| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
The primary target of RV 538 is ceramide UDP-glucosyltransferase (UGCG), also known as glucosylceramide synthase (GCS). This enzyme is responsible for the synthesis of glucosylceramide from ceramide and UDP-glucose. RV 538 acts as a potent and competitive inhibitor of this enzyme, meaning it competes with the natural substrate, ceramide, for binding to the active site. By inhibiting UGCG, RV 538 reduces the production of glucosylceramide and other glycosphingolipids, which can affect various cellular functions including cell growth, differentiation, and apoptosis.
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| ln Vitro |
In vitro, RV 538 demonstrates potent inhibition of glucosylceramide synthase. Its activity is assessed in enzyme assays using microsomal preparations or recombinant UGCG enzyme and radiolabeled UDP-glucose as a substrate. The compound shows competitive inhibition, with its potency determined by measuring the reduction in glucosylceramide synthesis. However, detailed IC50 or Ki values for RV 538 are not extensively reported in the available literature.
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| ln Vivo |
In vivo data for RV 538 are not extensively reported in the available literature. As an inhibitor of glucosylceramide synthase, the compound has potential for in vivo applications in studying the role of glycosphingolipids in cancer and other diseases. However, specific in vivo efficacy data, including animal models, dosing regimens, and pharmacokinetic-pharmacodynamic relationships, are not detailed in the available sources. The compound is classified as a research-use-only chemical.
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| Enzyme Assay |
In vitro enzyme assays for RV 538 typically involve measuring its inhibition of ceramide UDP-glucosyltransferase (UGCG) activity. The enzyme, often obtained from microsomal preparations or as a recombinant protein, is incubated with ceramide and UDP-glucose (or radiolabeled UDP-glucose) in the presence of varying concentrations of RV 538. The production of glucosylceramide is measured, and the compound's inhibitory activity is determined.
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| Cell Assay |
In vitro cellular assays for RV 538 are performed in various cell lines to assess its effects on glycosphingolipid metabolism and cellular functions. Cells are treated with RV 538, and the levels of glucosylceramide and other glycosphingolipids are measured by lipidomics or TLC. The compound's effects on cell viability, proliferation, and apoptosis are also assessed. These assays are used to study the role of glycosphingolipids in cellular physiology.
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| Animal Protocol |
In vivo animal studies with RV 538 are not extensively documented in the available literature. Based on its inhibition of glucosylceramide synthase, potential in vivo models could include xenograft models for cancer or models of lysosomal storage diseases. In such studies, RV 538 would be administered orally or intraperitoneally, and endpoints would include tumor growth, glycosphingolipid levels, and survival. However, specific protocols are not detailed in the available sources.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for RV 538 are not extensively reported. The compound is a ceramide analog with a molecular weight that is not specified in the available literature. It is expected to be lipophilic and cell-permeable. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not available in the literature for this research compound.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for RV 538 are not extensively reported. The compound is classified as a research-use-only chemical and is not intended for human consumption. As an inhibitor of glycosphingolipid synthesis, it may have effects on cellular membranes and signaling that could contribute to toxicity. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| References |
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| Additional Infomation |
RV 538 is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying the role of glucosylceramide synthase and glycosphingolipids in cellular processes. The compound is used to investigate the role of glycosphingolipids in cancer, apoptosis, and lysosomal storage diseases. It is also used as a reference standard in studies of sphingolipid metabolism.
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| Molecular Formula |
C23H39CLN2O3
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|---|---|
| Molecular Weight |
427.026
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| Exact Mass |
426.264
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| CAS # |
73257-80-4
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| PubChem CID |
114736
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| Appearance |
White to off-white solid powder
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| Boiling Point |
555.1ºC at 760 mmHg
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| Flash Point |
289.5ºC
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| LogP |
4.808
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
29
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| Complexity |
403
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| Defined Atom Stereocenter Count |
0
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| Chemical Name |
Decanamide, N-(2-hydroxy-1-(4-morpholinylmethyl)-2-phenylethyl)-, hydrochloride
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| Synonyms |
RV 538 PDMP DL-PDMPDAMPP
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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 | 2.3418 mL | 11.7088 mL | 23.4176 mL | |
| 5 mM | 0.4684 mL | 2.3418 mL | 4.6835 mL | |
| 10 mM | 0.2342 mL | 1.1709 mL | 2.3418 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06443385 | ACTIVE, NOT RECRUITING | Behavioral: PDMP Legal Mandate E-mail Behavioral: PDMP Clinical Benefit E-mail |
Opioid Prescribing Prescription Drug Misuse |
Columbia University | 2024-07-17 | Not Applicable |
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