CB1/2 agonist 4
CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively.
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- No. CAS: 2772949-38-7
- Fòrmula: C27H45NO3
- Peso molecular:431.65
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Descripciòn
IC50 & Target
Ki: 1.1 nM (hCB1); 4.2 nM (hCB2)[1].
EC50: 15.09 nM (CB1); EC50: 1.16 nM (CB2)[1].
IC50: 0.8 μM, EC50: 0.12 μM (TRPV1)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
1.16 nM
Compound: 24
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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
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[PMID: 32340793] |
| CHO | EC50 |
15.09 nM
Compound: 24
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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
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[PMID: 32340793] |
| HEK293 | EC50 |
0.12 μM
Compound: 24
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Activation of human TRPV1 expressed in HEK293 cells assessed as calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay
Activation of human TRPV1 expressed in HEK293 cells assessed as calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay
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[PMID: 32340793] |
| HEK293 | EC50 |
11.1 μM
Compound: 24
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Activation of rat recombinant TRPA1 expressed in HEK293 cells assessed as calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay
Activation of rat recombinant TRPA1 expressed in HEK293 cells assessed as calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay
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[PMID: 32340793] |
| HEK293 | IC50 |
>100 μM
Compound: 24
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Antagonist activity at rat recombinant TRPA1 expressed in HEK293 cells assessed as AITC-induced increase of calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay
Antagonist activity at rat recombinant TRPA1 expressed in HEK293 cells assessed as AITC-induced increase of calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay
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[PMID: 32340793] |
| HEK293 | IC50 |
0.8 μM
Compound: 24
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Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as capsaicin-induced increase of calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as capsaicin-induced increase of calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay
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[PMID: 32340793] |
In Vitro
CB1/2 agonist 4 (compound 24) has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively[1].
CB1/2 agonist 4 (0.1 mM) can induce a stimulation of [35S]GTPγS binding to hCB1-CHO cell membranes with an EC50 value of 15.09 nM[1].
CB1/2 agonist 4 (0.1 mM) is able to slightly stimulate [35S]GTPγS binding to hCB2-CHO cell membranes, behaving as a weak partial agonist to CB2 receptors of 1.16 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CB1/2 agonist 4 (1, 3 and 4 mg/kg, i.p.) can activate TRPV1 channel and it behaved as a good TRPV1 agonist with an IC50 value of 0.8 μM and EC50 value of 0.12 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD-1 outbred mice[1]
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Dosage:1, 3 and 4 mg/kg
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Administration:1, 3 and 4 mg/kg, i.p.
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Result:Significantly reduced the late phase of formalin-induced nociceptive behaviour in a dose dependent manner and slightly decreased also the first phase of nociceptive response.
Chemical Information
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No. CAS 2772949-38-7
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Peso molecular 431.65
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Fòrmula C27H45NO3
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SMILES
O=C(NC1CC1)CCCCCCCOC2=CC(C(CCCCCC)(C)C)=CC(OC)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CB1/2 agonist 4 Related Classifications
HY-150030 Related Classifications
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