2. Immunology/Inflammation
  3. FAP
  4. FAPI-X5

FAPI-X5 是一种成纤维细胞活化蛋白 (FAP) 抑制剂。FAPI-X5 可结合 FAP 的催化结构域，与关键活性残基形成氢键并发生 π-π 堆叠，从而实现功能性抑制。FAPI-X5 具有白蛋白结合活性，可延长全身循环半衰期。FAPI-X5 对胶质母细胞瘤细胞产生细胞抑制作用，可减缓肿瘤生长但不会使肿瘤消退。FAPI-X5 经 68Ga 标记后可作为 PET 示踪剂，在荷胶质母细胞瘤小鼠中表现出快速的肿瘤摄取和高对比度成像效果。FAPI-X5 经 177Lu 或 47Sc 标记后可作为靶向放射性核素药物，具有延长的肿瘤滞留性。FAPI-X5 可用于胶质母细胞瘤的研究。

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

FAPI-X5

FAPI-X5 Chemical Structure

CAS No. : 3056070-96-0

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.

FAPI-X5 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FAPI-X5 is a fibroblast activation protein (FAP) inhibitor. FAPI-X5 binds to the FAP catalytic domain, forming hydrogen bonds with key active residues and engaging in π-π stacking to drive functional inhibition. FAPI-X5 exhibits albumin binding activity to prolong systemic circulation half-life. FAPI-X5 induces cytostatic effects on glioblastoma tumors, slowing tumor growth without regression. FAPI-X5, when labeled with 68Ga, acts as a PET tracer with rapid tumor uptake and high-contrast imaging in glioblastoma tumor-bearing mice. FAPI-X5, when labeled with 177Lu or 47Sc, functions as a targeted radionuclide agent with prolonged tumor retention. FAPI-X5 can be used for the research of glioblastoma[1].

体外研究
(In Vitro)

FAPI-X5 (10 μg) 经 68Ga、177Lu 或 47Sc 放射性标记后，放射化学纯度 >95%，白蛋白结合率 >40%，且体外稳定性良好；其中 68Ga-FAPI-X5 的亲水性最强，177Lu-和 47Sc-FAPI-X5 的白蛋白结合率略高[1]。
FAPI-X5 (30-240 min) 经 68Ga、177Lu 或 47Sc 放射性标记后，在表达 FAP 的 U87MG 细胞中呈现时间依赖性的细胞摄取；其中 68Ga-FAPI-X5 在 2 h 时摄取量最高，且所有标记变体均在 4 h 时达到摄取峰值[1]。

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

FAPI-X5 相关抗体:
体内研究
(In Vivo)

FAPI-X5 (177Lu-FAPI-X5 and 47Sc-FAPI-X5) (18.5-55.5 MBq；静脉注射；单剂量) 可在荷 U87MG 胶质母细胞瘤小鼠中产生细胞抑制效应 (T/C 值为 35.49%-57.2%)，但会伴随剂量依赖性的肝胃肠道毒性[1]。

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

Animal Model: U87MG tumor-bearing mice[1]
Dosage: 18.5 MBq, 37 MBq, 55.5 MBq
Administration: I.v.; single dose
Result: Produced cytostatic effects with T/C values of 35.49% ± 3.8% at 18.5 MBq, 46.1% ± 4.7% at 37 MBq, and 57.2% ± 5.3% for 177Lu-FAPI-X5.
Produced cytostatic effects with T/C values of 37.50% ± 2.7% at 18.5 MBq, 36.8% ± 3.2% at 37 MBq, and 42.8% ± 3.6% for 47Sc-FAPI-X5.
Caused dose-dependent body weight loss, with a maximum loss of 11% at the 55.5 MBq 47Sc-FAPI-X5 dose, plateauing by day 10.
Resulted in one death in the 37 MBq 47Sc-FAPI-X5 group and one in the 55.5 MBq 177Lu-FAPI-X5 group.
Induced centrilobular coagulative necrosis of hepatocytes, ulcerative necrosis of intestinal mucosa, and mild inflammatory cell infiltration in cardiac and renal tissues.
分子量

1428.37

Formula

C63H88F2IN15O13
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

FAPI-X5 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:

FAPI-X53056070-96-0FAPFibroblast activation proteinhuman FAP protein 1Z68FAP catalytic domainhepatocyte necrosisPET tracertargeted radionuclide agentfibroblast activation protein (FAP)miceU87MG cellsglioblastoma tumorsintestinal mucosal ulcerationInhibitorinhibitorinhibit

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：
FAPI-X5
目录号：
HY-181494
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