2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  3. JAK
  4. RAI-20

RAI-20 (H018) 是一种口服有效的 JAK1/JAK2 双重抑制剂 (IC50=15.1 和 22.7 nM)。RAI-20 具备优异的药代动力学特性，包括血浆稳定性、全身暴露量以及较长的半衰期。在胶原诱导性关节炎大鼠模型中，RAI-20 展现出显著的抗炎和抗关节炎活性，有效降低了足爪肿胀体积和关节炎指数。RAI-20 可用于类风湿关节炎发病机制的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

RAI-20

RAI-20 Chemical Structure

CAS No. : 2549180-90-5

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

RAI-20 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

查看所有亚型
JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RAI-20 (H018) is an orally active JAK1/JAK2 dual inhibitor (IC50=15.1 and 22.7 nM). RAI-20 exhibits excellent pharmacokinetic properties, including plasma stability, systemic exposure, and a long half-life. In a collagen-induced arthritis rat model, RAI-20 shows significant anti-inflammatory and anti-arthritic activities, effectively reducing paw swelling volume and arthritis index. RAI-20 can be used for research on the pathogenesis of rheumatoid arthritis[1].
IC50 & Target

JAK2

22.7 nM (IC50)

JAK1

15.1 nM (IC50)

体外研究
(In Vitro)

RAI-20 抑制 Ba/F3 细胞增殖，IC50 为 1.21 μM[1]。
RAI-20 抑制人全血细胞中 IL-6 诱导的 pSTAT1 表达，IC50 为 1.45 μM[1]。
RAI-20 具有优良的体外药代动力学特性，包括人血浆稳定性强、肝微粒体代谢中等、血浆蛋白结合率高、无显著 CYP 抑制作用，以及 IC50 为 11.5 μM 的 hERG 抑制活性[1]。

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

RAI-20 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Ba/F3 cell
Concentration: 3x serial dilutions
Incubation Time: under standard cell culture conditions
Result: Inhibited Ba/F3 cell proliferation with an IC50 of 1.21 μM.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC AUC0-∞
Rat[1] 5 mg/kg p.o. 3.06 h 0.92 h 527.64 ng/mL / 3432.96 ng·h/mL
Rat[1] 10 mg/kg p.o. 7.4 h 1.0 h 2402.5 ng/mL 10941.5 ng·h/mL /
体内研究
(In Vivo)

RAI-20 (2-10 mg/kg；灌胃；每日给药；连续 14 天 ) 可在胶原诱导性关节炎的 Lewis 大鼠中诱导产生强效、剂量依赖性的抗关节炎活性，其中每日灌胃 10 mg/kg 的剂量对大鼠后爪体积和关节炎指数的降低作用最为显著[1]。

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

Animal Model: Lewis rats (immunized with type II collagen intradermally at the base of the tail on day 0, followed by a booster immunization on day 7)[1]
Dosage: 2 mg/kg; 3 mg/kg; 5 mg/kg; 10 mg/kg
Administration: p.o.; daily; 14 days
Result: Exhibited dose-dependent reductions in arthritis index, with scores of 8.63, 9.25, 8.00, and 7.25 for the 2 mg/kg, 3 mg/kg, 5 mg/kg, and 10 mg/kg doses, respectively.
Showed lower hind paw volume (3.826 ± 0.075 cm3 at day 28) and arthritis index at every time point from day 17 to day 28 in the 10 mg/kg group compared to other control drugs.
Demonstrated a trend of body weight recovery in all dose groups during days 24-28.
分子量

448.53

Formula

C20H21FN4O3S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

RAI-20 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RAI-202549180-90-5H018RAI20RAI 20H 018H-018JAKJanus kinaseLewis ratspSTAT1TYK2rheumatoid arthritiscollagen-induced arthritis rat modelsJAK3JAK1human whole blood cellsJAK2Ba/F3 cellsInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
RAI-20
目录号：
HY-181929
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z