PM226
PM226 is a selective cannabinoid CB2R agonist (Ki (CB2R)=13 nM; EC50 (CB2R)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo.
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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。
- CAS 番号: 1949726-13-9
- 分子式: C22H31NO3
- 分子量:357.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
IC50 & Target
[1]|
CB2 13 nM (Ki) |
CB2 39 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
38.6 nM
Compound: 43
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Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method
Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method
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[PMID: 27309150] |
| HEK293 | IC50 |
4.2 nM
Compound: 43
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Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins by HTRF assay
Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins by HTRF assay
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[PMID: 27309150] |
体外実験
PM226 binds selectively to CB2 receptor with an affinity in the nanomolar range (Ki=12.8±2.4 nM). PM226 has negligible affinity for the CB1 receptor (Ki >40000 nM) and no activity at the GPR55. PM226 was also evaluated in GTPγS binding assays specific to the CB2 receptor showing agonist activity (EC50=38.67±6.70 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Malonate-lesioned adult (12 week old; 350-400 g) male Wistar rats[2]
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Dosage:0.1, 1 and 10 mg/kg
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Administration:Administered i.p.
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Result:Reduced the volume of edema observed in Malonate-lesioned rats at the dose of 1 mg/kg.
化学情報
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CAS 番号 1949726-13-9
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分子量 357.49
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分子式 C22H31NO3
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SMILES
CC1(C)OC2=CC(C(C)(C)CCCCCC)=CC(OC)=C2C3=C1C=NO3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Gemma Navarro, et al. Targeting Cannabinoid CB2 Receptors in the Central Nervous System. Medicinal Chemistry Approaches with Focus on Neurodegenerative Disorders. Front Neurosci. 2016 Sep 13;10:406. [Content Brief]
[2]. M Gómez-Cañas, et al. Biological characterization of PM226, a chromenoisoxazole, as a selective CB2 receptor agonist with neuroprotective profile. Pharmacol Res. 2016 Aug;110:205-215. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PM226 関連分類
HY-136238 関連分類
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