2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. 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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CB1/2 agonist 4 Chemical Structure

CB1/2 agonist 4 Chemical Structure

CAS No. : 2772949-38-7

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CB1/2 agonist 4 Related Antibodies

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Description

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[1].

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].
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.

CB1/2 agonist 4 Related Antibodies
In Vivo

CB1/2 agonist 4 (compound 24) (1, 3 and 4 mg/kg, i.p.) has a stronger antinociceptive activity[1].
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.

Animal Model: Male CD-1 outbred mice[1]
Dosage: 1, 3 and 4 mg/kg
Administration: 1, 3 and 4 mg/kg, i.p.
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.
Molecular Weight

431.65

Formula

C27H45NO3
CAS No.
SMILES

O=C(NC1CC1)CCCCCCCOC2=CC(C(CCCCCC)(C)C)=CC(OC)=C2
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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CB1/2 agonist 4 Related Classifications

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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.

Keywords:

CB1/2 agonist 42772949-38-7Cannabinoid ReceptorCB1 agonistCB2 agonistTRPV1cannabinoidneurologicalInhibitorinhibitorinhibit

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