Cat. No.: HY-160603

PF-05214030

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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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Pureté: 99.81%
CAS No.: 1669444-50-1
Formule: C₁₇H₁₃Cl₂FN₂O₄S
Masse moléculaire:431.27

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PF-05214030 Chemical Structure

CAS No.: 1669444-50-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

TRPV4

Voir tous les produits spécifiques à Isoform TRP Channel :

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	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
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

Chemical Information

CAS No. 1669444-50-1
Appearance Solid
Masse moléculaire 431.27
Formule C₁₇H₁₃Cl₂FN₂O₄S
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (231.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3187 mL

11.5937 mL

23.1873 mL

5 mM

0.4637 mL

2.3187 mL

4.6375 mL

10 mM

0.2319 mL

1.1594 mL

2.3187 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (11.59 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (11.59 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (270 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Jiang Y, et al. Targeting extracellular matrix stiffness and mechanotransducers to improve cancer therapy. J Hematol Oncol. 2022 Mar 24;15(1):34. [Content Brief]

[2]. Sarah Skerratt, et al. The Discovery and Optimisation of a Highly Selective Series of TRPV4 Antagonists.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Voir tous les produits spécifiques à Isoform TRP Channel

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PF-05214030

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Voir tous les produits spécifiques à Isoform TRP Channel

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PF-05214030 Related Classifications

HY-160603 Related Classifications