1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. CB1/2 agonist 2

CB1/2 agonist 2 (compound 23) 是一种有效的非选择性大麻素 (cannabinoid) 配体,其 Ki 分别为 3.5 nM 和 1.2 nM。CB1/2 agonist 2 可以作为 CB1 的完全激动剂和 CB2 竞争性反向激动剂。CB1/2 agonist 2 具有抗伤害活性。

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CB1/2 agonist 2 Chemical Structure

CB1/2 agonist 2 Chemical Structure

CAS No. : 2772379-97-0

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  • 生物活性

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生物活性

CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity[1].

IC50 & Target

hCB2-R

1.2 nM (Ki)

hCB1-R

3.5 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
397.9 nM
Compound: 23
Agonist activity at human CB2 receptor expressed in CHO cell membrane assessed as inhibition of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay
Agonist activity at human CB2 receptor expressed in CHO cell membrane assessed as inhibition of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay
[PMID: 32340793]
CHO EC50
6.21 nM
Compound: 23
Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay
Agonist activity at human CB1 receptor expressed in CHO cell membrane assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay
[PMID: 32340793]
体外研究
(In Vitro)

CB1/2 agonist 2 (compound 23) (1 µM, 24-72 h) exhibits a very low cytotoxic potential in Hep-G2 cells[1].
CB1/2 agonist 2 (0-10 µM) shows a slight but significant inhibition of [35S]GTPγS binding to hCB2-CHO cell membranes, with a mean EC50 of 397.90 nM and a mean Emax value of -17.81%[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: Human hepatoblastoma (Hep-G2) cells
Concentration: 1 µM
Incubation Time: 24, 48 or 72 h
Result: Exhibited a very low cytotoxic potential, as Hep-G2 cell viability was comparable to controls after 24-72 h of treatment.
体内研究
(In Vivo)

CB1/2 agonist 2 (compound 23) (0-6 mg/kg, IP, once) significantly reduces the late phase of formalin-induced nocifensive behaviour at 6 mg/kg[1].

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

Animal Model: Male CD-1 outbred mice (40-45 g)[1]
Dosage: 0, 1, 3, and 6 mg/kg
Administration: IP, once, 10 min before the formalin or saline injection
Result: Significantly reduced the late phase of formalin-induced nocifensive behaviour at the highest dose (6 mg/kg, i.p.), whereas no effect was produced by doses of 1 and 3 mg/kg.
分子量

417.62

Formula

C26H43NO3

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
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  • 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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CB1/2 agonist 2
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HY-150028
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