JAK-IN-23|西域试剂

JAK-IN-23,98.90%

产品编号：Bellancom-151262| 分子式：C₂₃H₂₂Cl₂N₄O| 分子量：441.35

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货号	价格	库存与货期
Bellancom-151262	￥3000.00	杭州北京（现货）
Bellancom-151262	￥4800.00	杭州北京（现货）
Bellancom-151262	￥9500.00	杭州北京（现货）
Bellancom-151262	￥14500.00	杭州北京（现货）

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JAK-IN-23

产品介绍

JAK-IN-23 是 JAK/STAT 和 NF-κB 的双重抑制剂，具有口服活性。JAK-IN-23 对J AK1/2/3 具有抑制作用，IC₅₀ 值分别为 8.9 nM、15 nM 和 46.2 nM。JAK-IN-23 对干扰素刺激基因 (ISG) 和 NF-κB 通路具有较强的抑制活性，IC₅₀ 值分别为 3.3 nM 和 150.7 nM。JAK-IN-23 具有很强的抗炎作用，可以减少各种促炎因子的释放。JAK-IN-23 可用于炎症性肠病 (IBD) 的研究。

生物活性

JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC₅₀ values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC₅₀ values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).

体外研究

JAK-IN-23 inhibits JAK1/2/3 with IC₅₀ values of 8.9 nM, 15 nM and 46.2 nM, respectively.
JAK-IN-23 shows potent inhibitory activities against ISG and NF-KB with IC₅₀ values of 3.3 nM and 150.7 nM, respectively.
WB--- JAK-IN-23 (0.33μM, 1μM, 3μM; 24 h) can simultaneously block JAK-STAT1/3 and NF-κB proinflammatory signaling pathways in THP1-dual cells.
JAK-IN-23 (0.003-3 μM; 24 h) decreases the release of various proinflammatory factors, including IL-6, IL-8, IL-1β in THP1-dual cells stimulated by LPS.
JAK-IN-23 (0.11-3 μM; 24 h) decreases the release of various proinflammatory factors, including TNF-α, IL-12, IL-10 and IFNγ in LPS-induced peripheral blood mononuclear cells (PBMCs).
JAK-IN-23 (1 μM) inhibits the expression of a variety of inflammation-related genes induced by LPS, including IL-1B, TNF, IL12B, and IL-23A and has inhibitory effects on the expression of genes involved in the unfolded protein response that was induced by LPS (1 μg/mL).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	THP1-Dual Cells
Concentration:	0.33μM, 1μM, 3μM
Incubation Time:	24 h
Result:	Inhibited p-STAT1/3 in a dose-dependent manner that was induced by IL-6, as well as inhibited pNF-κB p65 in a dose-dependent manner, but not on MYD88 and p-IKK α/β that was induced by LPS.

体内研究
(In Vivo)

JAK-IN-23 (1-5 mg/kg, oral) produces a strong anti-inflammatory activity in both dextran sulfate sodium (DSS) - and 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced acute enteritis models and restores the structural composition of gut microbiota.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	DSS-Induced Acute Colitis Mice Model
Dosage:	1 mg/kg, 3 mg/kg
Administration:	oral
Result:	Significantly decreased the DAI scores (1 and 3 mg/kg). Recovered the length of the colon (3 mg/kg). Significantly reduced the histopathology of ulcerative colitis (1 and 3 mg/kg).

Animal Model:	The BALB/c mouse inflammatory bowel disease (IBD) model
Dosage:	1 mg/kg, 5 mg/kg
Administration:	oral
Result:	Significantly improved the survival probability, had low DAI scores and effectively relieved symptoms of colitis in the TNBS-induced IBD mice model (5 mg/kg). Did not improve the survival probability and decreases the DAI score (100 mg/kg).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	DSS-Induced Acute Colitis Mice Model
Dosage:	1 mg/kg, 3 mg/kg
Administration:	oral
Result:	Significantly decreased the DAI scores (1 and 3 mg/kg). Recovered the length of the colon (3 mg/kg). Significantly reduced the histopathology of ulcerative colitis (1 and 3 mg/kg).

Animal Model:	The BALB/c mouse inflammatory bowel disease (IBD) model
Dosage:	1 mg/kg, 5 mg/kg
Administration:	oral
Result:	Significantly improved the survival probability, had low DAI scores and effectively relieved symptoms of colitis in the TNBS-induced IBD mice model (5 mg/kg). Did not improve the survival probability and decreases the DAI score (100 mg/kg).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	DSS-Induced Acute Colitis Mice Model
Dosage:	1 mg/kg, 3 mg/kg
Administration:	oral
Result:	Significantly decreased the DAI scores (1 and 3 mg/kg). Recovered the length of the colon (3 mg/kg). Significantly reduced the histopathology of ulcerative colitis (1 and 3 mg/kg).

Animal Model:	The BALB/c mouse inflammatory bowel disease (IBD) model
Dosage:	1 mg/kg, 5 mg/kg
Administration:	oral
Result:	Significantly improved the survival probability, had low DAI scores and effectively relieved symptoms of colitis in the TNBS-induced IBD mice model (5 mg/kg). Did not improve the survival probability and decreases the DAI score (100 mg/kg).

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (11.33 mM; ultrasonic and warming and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2658 mL	11.3289 mL	22.6578 mL
5 mM	0.4532 mL	2.2658 mL	4.5316 mL
10 mM	0.2266 mL	1.1329 mL	2.2658 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

参考文献