| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
REV 5901 targets two main pathways: the cysteinyl leukotriene receptor 1 (CysLT1) and the 5-lipoxygenase (5-LOX) enzyme. By acting as a competitive receptor antagonist, it blocks the binding of leukotrienes like LTC4, LTD4, and LTE4, which are pro-inflammatory mediators. Concurrently, by inhibiting 5-LOX, it prevents the synthesis of leukotrienes from arachidonic acid in the first place. This dual mechanism disrupts the lipoxygenase pathway, affecting the production of inflammatory signaling molecules such as leukotrienes, resolvins, and lipoxins.
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| ln Vitro |
In cell-free biochemical assays, REV 5901 directly inhibits the 5-LOX enzyme, preventing the conversion of arachidonic acid to leukotrienes. It also binds to cysteinyl leukotriene receptors, acting as a competitive antagonist. The compound has been shown to induce apoptosis by activating caspases and causing morphological changes in cells, leading to a more differentiated phenotype. It also inhibits cell growth by disrupting the lipoxygenase pathway.
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| ln Vivo |
The cellular effects of REV 5901 include the inhibition of cell growth and the induction of caspase-dependent apoptosis. In the presence of an autophagy inhibitor, an increased mortality of cells is observed, suggesting a cytoprotective role for autophagy in the context of REV 5901 treatment. The compound's anti-inflammatory and anticancer activities are attributed to its ability to suppress the conversion of arachidonic acid into pro-inflammatory and pro-tumorigenic biologically active metabolites.
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| Enzyme Assay |
To assess the binding of REV 5901 to the CysLT1 receptor, a competition binding assay is performed using radiolabeled ligand, typically [3H]-LTD4, and guinea pig lung membranes. The membranes are incubated with the radioligand and varying concentrations of REV 5901 (0.1 nM-100 uM) in a binding buffer for 60-120 minutes at room temperature. Bound radioactivity is separated by filtration through glass fiber filters and counted. Ki values are calculated from IC50 values using the Cheng-Prusoff equation. For 5-LOX inhibition, rat neutrophil 5-LO is incubated with arachidonic acid and varying concentrations of REV 5901, and product formation is measured by HPLC.
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| Cell Assay |
The cytotoxic effects of REV 5901 on cancer cells are evaluated using standard cell viability assays. Colon carcinoma cell lines, such as HT-29 or HCT-116, are seeded in 96-well plates (5,000-10,000 cells/well) and cultured overnight. The cells are then treated with REV 5901 at concentrations ranging from 1-100 uM for 24-72 hours. Cell viability is measured using the MTT assay or the CellTiter-Glo luminescent assay. IC50 values are calculated from dose-response curves. Apoptosis is confirmed by Annexin V/PI staining and flow cytometry, as well as by measuring caspase-3/7 activity using a luminescent substrate.
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| Animal Protocol |
In vivo studies have shown that REV 5901 can inhibit the growth of colon carcinoma xenografts in mouse models. Tumor-bearing mice are typically treated with REV 5901 via oral gavage at doses ranging from 1-50 mg/kg daily for 2-4 weeks. Tumor volume is measured twice weekly with calipers. The primary endpoint is tumor growth inhibition (TGI), calculated relative to a vehicle-treated control group. At study termination, tumors are harvested for immunohistochemical analysis of proliferation (Ki-67) and apoptosis (cleaved caspase-3). In asthma models, airway hyperresponsiveness and bronchoalveolar lavage fluid (BALF) inflammatory cell counts are measured.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic studies for REV 5901 are limited in the public domain. However, based on its chemical properties (molecular weight 335.44, LogP ~4-5) and the fact that it is described as orally bioavailable, it is expected to have moderate-to-high intestinal absorption. It is typically formulated in vehicles such as DMSO or ethanol diluted in saline for in vivo administration. As a 5-LOX inhibitor, it is likely to be metabolized by the liver, potentially by cytochrome P450 enzymes, and excreted via bile. Its plasma half-life in animal models is likely between 2-6 hours, supporting a once- or twice-daily dosing regimen.
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| Toxicity/Toxicokinetics |
Formal toxicology data for REV 5901 have not been extensively published. However, as a dual CysLT1 antagonist and 5-LOX inhibitor, its safety profile may be related to its pharmacological mechanism. Potential side effects could include gastrointestinal disturbances and headache, similar to other leukotriene inhibitors and antagonists. In preclinical animal models at therapeutic doses (e.g., 10-50 mg/kg), the compound is generally well-tolerated, with no reports of significant body weight loss or acute organ toxicity. For research use, standard laboratory safety practices should be followed. The compound has not been approved for clinical use.
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| References |
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| Additional Infomation |
1-[3-(2-quinolinylmethoxy)phenyl]-1-hexanol is a member of the quinoline class of compounds.
REV 5901 (CAS 101910-24-1) is a research-grade compound used to study the role of the lipoxygenase pathway in inflammation and cancer. It is known by the synonym Rev-5901. The compound is a valuable chemical probe for dissecting the overlapping functions of CysLT1 antagonism and 5-LOX inhibition in disease models. It has been cited in literature for its potential to induce apoptosis and inhibit the growth of colon carcinoma in vivo. REV 5901 is not approved for human therapeutic use and is intended for laboratory research only. It should be stored at -20degC and protected from light. |
| Molecular Formula |
C22H25NO2
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|---|---|
| Molecular Weight |
335.4394
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| Exact Mass |
335.188
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| CAS # |
101910-24-1
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| PubChem CID |
5059
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
497.7±35.0 °C at 760 mmHg
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| Flash Point |
254.8±25.9 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.606
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| LogP |
4.94
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
25
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| Complexity |
375
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JRLOEMCOOZSCQP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H25NO2/c1-2-3-4-12-22(24)18-9-7-10-20(15-18)25-16-19-14-13-17-8-5-6-11-21(17)23-19/h5-11,13-15,22,24H,2-4,12,16H2,1H3
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| Chemical Name |
1-[3-(quinolin-2-ylmethoxy)phenyl]hexan-1-ol
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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 | 2.9812 mL | 14.9058 mL | 29.8116 mL | |
| 5 mM | 0.5962 mL | 2.9812 mL | 5.9623 mL | |
| 10 mM | 0.2981 mL | 1.4906 mL | 2.9812 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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