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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- 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.
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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
生物活性
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CB2 13 nM (Ki) |
CB2 39 nM (EC50) |
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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] |
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.
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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