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

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.

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PF-05214030 Chemical Structure

PF-05214030 Chemical Structure

CAS No. : 1669444-50-1

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Based on 1 publication(s) in Google Scholar

PF-05214030 Related Antibodies

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TRPC TRPM TRPV TRPA TRPML

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Description

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].

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
Molecular Weight

431.27

Formula

C17H13Cl2FN2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC=C(C=C1F)OCC2(CN(S(=O)(C3=CC=C(C=C3Cl)Cl)=O)C2)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (463.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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PF-05214030 Related Classifications

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:

PF-052140301669444-50-1PF05214030PF 05214030TRP ChannelTransient receptor potential channelsbladder capacityTRPV4 antagonistInhibitorinhibitorinhibit

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