2. Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. TREM receptor Syk
  4. As48

As48 是一种选择性 TREM2 激动剂，在 TRIC 结合试验中的 KD 值为 12.48 μM。As48 结合于 TREM2 切割区域附近，与 Gly68 形成氢键，降低 58-102 区域的构象灵活性，限制蛋白酶对切割位点的可及性。As48 可激活 SYK 磷酸化，增强小胶质细胞的吞噬功能，并在表达 TREM2 的细胞中诱导下游钙信号通路。As48 可抑制 TREM2 胞外域的脱落，且不影响 ADAM10/17 的蛋白酶活性。As48 可用于阿尔茨海默病的研究。

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

As48

As48 Chemical Structure

CAS No. : 1214405-38-5

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 价格 是否有货 数量
5 mg ￥6100
2 - 4 周
10 mg 询价 2 - 4 周
25 mg 询价 2 - 4 周
50 mg 询价 2 - 4 周
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

As48 相关抗体

Top Publications Citing Use of Products

查看 TREM receptor 亚型特异性产品:

查看所有亚型
TREM-1 TREM-2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

As48 is a selective TREM2 agonist with a KD value of 12.48 μM in TRIC binding assay. As48 binds near the TREM2 cleavage region, forms hydrogen bonds with Gly68, reduces conformational flexibility in regions 58-102, restricts protease accessibility to the cleavage site. As48 activates SYK phosphorylation, enhances microglial phagocytosis, and induces downstream calcium signaling in TREM2-expressing cells. As48 inhibits TREM2 ectodomain shedding without affecting ADAM10/17 protease activities. As48 can be used for the research of Alzheimer's disease[1].

IC50 & Target[1]

TREM-2

12.48 μM (Kd)

体外研究
(In Vitro)

As48 (0.1-1000 μM; 10 min) 可通过 TRIC 结合试验直接结合重组人 TREM2 蛋白，其 KD 值为 12.48 μM[1]。
As48 (0.01-100 μM; 10 min) 以 13.8 μM 的 KD 值结合重组人 TREM2，而与重组人 TREM1 的结合亲和力弱 7 倍 (KD = 97.92 μM)，上述结果由 MST 结合实验测得[1]。
As48 (30 μM; 20 min) 可通过热位移分析使重组人 TREM2 蛋白的热稳定性提升+3.86℃[1]。
As48 (1.23-100 μM) 通过 SPR 结合实验检测，可直接与生物素化重组人 TREM2 蛋白结合，其 KD 值为 29.5 μM[1]。
As48 (0-300 μM; 过夜) 在 HMC3 人小胶质细胞中仅表现出极低的细胞毒性；经 MTS 实验检测在浓度高达 100 μM 时，细胞活力未出现显著下降[1]。
As48 (5-100 μM; 5-60 min) 可通过诱导呈剂量和时间依赖性的 SYK 磷酸化，激活 HEK293-hTREM2/DAP12 细胞中的 TREM2 信号通路[1]。
As48 (0.3-30 μM; 10 min) 可在 HEK293-hTREM2/DAP12 细胞中诱导依赖于 TREM2 的细胞内钙动员[1]。
As48 (0.3-30 μM; 0-120 min) 可通过诱导呈剂量和时间依赖性的 SYK 磷酸化，激活 HMC3 TREM2 过表达人小胶质细胞中的 TREM2 信号通路[1]。
As48 (25 μM; 30 min) 可通过荧光乳胶微球摄取实验检测到其能使 BV2 小鼠小胶质细胞的吞噬活性提升 1 倍[1]。
As48 (1-30 μM; 18 h) 可在体外以剂量依赖方式抑制 HEK293-TREM2 OE 细胞中 TREM2 胞外域的脱落[1]。
As48 (10-300 μM; 30 min) 不会在高达 300 μM 的浓度下抑制重组人 ADAM10 或 ADAM17 的蛋白水解活性，该结果由荧光蛋白酶活性检测法测得[1]。

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

As48 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HMC3 human microglial cells
Concentration: 0, 3, 10, 30, 100, 300 μM
Incubation Time: overnight
Result: Showed no significant cytotoxicity at concentrations up to 100 μM; Showed ~20% reduction in cell viabilityat 300 μM.

Western Blot Analysis[1]

Cell Line: HMC3 human microglial cells stably overexpressing TREM2 (HMC3 TREM2 OE cells)
Concentration: 0.3, 1, 3, 10, 30 μM
Incubation Time: 5, 10, 30, 60, 120 min
Result: Induced dose- and time-dependent SYK phosphorylation.

Western Blot Analysis[1]

Cell Line: HEK293 cells stably overexpressing TREM2 (HEK293-TREM2 OE cells)
Concentration: 1, 3, 10, 30 μM
Incubation Time: 18 h
Result: Showed dose-dependent preservation of the TREM2 extracellular domain, with significant protection against shedding at concentrations above 10 μM and maximal effect at 30 μM.
Reduced soluble TREM2 levels in conditioned media to a magnitude comparable to GM6001(HY-15768) (30 μM) at 3 μM, with no effect on APP secretion.
分子量

345.42

Formula

C20H15N3OS
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

As48 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:

As481214405-38-5As 48As-48TREM receptorSykTriggering receptors expressed on myeloid cellsSpleen tyrosine kinaseSYKGly68Alzheimer's diseaseTREM1TREM2HMC3 human microglial cellsmicroglial phagocytosisHEK293-hTREM2/DAP12 cellsBV2 murine microglial cellsADAM10Inhibitorinhibitorinhibit

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：
As48
目录号：
HY-182702
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