TRPV4 agonist-1 free base |
Catalog No.GC63244
One-Click Copy Product Info
|
TRPV4 agonist-1 free base is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC50 value of 60nM in the hTRPV4 Ca2+ test.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2314467-59-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
TRPV4 agonist-1 free base is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC50 value of 60nM in the hTRPV4 Ca2+ test[1]. TRPV4 is a non-selective cation channel that can act as a cell sensor to sense mechanical stimulation, osmotic pressure changes, temperature and certain chemical signals, and plays an important role in the development of drugs for a variety of diseases[2, 3]. TRPV4 agonist-1 free base can bind to the TRPV4 channel protein. The binding site is located in the cytoplasmic pocket formed between S1 and S4. TRPV4 agonist-1 free base binds to this pocket, causing the S4-S5 linker in the TRPV4 structure to move upward, thereby causing S6 to move, opening the TRPV4 channel and playing the role of an agonist[4].
References:
[1] Atobe M, Nagami T, Muramatsu S, 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]. Journal of medicinal chemistry, 2019, 62(3): 1468-1483.
[2] Plant T D, Strotmann R. Trpv4[J]. Transient Receptor Potential (TRP) Channels, 2007: 189-205.
[3] Koskimäki S, Tojkander S. TRPV4—A multifunctional cellular sensor protein with therapeutic potential[J]. Sensors, 2024, 24(21): 6923.
[4] Zhen W, Zhao Z, Chang S, et al. Structural basis of ligand activation and inhibition in a mammalian TRPV4 ion channel[J]. Cell discovery, 2023, 9(1): 70.
| Cas No. | 2314467-59-7 | SDF | |
| Formula | C25H22F2N4O2 | M.Wt | 448.46 |
| Solubility | DMSO : 83.33 mg/mL (185.81 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2299 mL | 11.1493 mL | 22.2985 mL |
| 5 mM | 446 μL | 2.2299 mL | 4.4597 mL |
| 10 mM | 223 μL | 1.1149 mL | 2.2299 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)