| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Human Endogenous Metabolite
Sphinganine 1-phosphate targets sphingosine-1-phosphate receptor 1 (S1P1) as an antagonist. The compound also activates the EDG family of G-protein coupled receptors, which are involved in various cellular signaling pathways. Through these receptors, sphinganine 1-phosphate regulates cell proliferation, survival, differentiation, and migration. The compound functions as a potent signaling molecule through both intracellular pathways and extracellular receptor-mediated signaling. In addition to receptor-mediated effects, sphinganine 1-phosphate may also act intracellularly as a second messenger. The compound is an intermediate in the metabolism of glycosphingolipids and sphingolipids, and its levels are tightly regulated by the balance between synthesis and degradation. Sphinganine 1-phosphate is involved in various physiological processes including angiogenesis, cancer, lymphocyte trafficking, and cell stress responses. Its role as an S1P1 antagonist distinguishes it from sphingosine-1-phosphate (S1P), which is an agonist at S1P receptors. The compound's ability to regulate cell migration and differentiation makes it a key player in immune regulation and vascular biology. |
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| ln Vitro |
Sphinganine 1-phosphate (S1P) is a powerful signaling molecule implicated in angiogenesis, cancer, lymphocyte trafficking, and cell stress responses. The main way that sphinganine 1-phosphate works is by stimulating a particular subset of G-protein coupled cell surface receptors called the endothelial differentiation gene (EDG) family. Sphinganine 1-phosphate regulates cell metabolism in the opposite way. Skeletal muscle regeneration and differentiation are regulated by sphinganine 1-phosphate[1]. In cancer, sphinganine 1-phosphate (S1P) plays a role. Sphinganine 1-phosphate controls a number of biological processes, including neovascularization, which gives cancer cells oxygen and nutrition, development, and survival of cells, and inflammation, which can promote tumorigenesis[1]. Human renal endothelial cells are stimulated to produce HSP27 and phosphorylated ERK MAPK, Akt, and HSP27 by Sphinganine-1-Phosphate (1 μM)[2].
In vitro, exogenous sphinganine-1-phosphate activates S1P1 and exhibits protective effects against ischemia-reperfusion injury. The compound is used in cell-based assays to study sphingolipid signaling and its effects on cell function. In these assays, cells are treated with sphinganine 1-phosphate at various concentrations (typically 0.1-10 μM) for varying periods, and cell proliferation, survival, migration, and differentiation are assessed. The compound's effects on signaling pathways such as AKT, ERK, and PLC are measured by western blotting or phospho-specific antibodies. In studies of immune regulation, sphinganine 1-phosphate is used to study lymphocyte trafficking and the effects of S1P receptor modulation on immune cell migration. In cancer research, the compound is used to study the role of sphingolipid signaling in tumor cell proliferation, survival, and metastasis. The compound's protective effects against ischemia-reperfusion injury have been demonstrated in in vitro models using cardiomyocytes or endothelial cells. |
| ln Vivo |
In diabetic mice, sphinganine 1-phosphate can improve wound healing[1]. After liver ischemia and reperfusion (IR) injury in rats, sphinganine 1-phosphate protects the kidneys and liver by selectively activating S1P1 receptors and pertussis toxin-sensitive G-proteins, which in turn activates ERK and Akt. After liver IR, sphinganine 1-phosphate (0.1 mg/kg iv just before reperfusion and 0.2 mg/kg sc two hours later) guards against hepatic and renal damage[2].
