| Size | Price | Stock | Qty |
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| 50mg |
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| Other Sizes |
| Targets |
TRPM3 Retinoblastoma protein
D-erythro-Sphingosine hydrochloride targets the transient receptor potential melastatin 3 (TRPM3) channel as a specific activator. TRPM3 is a non-selective cation channel involved in calcium signaling, pain sensation, and neuroinflammation. The compound also induces retinoblastoma protein dephosphorylation, indicating effects on cell cycle regulation. It inhibits protein kinase C and calmodulin-dependent enzymes. As a sphingolipid, it modulates sphingolipid metabolism and impacts cellular processes such as apoptosis, proliferation, and differentiation. The compound may stimulate mast cells through activation of protein kinase C. |
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| ln Vitro |
When D-erythro-Sphingosine (20 μM) is applied extracellularly, TRPM3-transfected HEK293 cells exhibit a rise in [Ca2+]i within 20 to 30 seconds of the administration beginning, but nontransfected control cells (NT) only exhibit very minor responses[1]. Through TRPM3, currents are induced by D-erythro-Sphingosine (10 μM)[1]. D-erythro-Sphingosine (500 nM; 24 h) induces retinoblastoma protein dephosphorylation, which occurs prior to growth inhibition and a particular arrest in the G0/G1 phase of the cell cycle[2].
In vitro studies demonstrate that D-erythro-Sphingosine hydrochloride is a specific TRPM3 activator. It induces retinoblastoma protein dephosphorylation, indicating effects on cell cycle regulation. The compound inhibits protein kinase C and calmodulin-dependent enzymes. As a sphingolipid, it modulates sphingolipid metabolism and impacts cellular processes including apoptosis, proliferation, and differentiation. It may stimulate mast cells through activation of protein kinase C. The compound is widely employed in lipid metabolism, cancer, and neurobiology research to study sphingolipid functions. |
| ln Vivo |
In vivo studies of D-erythro-Sphingosine hydrochloride are limited in publicly available literature, as the compound is primarily used as a research tool for in vitro characterization of sphingolipid and TRPM3 functions. Given its role as a TRPM3 activator and modulator of sphingolipid metabolism, the compound may have potential for in vivo investigations of pain, neuroinflammation, and cancer. It is widely employed in lipid metabolism, cancer, and neurobiology research to study sphingolipid functions and to develop potential therapeutic strategies targeting sphingolipid-mediated pathways. Further in vivo research is needed to establish its pharmacokinetic and pharmacodynamic profiles.
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| Enzyme Assay |
For TRPM3 channel activation assays, cells expressing TRPM3 channels (e.g., HEK293 cells) are cultured and loaded with calcium-sensitive fluorescent dyes. D-erythro-Sphingosine hydrochloride is dissolved in DMSO or appropriate buffer and diluted to varying concentrations. Cells are treated with the compound and calcium flux is measured using fluorescence plate readers. TRPM3 activation is assessed by measuring intracellular calcium increases. For kinase inhibition assays, protein kinase C or calmodulin-dependent enzymes are incubated with the compound and substrates. Enzyme activity is measured by appropriate methods (e.g., radioactive or colorimetric assays). IC50 or EC50 values are calculated from dose-response curves. Assays are performed in replicate with vehicle controls.
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| Cell Assay |
For in vitro cellular assays, cell lines of interest (e.g., cancer cells, neuronal cells, or TRPM3-expressing HEK293 cells) are cultured in appropriate media under standard conditions (37°C, 5% CO2). D-erythro-Sphingosine hydrochloride is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. Cellular responses are assessed by measuring calcium flux (for TRPM3 activation), cell viability (MTT assay), apoptosis markers, proliferation, differentiation markers, and retinoblastoma protein phosphorylation status (Western blot). Each concentration is tested in replicate wells with vehicle controls and positive controls.
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| Animal Protocol |
For in vivo animal studies of D-erythro-Sphingosine hydrochloride, no specific protocols have been published in the available literature. For general in vivo administration of sphingolipid analogs, compounds are typically formulated in suitable vehicles (e.g., DMSO/PEG/saline mixtures or cyclodextrin-based formulations) and administered via intraperitoneal (i.p.), intravenous (i.v.), or subcutaneous (s.c.) injection. Dosing regimens vary by study objective. Blood samples are collected at predetermined time points for pharmacokinetic analysis by LC-MS/MS. Tissue distribution and target engagement can be assessed post-mortem. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of D-erythro-Sphingosine hydrochloride are characteristic of a sphingolipid compound. The compound has a molecular weight of 335.95, formula C18H38ClNO2, and CAS number 2673-72-5. The hydrochloride form enhances solubility and stability for experimental use. Storage: typically at -20°C for powder; in solvent at -80°C. Solubility: soluble in DMSO, ethanol, and other organic solvents; aqueous solubility is enhanced by the hydrochloride salt form. The compound is a natural sphingolipid that plays a crucial role in various biological processes. Specific pharmacokinetic parameters such as half-life, clearance, and bioavailability are not extensively reported in publicly available sources.
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| Toxicity/Toxicokinetics |
According to available safety information, D-erythro-Sphingosine hydrochloride is intended for research use only and not for human therapeutic applications. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. The compound is not for human use and no clinical toxicity data are available. As a sphingolipid, it may have effects on cell signaling and apoptosis that should be considered in experimental design.
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| References | |
| Additional Infomation |
D-erythro-Sphingosine hydrochloride (Erythrosphingosine hydrochloride) is a specific TRPM3 activator that also induces retinoblastoma protein dephosphorylation. It inhibits protein kinase C and calmodulin-dependent enzymes and may stimulate mast cells through activation of protein kinase C. As a sphingolipid, it modulates sphingolipid metabolism and impacts cellular processes such as apoptosis, proliferation, and differentiation. The compound is widely employed in lipid metabolism, cancer, and neurobiology research. It is for research use only with no clinical development or regulatory approvals reported.
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| Molecular Formula |
C18H38CLNO2
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| Molecular Weight |
335.95
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| Exact Mass |
335.259
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| CAS # |
2673-72-5
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| Related CAS # |
D-erythro-Sphingosine;123-78-4
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| PubChem CID |
17998971
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| Appearance |
White to off-white solid powder
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| LogP |
5.426
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
22
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| Complexity |
231
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCCCCCCCCCCCC/C=C/[C@H]([C@H](CO)N)O.Cl
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| InChi Key |
YDIHJJLAPMAISR-ZNWYJMOFSA-N
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| InChi Code |
InChI=1S/C18H37NO2.ClH/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-18(21)17(19)16-20;/h14-15,17-18,20-21H,2-13,16,19H2,1H3;1H/b15-14+;/t17-,18+;/m0./s1
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| Chemical Name |
(E,2S,3R)-2-aminooctadec-4-ene-1,3-diol;hydrochloride
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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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9766 mL | 14.8832 mL | 29.7663 mL | |
| 5 mM | 0.5953 mL | 2.9766 mL | 5.9533 mL | |
| 10 mM | 0.2977 mL | 1.4883 mL | 2.9766 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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