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.

ROR agonist-1 is a potent and orally bioavailable the retinoic acid receptor-related orphan receptor C2 (RORC2) inverse agonist(inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5).

RORγ inverse agonist 1具有抗炎活性，可用来治疗风湿和银屑病。

RORγt agonist 1 is a potent, orally bioavailable agonist of RORγt(EC50 of 20.8 nM).

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。

SR 1903是一种RORγ、PPARγ 反向激动剂（对 RORγ、PPARγ 的 IC50 分别为 100 nM、209 nM），同时也是LXR 激动剂（EC50 为 154 nM）。在胶原诱导性关节炎及饮食诱导性肥胖小鼠模型中，SR-1903 可发挥抗炎、抗糖尿病作用 。

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。

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 human na ve CD4+ T cells when used at a concentration of 300 nM. 7β,27-dihydroxy Cholesterol (60 mg/kg) increases IL-17A production in isolated mouse γδ T cells stimulated with 12-myristate 13-acetate and ionomycin .

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。

SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-1903 reduces the severity of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.

SR1555 hydrochloride为SR1555的盐酸盐形式,作为视黄酸受体相关孤儿核受体γ (RORγ) 的反向激动剂,其IC50值为1 μM.该化合物能够抑制促炎性TH17细胞的发展与功能,同时提升抗炎性T调节 (Treg) 细胞的频率,因而用于自身免疫性疾病的研究.