1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. PM226

PM226 是一种选择性的大麻素 CB2R 激动剂 (Ki (CB2R)=13 nM;EC50 (CB2R)=39 nM;Ki (CB1R) >40 μM),在体内外均具有神经保护特性。

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PM226 Chemical Structure

PM226 Chemical Structure

CAS No. : 1949726-13-9

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  • 生物活性

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  • 参考文献

生物活性

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[1].

IC50 & Target[1]

CB2

13 nM (Ki)

CB2

39 nM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
38.6 nM
Compound: 43
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
[PMID: 27309150]
HEK293 IC50
4.2 nM
Compound: 43
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
[PMID: 27309150]
体外研究
(In Vitro)

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].

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

体内研究
(In Vivo)

PM226 (0.1, 1 and 10 mg/kg; administered i.p.) administration decreases the volume of the striatal lesion caused by Malonate[2].

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

Animal Model: Malonate-lesioned adult (12 week old; 350-400 g) male Wistar rats[2]
Dosage: 0.1, 1 and 10 mg/kg
Administration: Administered i.p.
Result: Reduced the volume of edema observed in Malonate-lesioned rats at the dose of 1 mg/kg.
分子量

357.49

Formula

C22H31NO3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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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PM226
目录号:
HY-136238
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