| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
TRPV4 (transient receptor potential vanilloid 4)
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|---|---|
| ln Vitro |
TRPV4 agonist-1 (compound 36) had noticeably higher potency (ECmax: 20 nM in SOX9 reporter assay). On TRPV1 channels, TRPV4 agonist-1 is inactive [1].
TRPV4 agonist is a potent activator of the TRPV4 channel with an EC50 of 60 nM in the hTRPV4 Ca2+ assay. The compound exhibits significantly increased potency (ECmax: 20 nM) in the SOX9 reporter assay. TRPV4 is a calcium-permeable cation channel that responds to mechanical stimuli, osmotic changes, and chemical agonists. Activation of TRPV4 leads to calcium influx and subsequent cellular responses including regulation of cell volume, pain signaling, and cartilage homeostasis. |
| ln Vivo |
In vivo studies of TRPV4 agonists explore their roles in pain modulation, inflammation, and cartilage homeostasis. TRPV4 activation has been shown to have analgesic effects in some pain models, while in other contexts it may promote pain signaling. The compound is being investigated as a research tool to study TRPV4 function in various physiological and pathological conditions.
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| Enzyme Assay |
TRPV4 channel activity is measured using calcium flux assays in cells expressing recombinant human TRPV4. EC50 values are determined from dose-response curves measuring calcium influx upon compound treatment. SOX9 reporter assays are used to assess the compound's activity in chondrocyte differentiation and cartilage-related pathways.
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| Cell Assay |
Cellular potency is evaluated in cells expressing human TRPV4 using calcium flux assays to measure channel activation. EC50 of 60 nM is determined from dose-response curves. SOX9 reporter gene assays are used to assess the compound's activity in chondrocyte-related signaling. Effects on intracellular calcium levels and downstream signaling pathways are measured to characterize the compound's cellular activity.
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| Animal Protocol |
In vivo studies are conducted in animal models of pain, inflammation, and cartilage disorders. TRPV4 agonist is administered via appropriate routes at various doses. Pain-related endpoints, inflammatory markers, and cartilage integrity are assessed. Pharmacodynamic biomarkers are measured to confirm target engagement and pathway modulation.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for TRPV4 agonist are limited as the compound is primarily used as a research tool. The compound is soluble in DMSO for formulation. In vivo formulations may be prepared using DMSO-based vehicles. The compound has a molecular weight of 484.93 and a molecular formula of C25H23ClF2N4O2.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for TRPV4 agonist are limited as the compound is primarily used for research purposes. Standard laboratory safety precautions should be observed during handling. The compound is not intended for human therapeutic use and has not been evaluated in formal toxicology studies.
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| References | |
| Additional Infomation |
TRPV4 agonist (OUN67600) is a research tool for studying TRPV4 channel function in various physiological and pathological processes including pain, inflammation, and cartilage homeostasis. The compound exhibits potent activity with an EC50 of 60 nM in calcium flux assays and ECmax of 20 nM in SOX9 reporter assays. TRPV4 is an emerging therapeutic target for pain, osteoarthritis, and other conditions. The compound remains a research tool for studying TRPV4 biology.
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| Molecular Formula |
C25H23CLF2N4O2
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|---|---|
| Molecular Weight |
484.925531625748
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| Exact Mass |
484.147
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| Elemental Analysis |
C, 61.92; H, 4.78; Cl, 7.31; F, 7.84; N, 11.55; O, 6.60
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| CAS # |
2314467-60-0
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| Related CAS # |
2314467-60-0 (HCl);2314467-59-7;
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| PubChem CID |
137628675
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
713
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.FC1=CC=CC2=C1N=C(N(C1C=CC(=CC=1)OC1C=CC(=CC=1)F)C2=O)N1CCN(C)CC1
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| InChi Key |
ONVDBGZQVBEFIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H22F2N4O2.ClH/c1-29-13-15-30(16-14-29)25-28-23-21(3-2-4-22(23)27)24(32)31(25)18-7-11-20(12-8-18)33-19-9-5-17(26)6-10-19;/h2-12H,13-16H2,1H3;1H
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| Chemical Name |
8-fluoro-3-[4-(4-fluorophenoxy)phenyl]-2-(4-methylpiperazin-1-yl)quinazolin-4-one;hydrochloride
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| Synonyms |
OUN67600; OUN-67600;; OUN 67600; TRPV4 Agonist;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0622 mL | 10.3108 mL | 20.6215 mL | |
| 5 mM | 0.4124 mL | 2.0622 mL | 4.1243 mL | |
| 10 mM | 0.2062 mL | 1.0311 mL | 2.0622 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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