Mizacorat是一种有效的、口服活性非甾体类选择性糖皮质激素受体调节剂 (SGRM),其 IC50 为 3.8 nM。在与 SCW 联合炎症的模型中,Mizacorat 展现了显著的抗炎疗效,适用于慢性炎症性疾病的研究。


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| 描述 | Mizacorat is a potent, orally active, non-steroidal and selective glucocorticoid receptor modulator (SGRM) with an IC50 of 3.8 nM. It has demonstrated superior efficacy in a streptococcal cell wall (SCW) reactivation model of joint inflammation[1]. |
| Concentration | Treated Time | Description | References | |
| primary CD4+ T cells | 0.01 µM–10 µM | 24 hours and 48 hours | AZD9567 triggered luciferase expression even at the lowest concentration tested (0.01 µM) | J Virol. 2025 Feb 25;99(2):e0188624 |
| U1 cells | 0.01 µM–10 µM | 48 hours and 96 hours | AZD9567 consistently reactivated HIV-1 in all cell lines tested | J Virol. 2025 Feb 25;99(2):e0188624 |
| ACH-2 cells | 0.01 µM–10 µM | 48 hours and 96 hours | AZD9567 consistently reactivated HIV-1 in all cell lines tested | J Virol. 2025 Feb 25;99(2):e0188624 |
| J-Lat 10.6 cells | 0.01 µM–10 µM | 48 hours and 96 hours | AZD9567 consistently reactivated HIV-1 in all cell lines tested | J Virol. 2025 Feb 25;99(2):e0188624 |
| Hela cells | 10 μM | 18 hours | GR ligand binding test, 16 compounds at 10 μM exhibit good inhibition activities (>70%) | Adv Sci (Weinh). 2022 Jan;9(3):e2102435 |
| Raw264.7 cells | 25 μM | 48 hours | Cytotoxicity test, 72 compounds do not affect cell viability at 25 μM | Adv Sci (Weinh). 2022 Jan;9(3):e2102435 |
| Animal study | Mizacorat inhibited SCW-induced ankle swelling in a rat model of joint inflammation when administered orally daily for 8 days at a dose of 15 mg/kg[1]. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.02mL 0.40mL 0.20mL |
10.11mL 2.02mL 1.01mL |
20.22mL 4.04mL 2.02mL |
|
| CAS号 | 1893415-00-3 |
| 分子式 | C27H28F2N4O3 |
| 分子量 | 494.53 |
| SMILES Code | CN1C(C=CC(N2N=CC3=CC(O[C@@H]([C@@H](NC(C(F)(C)F)=O)C(C)C)C4=CC=CC=C4)=CC=C32)=C1)=O |
| MDL No. | MFCD31619227 |
| 别名 | AZD9567 |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 105 mg/mL(212.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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