ROR
The nuclear receptors (NRs) are a large family of ligand-regulated transcriptional factors and include the receptors for steroid hormones, thyroid hormones, lipophilic vitamins, and cholesterol metabolites. Retinoic acid receptor-related orphan receptor (ROR) α, β and γ belong to the NR superfamily, the ROR subfamily of transcription factors consists of RORα (NR1F1), RORβ (NR1F2) and RORγ (NR1F3) and has been identified in several mammalian species that exhibit tissue-specific expression of these transcription factors. RORα is widely expressed in liver, skeletal muscle, skin, lung, adipose tissue, kidney, thymus, and brain. RORβ exhibits a more restricted neuronal-specific expression pattern in the brain, retina, and pineal gland. RORγ is highly expressed in thymus (the thymus-specific isoform is referred to as RORγt), muscle, testis, pancreas, prostate, heart, and liver.
References
1.Zhang Y, et al. Acta Pharmacol Sin. 2015;36(1):71–87.
References
1.Zhang Y, et al. Acta Pharmacol Sin. 2015;36(1):71–87.
Nuclear Receptor/Transcription Factor
ROR
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ML 209
产品货号 : M34963
cas no: 1334526-14-5
(±)-ML 209 (compound 4n) 是一种二苯基丙酰胺,一种视黄酸相关的孤儿受体 RORγ 拮抗剂,IC50 为 1.1 μM。(±)-ML 209 在 HEK293t 细胞中抑制 RORγt 转录活性,IC50 为 300 nM。(±)-ML 209 抑制细胞中 RORγt 的转录活性,但不抑制 RORα。(±)-ML 209 选择性抑制鼠 Th17 细胞分化,而不影响幼稚 CD4+ T 细胞分化为Th1 和调节性 T 细胞。 -
XY018
产品货号 : M33993
cas no: 1873358-87-2
XY018 是一种有效的 ROR-γ 选择性拮抗剂。XY018 作用于 293T 细胞,抑制 ROR-γ 活性,EC50 为 190 nM。XY018 与 ROR-γ 疏水配体结合域 (LBD) 结合 。 -
SR2211
产品货号 : M33503
cas no: 1359164-11-6
SR2211 是 RORγ 有效的,选择性合成调节剂,可作为逆向激动剂发挥功能,其 Ki 值为 105 nM,IC50 值为 ~320 nM。 -
Cedirogant
产品货号 : M28818
cas no: 2055496-11-0
Cedirogant 是一种口服活性视黄醇相关孤儿受体-γt(RORγt) 反向激动剂,用于银屑病研究。 -
RORγt inverse agonist 13
产品货号 : M28809
cas no: 2170477-75-3
RORγt 反向激动剂 13 (Compound 3i) 是一种有效的、口服活性的、选择性的 RORγt 反向激动剂 (IC50=63.8 nM),具有改善的化合物样特性。