| Bioactivity | UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions[1]. | ||||||||||||
| Invitro | UNC9995(10 μM;1 小时)预处理原代星形胶质细胞,使它受IL-6(300 ng/mL;24 小时)诱导后,STAT3 和 β-arrestin2 的结合得到增强。它还抑制 STING、TBK1、JAK 的激活[1]。UNC9995(1、5、10 和 20 μM;1 小时)能够消除细胞凋亡和炎症,当用 IL-6 (300 ng/mL;24 小时) 刺激 WT 和 Arrb2−/− 星形胶质细胞后[1]。 Western Blot Analysis[1] Cell Line: | ||||||||||||
| In Vivo | UNC9995(2 mg/kg/天,腹腔注射,2 周)在小鼠的慢性社交失败应激 (CSDS) 模型和慢性不可预知轻度应激 (CUMS) 模型中,改善了抑郁样行为表型并改善海马体中星形胶质细胞的丢失[1]。 Animal Model: | ||||||||||||
| Name | UNC9995 | ||||||||||||
| CAS | 1354030-52-6 | ||||||||||||
| Formula | C20H21Cl2N3OS | ||||||||||||
| Molar Mass | 422.37 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Liu Y, et al. β-Arrestin2-biased Drd2 agonist UNC9995 alleviates astrocyte inflammatory injury via interaction between β-arrestin2 and STAT3 in mouse model of depression. J Neuroinflammation. 2022 Oct 1;19(1):240. |