TRPV4 agonist-1 free base

Name: TRPV4 agonist-1 free base
Brand: MedChemExpress
SKU: HY-114400
Rating: 4.5 (1 reviews)

Cat. No.: HY-114400 Purity: 99.58%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

TRPV4 agonist-1 free base is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC₅₀ of 60 nM in the hTRPV4 Ca²⁺ assay.

For research use only. We do not sell to patients.

TRPV4 agonist-1 free base Chemical Structure

CAS No. : 2314467-59-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 160	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 160	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of TRPV4 agonist-1 free base:

TRPV4 agonist-1 Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

TRPV4 agonist-1 free base is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC₅₀ of 60 nM in the hTRPV4 Ca²⁺ assay^[1].

IC₅₀ & Target

EC50: 60 nM (hTRPV4 hTRPV4 Ca²⁺)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	60 nM Compound: 36	Agonist activity at recombinant human TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium level after 30 mins by Fura-2 AM/Pluronic F-127 probe based fluorescence assay Agonist activity at recombinant human TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium level after 30 mins by Fura-2 AM/Pluronic F-127 probe based fluorescence assay	[PMID: 30629441]

In Vitro

TRPV4 agonist-1 (Compound 36) exhibits significantly increased potency (EC_max: 20 nM in the SOX9 reporter assay). TRPV4 agonist-1 is inactive against TRPV1 channels^[1].

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

Molecular Weight

448.46

Formula

C₂₅H₂₂F₂N₄O₂

CAS No.

2314467-59-7

Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C2=CC=C(OC3=CC=C(F)C=C3)C=C2)C(N4CCN(C)CC4)=NC5=C(F)C=CC=C51

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL (185.81 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	2.2299 mL	11.1493 mL	22.2985 mL
5 mM	0.4460 mL	2.2299 mL	4.4597 mL
10 mM	0.2230 mL	1.1149 mL	2.2299 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.58%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (249 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Atobe M, et al. Discovery of Novel Transient Receptor Potential Vanilloid 4 (TRPV4) Agonists as Regulators of Chondrogenic Differentiation: Identification of Quinazolin-4(3 H)-ones and in Vivo Studies on a Surgically Induced Rat Model of Osteoarthritis. J Med Chem. 2019 Jan 28. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2299 mL	11.1493 mL	22.2985 mL	55.7463 mL
	5 mM	0.4460 mL	2.2299 mL	4.4597 mL	11.1493 mL
	10 mM	0.2230 mL	1.1149 mL	2.2299 mL	5.5746 mL
	15 mM	0.1487 mL	0.7433 mL	1.4866 mL	3.7164 mL
	20 mM	0.1115 mL	0.5575 mL	1.1149 mL	2.7873 mL
	25 mM	0.0892 mL	0.4460 mL	0.8919 mL	2.2299 mL
	30 mM	0.0743 mL	0.3716 mL	0.7433 mL	1.8582 mL
	40 mM	0.0557 mL	0.2787 mL	0.5575 mL	1.3937 mL
	50 mM	0.0446 mL	0.2230 mL	0.4460 mL	1.1149 mL
	60 mM	0.0372 mL	0.1858 mL	0.3716 mL	0.9291 mL
	80 mM	0.0279 mL	0.1394 mL	0.2787 mL	0.6968 mL
	100 mM	0.0223 mL	0.1115 mL	0.2230 mL	0.5575 mL