| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
RN9893 HCl targets the transient receptor potential vanilloid 4 (TRPV4) ion channel. As a potent and selective antagonist, it blocks TRPV4-mediated calcium influx and downstream signaling. It shows excellent selectivity over related TRP receptors, such as TRPV1, TRPV3, and TRPM8. Its IC50 values vary across species, with the highest potency for mouse TRPV4.
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|---|---|
| ln Vitro |
In vitro, RN9893 HCl inhibits human, rat, and murine TRPV4 variants with IC50 values of 420 nM (human), 660 nM (rat), and 320 nM (mouse). It shows >15-fold selectivity for TRPV4 over TRPV1, TRPV3, and TRPM8. Its activity is confirmed in calcium flux assays using cells expressing TRPV4 channels.
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| ln Vivo |
In vivo, RN9893 HCl is a potent and specific TRPV4 receptor blocker. However, specific in vivo efficacy data in animal models are limited. Its selectivity and potency make it a valuable tool for studying TRPV4 function in vivo. It has potential applications in pain, inflammation, and other TRPV4-mediated conditions.
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| Enzyme Assay |
Cell-free assays for RN9893 HCl are not standard because it targets an ion channel. Its activity is assessed using calcium flux assays or electrophysiological techniques on cells expressing TRPV4 channels. The IC50 for TRPV4 inhibition is determined. Its molecular weight and formula are confirmed by mass spectrometry. Its purity is confirmed by HPLC.
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| Cell Assay |
Cellular assays for RN9893 HCl are performed using cell lines expressing human, rat, or mouse TRPV4 channels. Cells are loaded with a calcium-sensitive fluorescent dye and treated with varying concentrations of RN9893 HCl. Calcium influx is induced by a TRPV4 agonist, and the inhibition of calcium flux is measured. The IC50 for TRPV4 inhibition is determined.
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| Animal Protocol |
In vivo animal experiments for RN9893 HCl are not extensively documented. To study TRPV4 function, animal models of pain, inflammation, or cardiovascular disease could be used. Animals would be administered RN9893 HCl via appropriate routes, and physiological or behavioral endpoints would be assessed.
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| ADME/Pharmacokinetics |
RN9893 HCl has a molecular weight of approximately 478.93 g/mol (for the hydrochloride salt) and a molecular formula of C20H21Cl2FN4O3·HCl. It is a solid powder with a purity of >98%. It is soluble in DMSO and should be stored under recommended conditions. Its chemical name is not specified in the available sources.
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| Toxicity/Toxicokinetics |
The toxicological profile of RN9893 HCl has not been extensively characterized. As a research compound, it is generally considered safe at the concentrations used in studies. No significant toxicity has been reported. Comprehensive toxicology studies are lacking. It is not an approved drug and is intended for research use only.
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| References | |
| Additional Infomation |
RN9893 HCl is a potent and selective TRPV4 antagonist with IC50 values of 320 nM (mouse), 420 nM (human), and 660 nM (rat). It shows >15-fold selectivity over TRPV1, TRPV3, and TRPM8. It is a research compound for studying TRPV4 function in pain, inflammation, and other conditions. It is also known as RN-9893.
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| Molecular Formula |
C21H24CLF3N4O5S
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|---|---|
| Molecular Weight |
536.95
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| Exact Mass |
500.134
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| Elemental Analysis |
C, 50.40; H, 4.63; F, 11.39; N, 11.19; O, 15.98; S, 6.41
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| CAS # |
1803003-68-0
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| Related CAS # |
2109450-40-8 (HCl);1803003-68-0;
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| PubChem CID |
121513879
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.584
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| LogP |
4.26
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
827
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.S(C1C=CC(=CC=1)NC(C1C=CC(C(F)(F)F)=CC=1[N+](=O)[O-])=O)(N1CCN(C(C)C)CC1)(=O)=O
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| InChi Key |
ULUOUAGDTULBRZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23F3N4O5S.ClH/c1-14(2)26-9-11-27(12-10-26)34(32,33)17-6-4-16(5-7-17)25-20(29)18-8-3-15(21(22,23)24)13-19(18)28(30)31;/h3-8,13-14H,9-12H2,1-2H3,(H,25,29);1H
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| Chemical Name |
2-nitro-N-[4-(4-propan-2-ylpiperazin-1-yl)sulfonylphenyl]-4-(trifluoromethyl)benzamide;hydrochloride
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| Synonyms |
RN 9893 HCl; RN-9893 HCl; RN9893 HCl
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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) |
DMSO : ~250 mg/mL (~499.51 mM)
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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 | 1.8624 mL | 9.3119 mL | 18.6237 mL | |
| 5 mM | 0.3725 mL | 1.8624 mL | 3.7247 mL | |
| 10 mM | 0.1862 mL | 0.9312 mL | 1.8624 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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