| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
L-Cystathionine functions as a substrate for the enzymes cystathionine beta-synthase (CBS) and cystathionine gamma-lyase (CTH) in the transsulfuration pathway. It also targets pathways involved in homocysteine metabolism and cellular redox balance.
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| ln Vitro |
L-Cystathionine dihydrochloride protects against homocysteine-induced mitochondria-dependent apoptosis of vascular endothelial cells (HUVECs). It also shows potential for cardiovascular protection by preventing endothelial cell dysfunction.
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| ln Vivo |
In animal studies, cystathionine has been shown to have hepatoprotective activity and may act as a prodrug for cysteine release. When administered subcutaneously to mice (500 mg/kg), cystathionine disappeared rapidly from the blood and was taken up in large amounts by the liver, but did not significantly cross the blood-brain barrier.
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| Enzyme Assay |
Non-cell enzyme kinetic assays are performed using purified recombinant human cystathionine beta-synthase (CBS) or cystathionine gamma-lyase (CTH). For CBS assay, the reaction mixture contains 100 mM HEPES (pH 7.4), 5 mM L-serine, 10 mM L-homocysteine, 0.2 mM pyridoxal phosphate (PLP), and varying concentrations of L-cystathionine (0-500 uM). After incubation at 37degC for 30 minutes, the reaction is stopped by adding 10% trichloroacetic acid. The product, cystathionine, is quantified by HPLC with fluorescent detection after derivatization with o-phthaldialdehyde (OPA) or by LC-MS/MS. For CTH assay, the reaction mixture contains 50 mM potassium phosphate (pH 7.4), 0.1 mM EDTA, 10 mM L-cystathionine, and recombinant CTH. After incubation at 37degC for 15-60 minutes, the production of cysteine and alpha-ketobutyrate is measured spectrophotometrically at 340 nm using lactate dehydrogenase (LDH) and NADH.
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| Cell Assay |
Cellular studies are performed using human umbilical vein endothelial cells (HUVECs) or primary hepatocytes. For protection assays, HUVECs are cultured in endothelial growth medium (EGM-2) at 37degC with 5% CO2. Cells are pretreated with L-cystathionine dihydrochloride at concentrations ranging from 50 to 500 uM for 2-4 hours, then exposed to 0.5-2 mM homocysteine for 24-48 hours to induce apoptosis. Apoptosis is quantified by measuring caspase-3/7 activity using fluorometric substrates, annexin V-FITC/PI double staining analyzed by flow cytometry, or TUNEL staining. Mitochondrial membrane potential (deltaΨm) is assessed using JC-1 or TMRE staining. Cellular glutathione (GSH) and reactive oxygen species (ROS) levels are measured using fluorescent probes including ThiolTracker Violet and DCFH-DA. For hepatocyte studies, primary mouse hepatocytes or HepG2 cells are treated similarly to investigate metabolic conversion of cystathionine to cysteine and glutathione.
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| Animal Protocol |
In vivo pharmacokinetic and metabolic studies of L-cystathionine have been conducted in male mice. Animals receive a subcutaneous injection of L-cystathionine at doses of 50-500 mg/kg body weight. Blood samples are collected via orbital sinus or tail vein at various time points (0, 15, 30, 60, 120, 240 minutes). Plasma is separated and cystathionine concentrations are measured by HPLC or LC-MS/MS. At predetermined intervals, mice are euthanized and tissues including liver, kidney, brain, and muscle are harvested, weighed, and homogenized in perchloric acid. Tissue concentrations of cystathionine, cysteine, and glutathione are determined. For hepatoprotective activity studies, mice receive an intraperitoneal injection of acetaminophen (APAP, 300-500 mg/kg) to induce acute liver injury, followed by L-cystathionine administration at varying doses (50-200 mg/kg IP or IV). Liver function markers (ALT, AST) are measured in serum, and liver sections are examined histologically for necrosis and inflammation.
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| ADME/Pharmacokinetics |
L-cystathionine is a naturally occurring intermediate in the methionine-cysteine transsulfuration pathway. Its pharmacokinetics in mice demonstrates rapid disappearance from blood following administration, with major accumulation in the liver. The compound does not significantly cross the blood-brain barrier, as shown by low brain uptake and lack of accumulation in brain tissue. L-cystathionine is relatively stable in vivo, with little degradation observed in brain tissue. When administered parenterally, the compound is taken up by hepatocytes and converted to cysteine via cystathionine gamma-lyase, which may subsequently be used for glutathione synthesis. The compound has been shown to be an important metabolic intermediate for maintaining intracellular redox balance in sulfur-containing amino acid metabolism.
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| Toxicity/Toxicokinetics |
L-Cystathionine dihydrochloride is an endogenous metabolite with low intrinsic toxicity. As a natural intermediate in amino acid metabolism, it is considered safe for research purposes. The dihydrochloride salt form may cause mild irritation at the injection site. High doses may lead to metabolic disturbances in sulfur-containing amino acid pathways, but no significant acute toxicity has been reported at typical research doses. The compound has shown protective effects against homocysteine-induced endothelial cell apoptosis, indicating a favorable safety profile. Long-term safety studies in animals have not been performed due to its status as a research tool rather than a therapeutic candidate.
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| References | |
| Additional Infomation |
L-Cystathionine dihydrochloride is widely used in biochemical and metabolic research to study amino acid metabolism, enzyme kinetics of cystathionine beta-synthase and gamma-lyase, and disorders related to sulfur-containing amino acids such as homocystinuria. It serves as an important research tool for investigating cardiovascular protection mechanisms, as it protects against homocysteine-induced mitochondrial-dependent apoptosis of vascular endothelial cells. The compound is also used to study the transsulfuration pathway, which is essential for cysteine biosynthesis from methionine via homocysteine in mammalian tissues. L-Cystathionine serves as a key amino acid for studying the metabolic state of sulfur-containing amino acids in various physiological and pathological conditions.
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| Molecular Formula |
C7H16CL2N2O4S
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|---|---|
| Molecular Weight |
295.18
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| Related CAS # |
L-Cystathionine;56-88-2;DL-Cystathionine;535-34-2;DL-Cystathionine-d4;146764-57-0;DL-Cystathionine dihydrochloride;(S)-Cystathionine-d4
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| Appearance |
White to off-white solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O :~125 mg/mL (~423.47 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 | 3.3878 mL | 16.9388 mL | 33.8776 mL | |
| 5 mM | 0.6776 mL | 3.3878 mL | 6.7755 mL | |
| 10 mM | 0.3388 mL | 1.6939 mL | 3.3878 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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