1967811-46-6

1967811-46-6 structure

1967811-46-6 structure

Name: ACT-777991
Chemical Name: ACT-777991
CAS Number: 1967811-46-6
Molecular Formula: C₂₀H₂₀F₆N₈O₂S
Molecular Weight: 550.48
Catalog: Signaling Pathways GPCR/G Protein CXCR
Create Date: 2023-04-30 10:14:49
Modify Date: 2024-02-23 21:09:05
ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11[1].

Name	ACT-777991

Description	ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11[1].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> CXCR Research Areas >> Inflammation/Immunology Signaling Pathways >> Immunology/Inflammation >> CXCR
Target	CXCR3
In Vitro	ACT-777991 在 CHO 细胞中抑制 hEGR，IC50 值为 26 μM[1]。 ACT-777991（1 μM；45 分钟）在人类、大鼠和狗的微粒体和肝细胞中稳定[1]。 ACT-777991（0.01-1 μM）抑制人和小鼠激活的 T 细胞向 CXCL11 的迁移，IC50 范围分别为 3.2-64 nM 和 4.9-21 nM[1]。 ACT-777991（1 nM、5 nM、20 nM 和 50 nM）抑制 CXCR3 介导的人和小鼠 T 细胞趋化性[1]。
In Vivo	ACT-777991（0.5 mg/kg，1 mg/kg；静脉注射；单次剂量）在雄性 Wistar 大鼠 (14/156) 或 Beagle 犬 (5/15) 中具有低体内血浆清除率[1]。 ACT-777991（0.006-2 mg/g 食物；口服；在 LPS 处理前 3 天开始给药，LPS 处理后 72 小时结束）剂量依赖性地抑制小鼠模型体内 CXCR3+ T 细胞的趋化性[1]。 Animal Model: LPS challenge model in mice[1] Dosage: 0.006, 0.02, 0.06, 0.2, 0.6, and 2 mg per g of food Administration: PO; started 3 days before LPS challenge and continued up to the end of the study (72 h post LPS challenge) Result: Reduced the number of BAL CD8+ T cells in a dose-dependent manner.
References	[1]. Meyer EA, et al. Discovery of Clinical Candidate ACT-777991, a Potent CXCR3 Antagonist for Antigen-Driven and Inflammatory Pathologies. J Med Chem. 2023 Mar 23;66(6):4179-4196.

Molecular Formula	C₂₀H₂₀F₆N₈O₂S
Molecular Weight	550.48