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 |
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| 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 (compound 29) binds to the human CB1 receptor with a Ki of 120 nM in HEK 293s cell membranes[1].
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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