In vivo, sphinganine 1-phosphate prevents liver and kidney damage following ischemia-reperfusion injury in mice at doses lower than 0.1 and 0.2 mg/kg. The compound's protective effects are thought to be mediated through S1P receptor signaling. In animal models of ischemia-reperfusion injury, the compound is administered prior to the ischemic insult, and markers of tissue damage (e.g., serum ALT, AST, creatinine, BUN) and histopathological changes are assessed. The compound's ability to regulate lymphocyte trafficking suggests potential applications in autoimmune diseases and transplant rejection. In models of cancer, sphinganine 1-phosphate has been studied for its effects on tumor growth and metastasis. However, comprehensive in vivo pharmacokinetic and toxicology studies have not been extensively reported. Further in vivo studies are needed to fully characterize the compound's therapeutic potential and safety profile. The compound's role as an S1P1 antagonist suggests that it may have different effects than S1P agonists, which are used clinically for the treatment of multiple sclerosis. |
| Enzyme Assay |
In vitro receptor binding assays for sphinganine 1-phosphate typically involve the use of S1P receptors. For S1P1 binding assays, membrane preparations from cells expressing S1P1 are incubated with radiolabeled or fluorescently labeled S1P in the presence of varying concentrations of sphinganine 1-phosphate. The binding affinity (IC₅₀ or Ki) is determined from competitive binding curves. For functional assays, cells expressing S1P1 are treated with sphinganine 1-phosphate, and downstream signaling is measured. For example, the activation of G proteins is measured by GTPγS binding assays, and the activation of downstream kinases (e.g., AKT, ERK) is measured by western blotting or by using phospho-specific antibodies. The compound's ability to act as an antagonist is confirmed by measuring its ability to inhibit S1P-induced signaling. Typical assay conditions include incubation at 25-37°C in appropriate buffer systems (pH 7.4), with reaction products measured by scintillation counting, fluorescence, or chemiluminescence.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Human renal endothelial cells or human kidney proximal tubule (HK-2) cells Tested Concentrations: 1 μM Incubation Duration: 2 or 4 hrs (hours) Experimental Results: Induced HSP27 mRNA in cultured human renal endothelial cells. Phosphorylated ERK MAPK and AKT in human renal endothelial cells in a time-dependent manner. Phosphorylated and induced HSP27. In vitro cell-based assays for sphinganine 1-phosphate are performed using various cell lines to study its effects on cell function. Cells are cultured in appropriate medium and treated with sphinganine 1-phosphate at various concentrations (typically 0.1-10 μM) for varying periods (hours to days). Following treatment, cell proliferation is assessed using MTT, CCK-8, or by counting cell numbers. Cell migration is assessed using wound healing or transwell assays. Cell survival is assessed by measuring apoptosis using flow cytometry (Annexin V/PI staining) or by measuring caspase activity. Cell differentiation is assessed by measuring the expression of differentiation markers. The compound's effects on signaling pathways are measured by western blotting or by using phospho-specific antibodies. Each experiment includes appropriate controls (untreated cells, vehicle controls, and positive controls such as S1P) and is performed in triplicate to ensure statistical reliability. The compound is typically dissolved in DMSO as a stock solution and diluted in culture medium to the desired final concentration, with the final DMSO concentration kept below 0.1% to avoid solvent effects. |
| Animal Protocol |
Animal/Disease Models: Male C57BL /6 mice (20-25 g)[2]
Doses: 0.1 mg/kg Route of Administration: Administered iv immediately before reperfusion and 0.2 mg/kg sc 2 h after reperfusion Experimental Results: The plasma level of alanine aminotransferase (ALT) and Creatinine (Cr ) was 80±6 U/L and 0.46±0.05 mg/dL, respectively. The increases in ALT (7474±557 U/L) and Cr (0.55±0.05 mg/dL) were Dramatically suppressed at 24 h after reperfusion in mice treated with 0.1 mg/kg iv before reperfusion and 0.2 mg/kg sc 2 h after reperfusion. In vivo animal experiments with sphinganine 1-phosphate are conducted in mouse models of ischemia-reperfusion injury, cancer, or immune disorders. Typically, 8-12 week old mice are used, and the compound is administered via intravenous injection or intraperitoneal injection at doses ranging from 0.01-1 mg/kg. In models of ischemia-reperfusion injury, the compound is administered prior to the ischemic insult (e.g., renal or hepatic ischemia), and markers of tissue damage are measured. In models of cancer, the compound is administered to tumor-bearing mice, and tumor growth and metastasis are assessed. In models of immune disorders, the compound is administered to study its effects on lymphocyte trafficking and immune function. Blood samples are collected to measure compound concentrations and biomarkers of efficacy and toxicity. At the end of the experiment, animals are euthanized, and tissues are collected for histopathological examination and gene expression analysis. All animal procedures are conducted in accordance with institutional animal care and use committee guidelines, with appropriate sample sizes (typically n=6-10 per group) to ensure statistical power. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of sphinganine 1-phosphate are characteristic of a bioactive lipid. As a polar sphingolipid metabolite with a molecular weight of 381.5 g/mol and a phosphate group, the compound is expected to have limited oral bioavailability. Following intravenous administration, the compound is rapidly distributed to tissues and metabolized through lipid metabolic pathways. The compound is rapidly cleared from circulation, with a half-life of minutes to hours, due to metabolism by lipid phosphatases and other enzymes. The compound's levels are tightly regulated by the balance between synthesis and degradation. The pharmacokinetics of sphinganine 1-phosphate may be influenced by its formulation, with various vehicles affecting its solubility and bioavailability. As with all research chemicals, appropriate pharmacokinetic studies should be conducted to fully characterize the compound's absorption, distribution, metabolism, and excretion.
