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| 货号 | 产品名 | 中文名称 | 产品描述 |
|---|---|---|---|
| SJ-MX3576 | SR3335 (ML 176) | SR3335 (also known as ML-176) is a novel and selective RORα inverse agonist with a Ki of 220 nM. SR3335 directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays. Furthermore, SR3335 suppresses the expression of endogenous RORα target genes in HepG2 involved in hepatic gluconeogenesis including glucose-6-phosphatase and phosphoenolpyruvate carboxykinase. Pharmacokinetic studies indicate that SR3335 displays reasonable exposure following an ip injection into mice. We assess the ability of SR3335 to suppress gluconeogenesis in vivo using a diet-induced obesity (DIO) mouse model where the mice where treated with 15 mg/kg b.i.d., ip for 6 days followed by a pyruvate tolerance test. SR3335-treated mice displayed lower plasma glucose levels following the pyruvate challenge consistent with suppression of gluconeogenesis. Thus, SR3335 was identified as the first selective synthetic RORα inverse agonist, and this compound can be utilized as a chemical tool to probe the function of this receptor both in vitro and in vivo. Additionally, the data suggests that RORα inverse agonists may hold utility for suppression of elevated hepatic glucose production in type 2 diabetics. | |
| SJ-MX0712 | T0901317 |
TT0901317 是一种有效的，选择性的性肝 X 受体 (LXR)和FXR激动剂，对 LXRα 和FXR的EC50分别约为20 nM和5 μM。T0901317 是 RORα 和 RORγ 的双重反向激动剂，对应的Ki值分别为132 nM和51 nM。T0901317 可显着抑制细胞增殖并诱导凋亡 (apoptosis)，并抑制低密度脂蛋白 (LDL) 受体缺失小鼠动脉粥样硬化的发展。 |
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| SJ-MX2456 | Cintirorgon (LYC-55716) | Cintirorgon (LYC-55716) 是一种首创的、选择性的，具有口服活性的 RORγ 激动剂。Cintirorgon (LYC-55716) 调节 RORγ 表达的 T 淋巴细胞免疫细胞的基因表达，增强效应子功能，降低免疫抑制，降低肿瘤生长，提高生存率 。 | |
| SJ-MX2455 | SR1078 | SR1078 是一种视黄酸受体相关孤儿受体 (RORα/RORγ) 激动剂。SR1078 直接与 RORα和 RORγ的配体结合区结合，提高了这些受体的转录活性，从而刺激了 RORα/γ靶基因的转录。 | |
| SJ-MX2457 | SR1001 | SR1001 是选择性的 RORα和 RORγt 反向激动剂，Ki 分别为 172 和 111 nM。 | |
| SJ-MX2458 | GSK2981278 | GSK2981278 是一种有效的，选择性的 RORγ反向激动剂。 GSK2981278 可以抑制 il17 启动子的激活并干扰 RORγ-DNA 结合。 | |
| SJ-MN0603 | Nobiletin | 川陈皮素 | Nobiletin 是一种来自柑橘皮的聚甲氧基黄酮，可改善记忆力丧失，是一种 RORs 激动剂。Nobiletin 可以降低分化的 C2C12 肌管中的 ROS 的水平，并具有抗炎和抗癌特性，包括抗血管生成，抗增殖，抗转移和诱导细胞凋亡。 |
| SJ-MX3970 | SR0987 | SR 0987 is an agonist of RORγt with EC50 value of ~800 nM for inducing reporter gene expression. | |
| SJ-MX1592 | GSK805 | GSK805 是一种有效，生物可利用的，CNS 穿透性的 RORγt 抑制剂。 | |
| SJ-MX5702 | AZD-0284 |
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