Name: Icotrokinra
Brand: TargetMol
SKU: T89073
Price: 2780 CNY
Availability: InStock
Rating: 5 (10 reviews)

规格

价格

库存

数量

1 mg

¥ 2,780

In stock

10 mg

待询

50 mg

待询

产品介绍

生物活性

产品描述	Icotrokinra is an orally bioavailable and highly selective antagonist of the interleukin-23 receptor (IL-23R), thereby interfering with IL-23-mediated signaling cascades. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 value of 5.6 pM, and it suppresses IL-23-induced interferon-gamma production in natural killer cells with an IC50 value of 18.4 pM. Icotrokinra further demonstrates anti-inflammatory effects in a rat TNBS-induced colitis model, making it a compound of interest in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease.
靶点活性	IL-23:7.1 pM (Kd)
体内活性	在大鼠TNBS诱导的结肠炎模型中，口服Icotrokinra在剂量≥0.3 mg/kg/天时显著减轻体重损失和结肠重量/长度比。在IL-23诱导的皮肤炎症模型中，Icotrokinra在剂量≥10 mg/kg BID时显著抑制IL-17A、-17F和-22基因表达，并减轻皮肤厚度。[1]
别名	伊可白滞素, PN-235, PN235, JNJ-77242113, JNJ77242113, JNJ-2113, JNJ2113

化学信息

分子量	1898.17
分子式	C₉₀H₁₂₀N₂₀O₂₂S₂
CAS No.	2763602-16-8
Smiles	N(C([C@H](CC1=CC2=C(C=C1)C=CC=C2)NC([C@H](CC3=CC=C(OCCN)C=C3)NC(=O)[C@H]4NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](CC=5C=6C(NC5)=C(C)C=CC6)NC(=O)[C@]([C@@H](C)O)(NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(C)=O)C(C)(C)SSC4(C)C)[H])=O)=O)C7(C(N[C@H](C(N[C@H](C(N[C@@H](CC=8C=CC=NC8)C(N(CC(N)=O)C)=O)=O)CC(N)=O)=O)CCC(O)=O)=O)CCOCC7
颜色	White
物理性状	Solid

储存&溶解度

存储

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 80 mg/mL (42.15 mM), Sonication is recommended.

H2O: ≥ 80 mg/mL, Sonication is recommended.

溶液配制表

DMSO

体内实验配液计算器