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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 910798-82-2
- 分子式: C25H35N3O4S
- 分子量:473.63
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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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] |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 910798-82-2
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分子量 473.63
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AZ599 関連分類
HY-121022 関連分類
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