1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel
  3. PF-05214030

PF-05214030 是一种 TRPV4 拮抗剂 (IC50: 对 hTRPV4 和 rTRPV4 分别为 4 和 27 nM)。PF-05214030 逆转 TRPV4 激动剂膀胱内输注引起的膀胱容量减少。

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PF-05214030 Chemical Structure

PF-05214030 Chemical Structure

CAS No. : 1669444-50-1

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5 mg ¥1600
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10 mg ¥2710
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25 mg ¥5420
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查看 TRP Channel 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-05214030 is a TRPV4 antagonist (IC50: 4 and 27nM for hTRPV4 and rTRPV4 respectively). PF-05214030 reverses the reduction in bladder capacity caused by intravesical infusion of a TRPV4 agonist[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 EC50
> 1000 nM
Compound: 3c
Agonist activity at rat TRPV4 expressed in CHOK1 cells assessed as changes in intracellular calcium level measured for 5 mins by FLIPR assay
Agonist activity at rat TRPV4 expressed in CHOK1 cells assessed as changes in intracellular calcium level measured for 5 mins by FLIPR assay
10.1039/C2MD20259J
CHO-K1 EC50
> 1000 nM
Compound: 3c
Agonist activity at human TRPV4 expressed in CHOK1 cells assessed as changes in intracellular calcium level measured for 5 mins by FLIPR assay
Agonist activity at human TRPV4 expressed in CHOK1 cells assessed as changes in intracellular calcium level measured for 5 mins by FLIPR assay
10.1039/C2MD20259J
CHO-K1 IC50
3.8 nM
Compound: 3c
Antagonist activity at human TRPV4 expressed in CHOK1 cells assessed as inhibition of PF-04674114/GSK1016790A-induced changes in intracellular calcium level measured for 5 mins by FLIPR assay
Antagonist activity at human TRPV4 expressed in CHOK1 cells assessed as inhibition of PF-04674114/GSK1016790A-induced changes in intracellular calcium level measured for 5 mins by FLIPR assay
10.1039/C2MD20259J
CHO-K1 IC50
34.1 nM
Compound: 3c
Antagonist activity at rat TRPV4 expressed in CHOK1 cells assessed as inhibition of PF-04674114/GSK1016790A-induced changes in intracellular calcium level measured for 5 mins by FLIPR assay
Antagonist activity at rat TRPV4 expressed in CHOK1 cells assessed as inhibition of PF-04674114/GSK1016790A-induced changes in intracellular calcium level measured for 5 mins by FLIPR assay
10.1039/C2MD20259J
分子量

431.27

Formula

C17H13Cl2FN2O4S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 200 mg/mL (463.75 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3187 mL 11.5937 mL 23.1873 mL
5 mM 0.4637 mL 2.3187 mL 4.6375 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3187 mL 11.5937 mL 23.1873 mL 57.9683 mL
5 mM 0.4637 mL 2.3187 mL 4.6375 mL 11.5937 mL
10 mM 0.2319 mL 1.1594 mL 2.3187 mL 5.7968 mL
15 mM 0.1546 mL 0.7729 mL 1.5458 mL 3.8646 mL
20 mM 0.1159 mL 0.5797 mL 1.1594 mL 2.8984 mL
25 mM 0.0927 mL 0.4637 mL 0.9275 mL 2.3187 mL
30 mM 0.0773 mL 0.3865 mL 0.7729 mL 1.9323 mL
40 mM 0.0580 mL 0.2898 mL 0.5797 mL 1.4492 mL
50 mM 0.0464 mL 0.2319 mL 0.4637 mL 1.1594 mL
60 mM 0.0386 mL 0.1932 mL 0.3865 mL 0.9661 mL
80 mM 0.0290 mL 0.1449 mL 0.2898 mL 0.7246 mL
100 mM 0.0232 mL 0.1159 mL 0.2319 mL 0.5797 mL
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.

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Inquiry Information

产品名称:
PF-05214030
目录号:
HY-160603
需求量: