Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T67943 |
RORγ inverse agonist 1
|
||
RORγ inverse agonist 1具有抗炎活性,可用来治疗风湿和银屑病。 | |||
T39797 |
RORγ agonist 1
|
||
RORγ agonist 1 is a highly potent and orally bioavailable compound that activates the RORγ receptor. Its efficacy is demonstrated by an EC50 value of 21 nM and it exhibits antitumor activity. | |||
T79464 |
RORγ antagonist 1
|
ROR | Metabolism |
RORγ antagonist1 (化合物22) 作为RORγ的有效拮抗剂 (KD=0.18 μM),在HPAF-II胰腺癌异种移植模型中显示出了抗增殖性能。该化合物通过抑制RAS/MAPK和AKT/mTORC1通路,并引发caspase依赖的细胞凋亡(apoptosis)机制,从而在胰腺癌细胞中发挥作用。 | |||
T9623 |
RORγt inverse agonist 13
|
ROR | Metabolism |
RORγt inverse agonist 13 是一种口服有效的RORγt 选择性反向激动剂,IC50为 63.8 nM。 | |||
T12753 |
RORγt Inverse agonist 6
|
ROR | Metabolism |
RORγt Inverse agonist 6 是 RORγt inverse 的激动剂。 RORγt Inverse agonist 6 可用于研究 Th17 驱动的自身免疫性疾病。 | |||
T4050 |
GSK2981278
ROR gama modulator 1 |
ROR | Metabolism |
GSK2981278 (ROR gama modulator 1) 是 RORγ的选择性反向激动剂。它能够抑制 il17启动子的激活,并且干扰 RORγ-DNA 结合。 | |||
T6690 |
T0901317
N-(2,2,2-三氟乙基)-N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]苯磺酰胺 |
Apoptosis; FXR; Liver X Receptor; ROR | Apoptosis; Metabolism |
T0901317 是一种口服有效且高度选择性的LXR 激动剂,对 LXRα 的EC50为 20 nM。它激活FXR,EC50为 5 μM。它是RORα和RORγ双重反向激动剂,Ki 值分别为 132 nM 和 51 nM。它诱导细胞凋亡,并抑制低密度脂蛋白受体缺失小鼠动脉粥样硬化的发展。 | |||
T39038 | RORγt inhibitor 1 | ||
RORγt inhibitor 1 is a RORγt allosteric inhibitor with an IC 50 value of 1 nM. | |||
T39720 |
RORγt inverse agonist 23
|
||
RORγt inverse agonist 23, an orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist, is a potent and selective RORγt inverse agonist. | |||
T40043 |
RORγt Inverse agonist 10
|
||
RORγt Inverse agonist 10 is a highly potent and orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R. | |||
T64017 |
RORγt agonist 3
|
||
RORγt agonist 3 是 RORγt 的有效激动剂。RORγt agonist 3 能够促使 Th17 细胞分化,增加促炎细胞因子水平,进而提高淋巴细胞的细胞毒性。RORγt agonist 3 能够阻碍调节性 T 细胞的产生,并免疫反应产生抑制作用。 | |||
T64140 |
RORγt agonist 2
|
||
RORγt agonist 2 是 RORγt 的有效的激动剂。RORγt agonist 2 能够诱导 Th17 细胞分化,增加促炎细胞因子水平,进而增强淋巴细胞的细胞毒性。RORγt agonist 2 对调节性 T 细胞的产生表现出抑制作用,能够抑制免疫反应。 | |||
T72596 |
RORγt modulator 5
|
||
RORγt modulator 5 是一种 RORγt 调节剂,Ki 值 <100 nM。RORγt modulator 5 可用于研究 RORy 介导的炎症、代谢、自身免疫和其他疾病。 | |||
T63124 | RORγt modulator 4 | ||
RORγt modulator 4 是一种 RORγt 调节剂。RORγt modulator 4 能够调节源自小鼠脾脏的细胞中 IL-17A 产生的活性。 | |||
T63678 |
RORγt modulator 2
|
||
RORγt modulator 2 是一种类视黄醇相关孤儿受体 γt (RORyt) 的调节剂 (IC50<50 nM),能够用于 RORγt 介导的疾病的研究,如疼痛、炎症、哮喘、类风湿性关节炎、COPD、多发性硬化、银屑病、结肠炎、神经退行性疾病和癌症。 | |||
T63874 | RORγt inverse agonist 28 | ||
RORγt inverse agonist 28 是有效的 RORγt 反向激动剂。RORγt inverse agonist 28 能够调节 Th17 细胞的分化,并抑制 IL-17 的产生。RORγt inverse agonist 28 对炎症和自身免疫性疾病表现出研究潜力。 | |||
T64145 | RORγt/DHODH-IN-1 | ||
