AZ599
AZ599 is a mixed CB1/CB2 cannabinoid receptor agonist with an EC50 of 49 nM and a Ki of 120 nM for the human CB1 receptor, and a Ki of 9 nM for the human CB2 receptor. AZ599 inhibits hERG potassium channels and CYP enzymes. AZ599 can be used for research on chronic pain.
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- CAS No.: 910798-82-2
- Formule: C25H35N3O4S
- Masse moléculaire:473.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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CB1 49 nM (EC50) |
CB1 120 nM (Ki) |
CB2 9 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
49 nM
Compound: 5, AZ599
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Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding
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[PMID: 22607668] |
| HEK293-EBNA | EC50 |
49 nM
Compound: 29
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Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay
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[PMID: 22284817] |
In Vitro
AZ599 is a potent agonist at the human CB1 receptor with an EC50 of 49 nM in HEK 293 EBNA cell membranes[1].
AZ599 demonstrates metabolic stability in human liver microsomes with a value of 52 μL/min/mg[1].
AZ599 demonstrates good permeability in Caco-2 cells with a Papp of 13 × 10−6 cm/s and a low efflux ratio of 1.5 in MDR1/MDCK cells[1].
AZ599 exhibits a favorable physicochemical profile with an aqueous solubility of 0.48 mg/mL, ClogP of 2.4, and PSA of 67[1].
AZ599 has low CYP inhibition potential with IC50 values greater than 20 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4[1].
AZ599 shows moderate hERG activity with an IC50 of 3.1 μM using voltage ion flux electrophysiology assay[1].
AZ599 (compound 5) binds to human cannabinoid receptors hCB1 and hCB2 with Ki values of 120 nM and 9 nM, respectively[2].
AZ599 acts as a full agonist at hCB1 with an EC50 of 49 nM and an Emax of 120%[2].
AZ599 inhibits the hERG potassium channel with an IC50 of 3.1 μM[2].
AZ599 (1 μM) has a human intrinsic clearance of 52 μL/min/mg in human liver microsomes[2].
AZ599 (10 μM) has a Caco-2 permeability of 13 × 10-6 cm/s[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat Carrageenan (HY-125474)
inflammatory pain model[1] -
Dosage:0.35 mg/kg; 0.70 mg/kg; 1.4 mg/kg
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Administration:s.c.
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Result:Exhibited dose-dependent reversal of heat hyperalgesia.
Achieved total plasma concentrations of 126-213 nM.
Achieved brain concentrations of 10-13 nM.
Did not cause severe side effects associated with central CB1 receptor activation.
Chemical Information
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CAS No. 910798-82-2
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Masse moléculaire 473.63
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Formule C25H35N3O4S
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SMILES
O=C(C=1C=CC2=C(C1)C3=C(N2S(=O)(=O)CC)CCN(C3)C4CCOCC4)N5CCC(C)CC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AZ599 Related Classifications
HY-121022 Related Classifications
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