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Deucravacitinib(BMS-986165)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Deucravacitinib(BMS-986165)图片
CAS NO:1609392-27-9
包装:1mg, 5mg, 10mg, 25mg, 50mg
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品名称
BMS986165
产品介绍

生物活性

Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain with IC50 of 1.0 nM and Ki value of 0.02 nM. Deucravacitinib (BMS-986165) inhibited IL-23, IL-12, and Type I interferon-driven cellular signaling and transcriptional responses (IC50 range 2-14 nM).

Deucravacitinib (BMS-986165) treatment in NZB/W lupus-prone mice rapidly (24 hours) reduced the elevated expression of Type I interferon-dependent genes and dose-dependently protected from nephritis and other disease endpoints with chronic dosing, with efficacy correlating with inhibition of Type I interferon-dependent gene expression. Deucravacitinib (BMS-986165) was also highly efficacious in the anti-CD40-induced colitis model in SCID mice, providing protection against both weight loss (wasting) and histologically evident colitis, and was as effective as an anti-p40 antibody.


化学数据

分子量425.46
分子式C20H19D3N8O3
CAS号1609392-27-9
纯度>99.5%
溶解性(25°C)DMSO ≥ 30 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系CD3+ T-cells, CD161+ CD3+ T-cells, TF-1 cells, mononuclear cells, platelets
方法Deucravacitinib (BMS-986165) is evaluated in both binding and human cellular assays to determine selectivity within the JAK family and across the kinome. Mean values are determined from at least three separate experiments unless otherwise noted. Measuring STAT5 phosphorylation in CD3+ T-cells as end point. Measuring STAT3 phosphorylation in CD161+ CD3+ T-cells. Measuring STAT5A phosphorylation in TF-1 cells (n = 2). Measuring STAT6 phosphorylation in mononuclear cells (n = 2). Measuring STAT5 phosphorylation in platelets. Measuring STAT3 phosphorylation in CD3+ T-cells.
浓度0-10 μM
处理时间-

动物实验
动物模型6–8 weeks old C57BL/6 female mice
配制-
剂量7.5 mg/kg, 15 mg/kg, and 30 mg/kg
给药处理oral gavage

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM2.3504 mL11.752 mL23.504 mL
5 mM0.4701 mL2.3504 mL4.7008 mL
10 mM0.235 mL1.1752 mL2.3504 mL