RORγt/DHODH-IN-1 (compound (R)-14d) 是一种有效的、口服具有活力 RORγt (IC50: 0.083 μM) 和 DHODH (IC50: 0.172 μM) 的双重抑制剂。RORγt/DHODH-IN-1 具有明显的体内抗炎作用。 | |||
T64146 | RORγt/DHODH-IN-3 | ||
RORγt/DHODH-IN-3 (compound (S)-14d) 是一种有效的、口服具有活力 RORγt (IC50: 0.098 μM) 和 DHODH (IC50: 0.432 μM) 的双重抑制剂。RORγt/DHODH-IN-1 具有明显的体内抗炎作用。 | |||
T79470 |
RORγt inverse agonist 31
|
ROR | Metabolism |
RORγt inverse agonist 31 (14g) 为一有效RORγt反向激动剂,具备0.428 μM的IC50值。该化合物能够缓解Imiquimod诱发的小鼠牛皮癣症状。 | |||
T62564 |
RORγt inverse agonist 30
|
||
RORγt inverse agonist 30 (Compound 1) 是一种有效的 RORγt 反向激动剂 (IC50: 46 nM)。靶向核受体 RORγt 能够有效治疗自身免疫性疾病。 | |||
T62956 | RORγt inverse agonist 29 | ||
RORγt inverse agonist 29 是一种有效的、选择性的、口服具有活力的 RORγt 反向激动剂,其 IC50 值为 21 nM。RORγt inverse agonist 29 能够用于皮肤炎症和银屑病等自身免疫性疾病的研究。 | |||
T63609 | RORγt modulator 3 | ||
RORγt modulator 3 是一种类视黄醇相关孤儿受体 γt (RORγt) 的调节剂,能够用于研究 RORγt 介导的疾病,如疼痛、COPD、炎症、哮喘、结肠炎、多发性硬化、类风湿性关节炎、银屑病、神经退行性疾病和癌症。 | |||
T72595 |
RORγt inhibitor 2
|
||
RORγt inhibitor 2 是一种有效的RORγt 抑制剂,IC50为 9.2 nM。RORγt inhibitor 2可用于研究由RORγt 介导的癌症、炎症或自身免疫性疾病。 | |||
T62462 | RORγt/DHODH-IN-2 | ||
RORγt/DHODH-IN-2 (compound 1) 是一种有效的 RORγt/DHODH 双重抑制剂,能够用于研究炎症性肠病 (IBD)。 | |||
T72254 |
RORγt inverse agonist 26
|
||
RORγt inverse agonist 26 是一种有效的 RORγt 反向激动剂。RORγt inverse agonist 26 调节 Th17 细胞的分化并抑制 IL-17的产生。RORγt inverse agonist 26 具有研究炎症和自身免疫性疾病的潜力。 | |||
T72252 | RORγt inverse agonist 14 | ROR | Metabolism |
RORγt inverse agonist 14 (8e) 是一种高效、口服活性及选择性 RORγt 反向激动剂(EC50 为 2.5 nM),具有抗炎作用,主要应用于风湿性关节炎和牛皮癣的研究。 | |||
T12752 |
RORγt Inverse agonist 3
|
Others | Others |
RORγt Inverse agonist 3 is a potent, selective and orally active inverse agonist of RORγ(EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively). | |||
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). | |||
T12755 |
RORγt Inverse agonist 2
|
Others | Others |
RORγt Inverse agonist 2 is a selective, orally active inverse agonist of RORγt(EC50 of 119 nM). | |||
T12751 | RORγt agonist 1 | Others | Others |
RORγt agonist 1 is a potent, orally bioavailable agonist of RORγt(EC50 of 20.8 nM). | |||
T16929 |
SR2211
|
ROR | Metabolism |
SR2211 是一种特异性调节剂和 RORγ 的反向激动剂(IC50 = 320 nM,Ki = 105 nM)。 | |||
T13362 |
XY101
|
ROR | Metabolism |
XY101 是一种有效选择性的、代谢稳定的口服 RORγ 反向激动剂,IC50 为 30 nM,Kd 为 380 nM。 | |||
T14369 |
AZD-0284
|
ROR | Metabolism |
AZD-0284 是核受体 (RORγ) 的选择性反向激动剂。它对呼吸道疾病及斑块型寻常型银屑病具有潜在的应用价值。 | |||
TQ0007 |
Cintirorgon
LYC-55716 |
ROR | Metabolism |
Cintirorgon (LYC-55716) 是一种首创的、口服有活力的的RORγ选择性激动剂。它通过调节 RORγ 表达的 T 淋巴免疫细胞的基因表达,提高效应子功能,降低免疫抑制,抑制肿瘤生长,提高生存率。 | |||
T5163 |
SR1001
|
ROR | Metabolism |
SR1001 是选择性RORα及RORγt 的反向激动剂,其Ki 分别为 172 和 111 nM。 | |||
T4594 |
SR1078
SR 1078 |
ROR | Metabolism |
SR1078 是视黄酸受体相关孤儿受体 (RORα/RORγ) 激动剂。它能够与 RORα 和 RORγ 的配体结合区直接结合,增强该受体的转录活性,促使 RORα/γ 靶基因的转录。 | |||
T37587 |
ML 209
