabinoid ligand, MDA19, for treatment of neuropathic pain. Anesth Analg. 2010 Jul;111(1):99-109. [Content Brief]
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 |