2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. c-Fms Akt PERK Aminotransferases (Transaminases) Apoptosis TNF Receptor Interleukin Related
  4. CSF1R-IN-27

CSF1R-IN-27 是一种具有口服活性的 CSF1R 抑制剂，IC50 为 19 nM。CSF1R-IN-27 可抑制巨噬细胞中 M-CSF 诱导的 CSF1R、AKT 和 ERK 磷酸化，并阻断肝脏中的 p-CSF1R/p-AKT/p-ERK 信号通路。\nCSF1R-IN-27 在小鼠急性肝损伤模型中发挥保肝作用，可降低血清转氨酶 (transaminase) 水平、减轻炎症细胞浸润、减少凋亡 (apoptosis) 肝细胞数量，并降低循环中 TNF-α 和 IL-6 的水平。CSF1R-IN-27 可用于急性肝损伤的研究。

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

CSF1R-IN-27

CSF1R-IN-27 Chemical Structure

CAS No. : 3034296-91-5

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

CSF1R-IN-27 相关抗体

Top Publications Citing Use of Products

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

查看 Aminotransferases (Transaminases) 亚型特异性产品:

查看所有亚型
GPT/ALT GOT/AST

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CSF1R-IN-27 is a CSF1R inhibitor with oral effectiveness, kinome-wide selective profile, low cellular cytotoxicity, and CSF1R IC50 values of 19 nM, 88 nM, 173 nM, 797 nM, 1448 nM, and >3000 nM.CSF1R-IN-27 suppresses M-CSF-induced phosphorylation of CSF1R, AKT, and ERK in macrophages, and inhibits hepatic p-CSF1R/p-AKT/p-ERK signaling.CSF1R-IN-27 reduces serum transaminase levels, improves hepatic histopathology, alleviates inflammatory cell infiltration, and decreases circulating TNF-α and IL-6 levels.CSF1R-IN-27 can be used for the research of acute liver injury[1].

IC50 & Target[1]

IL-6

 

TNF-α

 

体外研究
(In Vitro)

CSF1R-IN-27 (C52) (72 h) 可强效抑制 BaF3-ETV6-CSF1R 细胞的增殖，其 IC50 为 0.298 μM[1]。
CSF1R-IN-27 (72 h) 在 H9C2、HUVEC 和 HepG2 细胞中细胞毒性较低，在 HEK293 和 LX-2 细胞中具有中等细胞毒性，各受试细胞系的 CC50 值范围为 15.25 μM 至>40 μM[1]。
CSF1R-IN-27 (16-2000 nM; 4 h pretreatment, 30 min M-CSF stimulation) 可浓度依赖性地抑制 M-CSF 诱导的 RAW264.7 细胞和骨髓来源巨噬细胞 (BMDMs) 中 CSF1R、AKT 及 ERK 的磷酸化[1]。
CSF1R-IN-27 (24 h) 在 RAW264.7 细胞中的细胞毒性低于 PLX3397，暴露 24 h 后的 CC50 为 34.70 μM[1]。

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

CSF1R-IN-27 相关抗体:

Western Blot Analysis[1]

Cell Line: RAW264.7, bone marrow-derived macrophages (BMDMs)
Concentration: 0, 16, 80, 400, 2000 nM
Incubation Time: 4 h (pretreatment); 30 min (M-CSF stimulation)
Result: Induced concentration-dependent suppression of M-CSF-induced phosphorylation of CSF1R, AKT, and ERK in both RAW264.7 cells and BMDMs.
At concentrations ≥400 nM, substantially attenuated p-CSF1R, p-AKT, and p-ERK levels, with inhibitory effects approaching those of PLX3397 at 400 nM.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 Vz CL AUC0-t Bioavailability
Mice[1] 10 mg/kg p.o. 1612 μg/L 0.08 h 3.99 h 43.56 L/kg 7.91 L/h/kg 1312 h·μg/L 37 %
Mice[1] 10 mg/kg i.v. 7943 μg/L 0.08 h 4.55 h 19.92 L/kg 2.94 L/h/kg 3499 h·μg/L /
Mice[1] 10 mg/kg i.p. 3613 μg/L 0.21 h 4.45 h 17.45 L/kg 2.91 L/h/kg 3515 h·μg/L /
体内研究
(In Vivo)

CSF1R-IN-27 (10-20 mg/kg；口服；单次给药) 可剂量依赖性地对雄性 C57BL/6 小鼠中 Acetaminophen (HY-66005) 诱导的急性肝损伤发挥保肝作用，其中 20 mg/kg 口服剂量在降低血清转氨酶、炎性细胞因子水平、肝坏死程度、巨噬细胞浸润、细胞凋亡及 CSF1R 通路激活方面的效果优于 10 mg/kg 剂量[1]。

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

Animal Model: C57BL/6 (male, 8 weeks old, 20−25 g, acetaminophen-induced acute liver injury)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: p.o.; single dose
Result: Dose-dependently reduced serum ALT and AST levels compared to the acetaminophen-only model group.
Reduced serum TNF-α and IL-6 levels, with the 20 mg/kg dose showing a more pronounced effect.
Dose-dependently reduced the necrotic area in liver tissue, with the 20 mg/kg dose yielding a greater reduction than the 10 mg/kg dose.
Dose-dependently suppressed hepatic infiltration of CD11b+ and F4/80+ inflammatory macrophages, and reduced the number of TUNEL-positive apoptotic hepatocytes.
Dose-dependently decreased hepatic levels of p-CSF1R, p-AKT, and p-ERK.
分子量

557.57

Formula

C27H30F3N7O3
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

CSF1R-IN-27 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:

CSF1R-IN-273034296-91-5c-FmsAktPERKAminotransferases (Transaminases)ApoptosisTNF ReceptorInterleukin RelatedCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RPKBProtein kinase BProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseAminotransferases (Transaminases) Tumor Necrosis Factor ReceptorTNFRILERKH9C2BMDMsBaF3-ETV6-CSF1R cellsmacrophagesHepG2AKTHUVECRAW264.7 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：
CSF1R-IN-27
目录号：
HY-183569
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