Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7904 |
SR 19881
|
Estrogen/progestogen Receptor | Endocrinology/Hormones |
SR 19881 是 ERRγ 的完全激动剂(结合试验中的 EC50 值为 0.39 μM,基于细胞的试验中 EC50 值为 4.7 μM)。 | |||
T8779 |
HBT1
|
GluR | Neuroscience |
HBT1 是一种 AMPA 受体增强剂,可诱导脑源性神经营养因子 (BDNF) 的产生,并且在原代神经元中几乎没有激动作用。 HBT1 以谷氨酸依赖的方式与 AMPA-R 的配体结合结构域结合。 | |||
T13272 |
UT-155
|
Androgen Receptor | Endocrinology/Hormones |
UT-155 是雄激素受体选择性拮抗剂,能够与 AR-LBD 结合(Ki:267 nM)。 | |||
T75129 |
Luxdegalutamide
ARV-766 |
Androgen Receptor; PROTACs | Endocrinology/Hormones; PROTAC |
Luxdegalutamide (ARV-766) 是一种可口服且有效的蛋白水解靶向嵌合体 (PROTAC) 的蛋白质降解剂。Luxdegalutamide降解野生型雄激素受体 AR,也降解包括最普遍的致病性 AR L702H、H875Y 和 T878A 突变相关的 AR LBD 突变体。 | |||
T77549 |
Nurr1 agonist 2
|
Others | Others |
Nurr1 agonist 2 是一种 Nurr1 激动剂 ,EC50 值为 0.07 μM。Nurr1 agonist 2 增加 Nurr1 调节基因酪氨酸羟化酶 (TH) 和囊泡氨基酸转运蛋白 2 (VMAT2) 的 mRNA 表达。Nurr1 agonist 2 与重组 Nurr1 配体结合域 (LBD) 结合,Kd 值为 0.14 μM。Nurr1 agonist 2 可用于研究帕金森综合征。 | |||
T12406 |
PEPA
|
iGluR | Membrane transporter/Ion channel; Neuroscience |
PEPA 是一种变构 AMPA 受体调节剂,可与 GluA2o 和 GluA3o LBD 结合,可用作 AMPA 受体异质性的指标。 | |||
T8381 |
Amodiaquine
|
Others; Histone Methyltransferase; Parasite | Chromatin/Epigenetic; Microbiology/Virology; Others |
Amodiaquine 是一种合成的4-氨基喹啉类抗疟剂,是一种有口服活性的组胺 N-甲基转移酶抑制剂。它也是一种Nurr1激动剂,有抗炎活性,可特异性结合Nurr1的配体结合域,EC50约为20 μM。 | |||
T12754 |
RORγt Inverse agonist 8
|
ROR | Metabolism |
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist(human RORγt-LBD with an IC50 of 19 nM). | |||
T69982 |
VPC-16606
|
||
VPC-16606 is a potent and selective inhibitor of ERα-dependent cell growth and gene expression. VPC-16606 prevents the interaction between ERα-LBD and SRC-3 fusion proteins in a dose-dependent manner. | |||
T40349 |
DS45500853
|
||
DS45500853, an estrogen-related receptor α (ERRα) agonist, acts as an inhibitor of the binding interaction between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM), exhibiting an IC50 of 0.80 μM. This compound holds potential for research pertaining to metabolic disorders, particularly type 2 diabetes mellitus (T2DM). | |||
T73842 | Leriglitazone hydrochloride | ||
Leriglitazone (Hydroxypioglitazone) hydrochloride,吡格列酮的代谢产物。Leriglitazone (Hydroxypioglitazone) hydrochloride 是PPARγ激动剂,通过稳定PPARγ(AF-2) 共激活剂结合表面和增强共激活剂结合能力,提供高转录效力。 Leriglitazone (Hydroxypioglitazone) hydrochloride 与 PPARγC (LBD) 结合,其Ki 值为 1.2 μM,诱导PPARγ(LBD) 转录效率,EC50为 680 nM。 | |||
T76375 |
Targefrin
|
||
Targefrin 是一种有效的靶向 EphA2的试剂,作为拮抗剂发挥作用。Targefrin 结合 EphA2- LBD 的解离常数为 21 nM,IC50值为10.8 nM。Targefrin 在几种胰腺癌细胞系中诱导细胞受体内化和降解。 | |||
T39916 | GNE-274 | ||
GNE-274, a non-degrader compound structurally similar to GDC-0927 (an ER degrader), serves as a partial ER agonist in breast cancer cell lines without triggering ER turnover. Notably, GNE-274 enhances chromatin accessibility at ER-DNA binding sites, unlike GDC-0927. Acting as a potent inhibitor of the ER-ligand binding domain (LBD), GNE-274 exhibits potential for cancer research purposes. | |||
T60759 |
DS20362725
|
||
DS20362725 是可用于代谢紊乱研究,如二型糖尿病的雌激素相关受体 α (ERRα) 激动剂。DS20362725 抑制受体相互作用蛋白 140 (RIP140) 辅助抑制肽 (10 nM) 和 GST-ERRα 配体结合结构域 (LBD; 1.2 μM) 之间的结合的 IC50值为 0.6 μM。 | |||
T22242 |
Amodiaquine hydrochloride
|
||
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride) 是一种4-氨基喹啉类抗疟剂,是一种有效的口服活性的组胺 N-甲基转移酶 (histamine N-methyltransferase) 抑制剂,Ki 值为 18.6 nM。Amodiaquine dihydrochloride 也是一种Nurr1激动剂,可特异性结合Nurr1的配体结合域,EC50约为20 μM,具有抗炎作用。 | |||
T83894 |
4A7C-301-Nurr1 Agonist
4A7C-301-Nuclear Receptor-Related 1 |
||
4A7C-301-Nurr1激动剂是一种核受体相关1(Nurr1)的激动剂。它通过与Nurr1配体结合域(LBD;IC50 = 48.22 nM)结合,增加了在使用SK-N-BE(2)C人神经母细胞瘤细胞进行的报告基因测定中Nurr1-LBD和全长Nurr1的转录活性(EC50s = 6.53 和 50-70 µM,分别)。每天5 mg/kg的4A7C-301-Nurr1激动剂能减少在经MPTP神经毒素或α-突触核蛋白过表达诱导的帕金森病鼠模型中纹状体和黑质compacta部分多巴胺能细胞的死亡,并减少运动和嗅觉缺陷,而不诱发类似运动障碍的行为。 | |||
T15736 |
Leriglitazone
Hydroxypioglitazone |
Others | Others |
Leriglitazone, a metabolite of pioglitazone, binds to the PPARγ C-terminal ligand-binding domain (Ki: 1.2 μM) and induces transcriptional efficacy of the PPARγ (EC50: 680 nM). Leriglitazone PioOH is a PPARγ agonist, stabilizes the PPARγ activation functio |