|
ROR | Metabolism |
ML-209 是一种视黄酸相关的孤儿受体 RORγ 拮抗剂 (IC50= 1.1 μM)。ML-209 抑制 HEK293t 细胞中 RORγt 转录活性(IC50= 300 nM)。ML-209 不抑制细胞中 RORα。ML-209 对鼠 Th17 细胞分化具有选择性抑制,而不影响幼稚 CD4+ T 细胞分化为 Th1 和调节性 T 细胞。 | |||
T16787 |
Vimirogant
VTP-43742 |
ROR | Metabolism |
Vimirogant is a RORγ inhibitor (Ki: <100 nM). | |||
T15404 | GNE-6468 | Others | Others |
GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell). | |||
T35321 |
Zymostenol
delta(8)-Cholestenol,5a-Cholest-8-en-3b-ol,Δ8-Cholesterol |
Endogenous Metabolite; ROR | Metabolism |
Zymostenol (5a-Cholest-8-en-3b-ol) 是一种 RORγ 激动剂 ,EC50为1 μM。Zymostenol 是胆固醇生物合成的后期前体。 | |||
T24213 |
XY018
XY 018,XY-018 |
||
XY 018 is a RORγ antagonist. It also suppresses androgen receptor expression in prostate cancer cell lines and inhibits the growth of tumors in androgen receptor-positive xenograft models. | |||
T25109 |
ARN-6039
ARN 6039,ARN6039 |
||
ARN-6039 is an orally available inverse agonist of RORγ for Autoimmune Neuroinflammatory Demyelinating Disease. The activity of ARN-6039 against RORγ was demonstrated in a RORγ-activated IL-17A Prom/LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 r | |||
T23794 |
BIO592
BIO-592,BIO 592 |
||
BIO592 is a modulator of RORγt. BIO592 triggers inverse agonism of RORγ. | |||
T15398 |
GNE-0946
|
Others | Others |
GNE-0946 is a potent and selective agonist of RORγ (EC50: 4 nM for HEK-293 cell). | |||
T69695 | Izumerogant | ||
Izumerogant is an inverse agonist of the retinoid-related orphan receptor-gamma (RORγ). | |||
T39960 |
SHR168442
SHR168442 |
||
SHR168442 is a potent RORγ modulator, exhibiting an IC50 value of 0.035 μM. | |||
T5164 |
Cabozantinib hydrochloride
XL184,Cabozantinib hydrochloride (849217-68-1(free base)),BMS-907351,盐酸卡博替尼 |
VEGFR; FLT; c-Met/HGFR; TAM Receptor; c-Kit; ROR | Angiogenesis; Metabolism; Tyrosine Kinase/Adaptors |
Cabozantinib hydrochloride (XL184) 是一种有效的泛酪氨酸激酶抑制剂,可抑制 VEGFR2、c-Met、Kit、Axl 和 Flt4(IC50:0.035、1.3、4.6、7 和 6 nM)。 | |||
T70398 |
JTE-151
|
||
JTE-151 is a novel RORγ inverse agonist. | |||
T36998 |
7β,27-dihydroxy Cholesterol
7β,27-DHC,7β,27-dihydroxy Cholesterol |
||
7β,27-dihydroxy Cholesterol is an oxysterol and agonist of retinoic acid receptor-related orphan receptor γ (RORγ) and RORγt. [1] It activates RORγ- or RORγt-dependent signaling with EC50 values of 691 and 1,045 nM, respectively, in reporter assays using HEK293T cells expressing the recombinant human receptors. 7β,27-dihydroxy Cholesterol is selective for RORγ and RORγt over a panel of eight additional nuclear receptors at 30 µM. It increases IL-17A production in Th17-polarized isolated hum... | |||
T25216 |
CD12681
CD 12681,CD-12681 |
||
CD12681 is an effective RORγ inverse agonist, preclinical Candidate for the topical therapy of psoriasis. |