RORγt inverse agonist 34

CAS: 2247604-77-7 F: C31H37N3O3S W: 531.71

RORγt inverse agonist 34 (compound 5a) is a RORγt inverse agonist with an IC50 of 0.094 μM for RORγt-LBD. RORγt inv

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Bioactivity	RORγt inverse agonist 34 (compound 5a) is a RORγt inverse agonist with an IC50 of 0.094 μM for RORγt-LBD. RORγt inverse agonist 34 is used for psoriasis research[1].
Invitro	RORγt inverse agonist 34 影响 RORγt-LBD 对 SRC1 共激活肽的募集，IC50 为 0.094 μM[1]。RORγt inverse agonist 34 有效抑制 Th17 细胞分化的 IC50 为 1.57 μM[1]。RORγt inverse agonist 34 (1 μM, 1 h) 在小鼠肝微粒体中的半衰期为 18 min[1]。RORγt inverse agonist 34 抑制 hERG 的 IC50 超过 40 μM, 表明对心脏毒性低[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> RORγt inverse agonist 34 相关抗体:
In Vivo	RORγt inverse agonist 34 (100 mg/kg, i.p., daily, 7days) 在改善 Imiquimod (HY-B0180) 诱导的银屑病病变方面表现出显著效果[1]。RORγt inverse agonist 34 (0.25%-4% ointment, daily, 11 days) 在 Imiquimod (HY-B0180) 诱导的银屑病小鼠模型中表现出抗银屑病效果[1]。RORγt inverse agonist 34 (4% ointment, transdermal administration, 用量约50 g) 在 BALB/c 小鼠中，约 10min 在血浆中达到峰值，浓度为 0.075 μg/mL[1]。RORγt inverse agonist 34 (10%-20% mg/kg ointment, daily, 12days) 在 BALB/c 鼠中无明显的急性毒性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	2247604-77-7
Formula	C31H37N3O3S
Molar Mass	531.71
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Lv L, Chen B, et.al. Discovery of Novel N-Sulfonamide-tetrahydroquinolines as Potent Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists for the Treatment of Psoriasis. J Med Chem. 2024 Dec 12;67(23):21400-21420.