货号	规格	价格	上海	北京	珠海	重庆	武汉
S89375-5mg促销	99.20%	￥1100.00 ￥880.00 S89375-5mg ￥880.00 现货	4 4	-	-	-	-
S89375-10mg促销	99.20%	￥1820.00 ￥1450.00 S89375-10mg ￥1450.00 现货	3 3	-	-	-	-
S89375-25mg促销	99.20%	￥2930.00 ￥2340.00 S89375-25mg ￥2340.00 现货	4 4	-	-	-	-
S89375-100mg促销	≥98%	￥5830.00 ￥4660.00 S89375-100mg ￥4660.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved agent-like properties, with an IC50 of 63.8 nM

靶点：

ROR-γ:63.8 nM (IC50);ROR

体外研究：

RORγt inverse agonist 13 (Compound 3i) exhibits activity with an inhibition of 76% at 0.3 µM in Th17 cell differentiation assay.

体内研究：

RORγt inverse agonist 13 (Compound 3i, 25 mg/kg, Orally, twice daily) demonstrats excellent in vivo PK profile in mice and good in vivo efficacy in an IMQ-induced psoriasis mice model. Animal Model: Imiquimod (IMQ)-induced psoriasis mice model. Dosage: 25 mg/kg. Administration: Orally, twice daily. Result: Brought in a significant reduction in clinical severity of psoriasis as measured through the ear erythema, back skin erythema and scaliness scales. Animal Model: Male CD-1 Mice. Dosage: 1 mg/kg (i.v.) and 5 mg/kg (p.o.)(Pharmacokinetic Analysis). Administration: IV or PO, single dose. Result: Cmax: 609.67 ng/mL (PO), 1550 ng/mL (IV).T1/2: 3.63 h (PO), 3.04 h (IV).

参考文献：

1. Nannan Sun, et al. Discovery of carboxyl-containing biaryl ureas as potent RORγt inverse agonists. Eur J Med Chem. 2020 Jul 5;202:112536.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.948 ml	9.741 ml	19.482 ml
5 mM	0.39 ml	1.948 ml	3.896 ml
10 mM	0.195 ml	0.974 ml	1.948 ml
50 mM	0.039 ml	0.195 ml	0.39 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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