2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. PSFL2915

PSFL2915 是一种具有口服活性的 P2X 受体抑制剂，对人源 P2X3 的 IC50 为 0.319 μM，对大鼠 P2X2/3 的 IC50 为 0.261 μM，对人源 P2X2 的 IC50 为 13.3 μM，对人源 P2X3 的选择性约为对人源 P2X2 的 42 倍。\nPSFL2915 可通过阻止通道开放所需的头部结构域内口袋的变构收紧来抑制人源 P2X3 的激活，且其抑制作用具有镁离子依赖性。PSFL2915 可用于慢性咳嗽的研究。

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

PSFL2915

PSFL2915 Chemical Structure

CAS No. : 88134-39-8

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
1 mg ￥3000
2 - 4 周
5 mg 询价 2 - 4 周
10 mg 询价 2 - 4 周
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

PSFL2915 相关抗体

Top Publications Citing Use of Products

查看 P2X Receptor 亚型特异性产品:

查看所有亚型
P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PSFL2915 is a P2X receptor inhibitor with oral effectiveness, with an IC50 of 0.319 μM for human P2X3, 0.261 μM for rat P2X2/3, and 13.3 μM for human P2X2, and exhibits ~42-fold selectivity for human P2X3 over human P2X2. PSFL2915 inhibits human P2X3 activation by preventing allosteric tightening of the inner pocket of the head domain required for channel opening, with magnesium-dependent inhibition. PSFL2915 inhibits rat P2X2/3 and human P2X2 receptor activation, and has low activity against human P2X1, P2X4, and P2X7 receptors. PSFL2915 can be used for the research of chronic cough[1].

体外研究
(In Vitro)

PSFL2915 (0.01-3 μM; 0.6 μM; 1 μM) 是一种非竞争性、依赖 Mg2+的 hP2X3 变构抑制剂，对 hP2X3 的选择性约为 hP2X2 的 42 倍，可强效抑制 rP2X2/3 异源三聚体，且对其他 P2X 亚型的活性较低[1]。
PSFL2915 (1 μM) 通过靶向 hP2X3 头部结构域的内部口袋发挥抑制作用，这一点可通过其对包含该 hP2X3 结构域的 hP2X4 嵌合体的强效抑制作用得到证实[1]。
PSFL2915 (500 nM) 可抑制 ATP 诱导的 hP2X3 头部结构域内口袋构象变化，而该构象变化是通道激活所必需的[1]。

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

PSFL2915 相关抗体:
体内研究
(In Vivo)

PSFL2915 (15 mg/kg；灌胃；每日 2 次；连续 7 天) 可在氨气诱导的慢性咳嗽雄性 C57BL/6 小鼠中产生显著的镇咳活性，效力与相同剂量的 Gefapixant (HY-101588) 相当[1]。
PSFL2915 (10 mg/kg；灌胃；每日 2 次；连续 7 天) 可在柠檬酸/ATP 诱导的慢性咳嗽雄性 Hartley 豚鼠模型中产生显著的镇咳活性，其效力与相同剂量的 Gefapixant (HY-101588) 相当[1]。
PSFL2915 (15 mg/kg；灌胃；每日 2 次；7-10 天) 不会损伤雄性 C57BL/6 小鼠的味觉感知，这一点已通过针对苦味和甜味物质的双瓶偏好试验得到验证[1]。
PSFL2915 (10-20 mg/kg；腹腔注射) 不会损害雄性 Sprague Dawley 大鼠的苦味感知，该结果通过采用奎宁的双瓶偏好试验测得[1]。

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

Animal Model: C57BL/6 (male, 6-7 weeks old)[1]
Dosage: 15 mg/kg
Administration: oral gavage; twice daily; 7 days
Result: Significantly reduced cough frequency, with efficacy comparable to Gefapixant (HY-101588) at an equivalent dose.
Animal Model: C57BL/6 (male, 6-7 weeks old)[1]
Dosage: 15 mg/kg
Administration: oral gavage; twice daily; 7-10 days
Result: Did not alter quinine consumption rate 46.1%.
Did not alter acesulfame-K consumption rate 86.7%.
分子量

462.36

Formula

C15H10O13S2
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

PSFL2915 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:

PSFL291588134-39-8PSFL 2915PSFL-2915P2X ReceptorP2XRshuman P2X7P2X receptorhuman P2X2head domain inner pocketC57BL/6 micechronic coughhuman P2X1human P2X4rat P2X2/3human P2X3Inhibitorinhibitorinhibit

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：
PSFL2915
目录号：
HY-186112
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