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| Toxicity/Toxicokinetics |
The toxicological profile of sphinganine 1-phosphate has not been extensively characterized in formal toxicology studies. As an endogenous sphingolipid metabolite, the compound is naturally present in the body and is expected to be relatively non-toxic at physiological concentrations. However, dysregulation of sphingolipid metabolism has been associated with various diseases. In cell-based assays, the compound has been shown to regulate cell proliferation, survival, and migration without causing cytotoxicity at low concentrations. In animal studies, the compound has been administered at doses that protect against ischemia-reperfusion injury without reported overt toxicity. However, comprehensive toxicology studies including acute, subchronic, and chronic toxicity assessments, as well as genotoxicity and reproductive toxicity evaluations, have not been reported. The compound is classified as a research chemical and is not approved for human use. Standard safety precautions should be observed when handling the compound, including the use of appropriate personal protective equipment.
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| References |
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| Additional Infomation |
Sphingosine-1-phosphate is a monophosphate derivative of sphingosine and belongs to the sphingosine class of compounds. It is a mouse metabolite functionally related to sphingosine and is the conjugate acid of sphingosine-1-phosphate (1-). It has been reported that sphingosine-1-phosphate also exists in Homo sapiens, and relevant data are available.
Sphinganine 1-phosphate is a valuable research tool for studying sphingolipid metabolism, immune regulation, vascular biology, and cancer progression. It is a polar sphingolipid metabolite that regulates numerous physiological processes including cell proliferation, survival, differentiation, and migration. The compound acts as an antagonist at the S1P1 receptor. It is an intermediate in the metabolism of glycosphingolipids and sphingolipids. The compound has the molecular formula C₁₈H₄₀NO₅P and a molecular weight of 381.5 g/mol. In research, it is used to investigate sphingolipid metabolism, immune regulation, vascular biology, and cancer progression, providing insights into lipid-mediated cellular communication and disease mechanisms. It is not approved for any clinical indication and is strictly for research use only. Its role as a key sphingolipid signaling molecule makes it an essential tool for studying lipid biology and its implications in health and disease. |
| Molecular Formula |
C18H40NO5P
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|---|---|
| Molecular Weight |
381.49
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| Exact Mass |
381.264
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| CAS # |
19794-97-9
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| Related CAS # |
Sphinganine 1-phosphate-d7;2315262-23-6
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| PubChem CID |
644260
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| Appearance |
White to off-white solid powder
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| Vapour Pressure |
2.66E-14mmHg at 25°C
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| LogP |
4.965
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
25
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| Complexity |
337
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCCCCCCCCCCCCCC[C@H]([C@H](COP(=O)(O)O)N)O
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| InChi Key |
YHEDRJPUIRMZMP-ZWKOTPCHSA-N
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| InChi Code |
InChI=1S/C18H40NO5P/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-18(20)17(19)16-24-25(21,22)23/h17-18,20H,2-16,19H2,1H3,(H2,21,22,23)/t17-,18+/m0/s1
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| Chemical Name |
[(2S,3R)-2-amino-3-hydroxyoctadecyl] dihydrogen phosphate
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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 | 2.6213 mL | 13.1065 mL | 26.2130 mL | |
| 5 mM | 0.5243 mL | 2.6213 mL | 5.2426 mL | |
| 10 mM | 0.2621 mL | 1.3107 mL | 2.6213 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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