Orexin A (Hypocretin-1) (human, rat, mouse) acetate 是一种具有镇痛特性的下丘脑神经肽 (可透过血脑屏障)。Orexin A (human, rat, mouse) acetate 结合并激活两种 G 蛋白偶联受体,即 Orexin-1 受体 (OX1R) 和 Orexin-2 受体 (OX2R)。Orexin A (human, rat, mouse) acetate 可用于食欲调节、神经退行性疾病,以及调节伤害性信息传递的研究。
BPRMU191 是一种 μ-阿片受体 (MOR) 调节剂,通过将小分子吗啡类拮抗剂转变为 G 蛋白偏向的 MOR 激动剂,诱导 MOR 激活,从而发挥镇痛作用。BPRMU191 与吗啡类拮抗剂联合使用,可在减少副作用的同时提供 MOR-依赖性镇痛效果,显著降低了胃肠功能障碍、抗伤害性感受耐受性以及依赖性不良反应。BPRMU191 与吗啡类拮抗剂的联合应用可作为研究重度疼痛的潜在策略,同时为研究 G 蛋白偶联受体调节提供了新思路。
莱苞迪苷D
Rebaudioside D 是一种口服有效的甜味剂,靶向激活 FXR、调节 Acetyl-CoA Carboxylase 和抑制 3-hydroxy-3-methylglutaryl-CoA reductase。Rebaudioside D 调控胆汁酸稳态与脂质代谢,降低脂肪酸与胆固醇的合成速率,具有抗脂肪生成、保肝、抗脂肪变性、调节肠道菌群、增强次级胆汁酸代谢、抗内毒素、调控胆汁酸转运及抑制胆汁酸外排等多重作用。Rebaudioside D 还减少体重增长、内脏脂肪堆积、肝脏甘油三酯与胆固醇蓄积、肝脏脂质过氧化,并降低循环中脂多糖结合蛋白的水平。Rebaudioside D 还增强肠道细菌次级胆汁酸代谢通路,上调回肠有机溶质转运蛋白 α 的基因表达,下调肝脏胆盐输出泵蛋白的基因表达。Rebaudioside D 不影响葡萄糖稳态、改变总热量摄入或粪便能量排泄、诱导体重增加、加重肥胖、促进肝脏脂肪变性、损伤棕色脂肪组织功能,也不会改变骨骼肌代谢相关蛋白。Rebaudioside D 可用于饮食诱导肥胖及肥胖相关研究。
转录是 DNA 中遗传信息转化为蛋白质的第一步,也是调控基因表达的重要环节。蛋白编码基因的转录是由 RNA 聚合酶 II 和被称为转录因子 (TFs) 的一系列辅助蛋白完成。转录因子在细胞生长、分化和对环境信号的响应的长期调控中发挥重要的作用。转录因子调节失调与多种疾病发生有关,如糖尿病,炎症相关疾病及癌症等。因此这些转录因子作为药物靶点具有较高疾病治疗价值。
POI 指目标蛋白(Protein of Interest),即分子胶作用中需被降解或调控功能的致病蛋白或关键功能蛋白。分子胶 POI库是由一系列可特异性结合不同类型 POI 的小分子片段组成的。这些配体作为分子胶的关键组成部分,可与靶蛋白形成稳定结合,为分子胶诱导 POI 与 E3 泛素连接酶相互作用奠定基础,其涵盖的 POI 包括癌症相关的 GSPT1、雄激素受体以及神经退行性疾病相关的异常聚集蛋白等多种类型。
该片段库可应用于靶向蛋白降解剂筛选与优化,通过筛选库中对特定 POI 亲和力高、选择性强的配体,可以发现核心结构,开发新型分子胶,如针对 GSPT1 的配体经优化后,得到了降解活性更优的分子胶降解剂。由于许多 POI 因缺乏传统小分子结合口袋难以成药,POI 配体库中部分配体可通过诱导蛋白相互作用的方式调控这类 POI,进一步拓展 “不可成药” 靶标药物研发空间。
Orexin A (Hypocretin-1) (human, rat, mouse) acetate 是一种具有镇痛特性的下丘脑神经肽 (可透过血脑屏障)。Orexin A (human, rat, mouse) acetate 结合并激活两种 G 蛋白偶联受体,即 Orexin-1 受体 (OX1R) 和 Orexin-2 受体 (OX2R)。Orexin A (human, rat, mouse) acetate 可用于食欲调节、神经退行性疾病,以及调节伤害性信息传递的研究。
莱苞迪苷D
Rebaudioside D 是一种口服有效的甜味剂,靶向激活 FXR、调节 Acetyl-CoA Carboxylase 和抑制 3-hydroxy-3-methylglutaryl-CoA reductase。Rebaudioside D 调控胆汁酸稳态与脂质代谢,降低脂肪酸与胆固醇的合成速率,具有抗脂肪生成、保肝、抗脂肪变性、调节肠道菌群、增强次级胆汁酸代谢、抗内毒素、调控胆汁酸转运及抑制胆汁酸外排等多重作用。Rebaudioside D 还减少体重增长、内脏脂肪堆积、肝脏甘油三酯与胆固醇蓄积、肝脏脂质过氧化,并降低循环中脂多糖结合蛋白的水平。Rebaudioside D 还增强肠道细菌次级胆汁酸代谢通路,上调回肠有机溶质转运蛋白 α 的基因表达,下调肝脏胆盐输出泵蛋白的基因表达。Rebaudioside D 不影响葡萄糖稳态、改变总热量摄入或粪便能量排泄、诱导体重增加、加重肥胖、促进肝脏脂肪变性、损伤棕色脂肪组织功能,也不会改变骨骼肌代谢相关蛋白。Rebaudioside D 可用于饮食诱导肥胖及肥胖相关研究。
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.