| Size | Price | Stock | Qty |
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| 250mg |
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| 1g |
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| Other Sizes |
| Targets |
iNOS Human Endogenous Metabolite
Chondroitin sulfate does not target a single protein but interacts with multiple ECM components and cell surface receptors. It binds to CD44, a major hyaluronan receptor, modulating cell adhesion and migration. It also interacts with growth factors (e.g., FGF‑2) and cytokines, influencing cell signalling and tissue homeostasis. The sulfate groups are critical for these interactions. Its primary biological role is as a structural component of cartilage, providing resistance to compression, and it has anti‑inflammatory properties by inhibiting NF‑κB signalling in chondrocytes. |
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| ln Vitro |
Chondroitin sulfate sodium (from shark cartilage) is a type of sulfated glycosaminoglycan, a linear polysaccharide composed of repeating disaccharide units composed of uronic acid and N-acetylhexosamine. A variety of pathogens, including parasites, bacteria, and viruses, have been shown to utilize cell surface Chondroitin sulfate chains to attach to and infect host cells [1]. Chondroitin sulfate occurs naturally in the extracellular matrix of connective tissues such as bone, cartilage, skin, ligaments and tendons. Chondroitin sulfate has shown a range of beneficial effects: anti-inflammatory effects, increase in type II collagen and proteoglycans, reduced bone resorption, and a better anabolic/catabolic balance in chondrocytes [2]. A wide range of chondroitin sulfate concentrations (eg, 12.5 to 2000 mg/mL, but usually less than 200 mg/mL) has been used in in vitro studies. Chondroitin suLfate (200 mg/mL) reduces the sensitivity of chondrocytes to single nucleotide polymorphism-induced apoptosis [3]. Chondroitin sulfate can reduce inflammatory mediators and apoptotic processes, and can reduce the protein production of inflammatory cytokines, iNOS, and MMPs [4].
In vitro, chondroitin sulfate sodium stimulates the synthesis of proteoglycans and collagen type II in cultured human chondrocytes, promoting cartilage repair. At concentrations of 10‑100 µg/mL, it reduces the production of matrix metalloproteinases (MMP‑3, MMP‑13) and pro‑inflammatory cytokines (IL‑1β, TNF‑α) in IL‑1β‑stimulated chondrocytes. It also inhibits the activity of the enzyme ADAMTS‑5 (aggrecanase) in cell‑free assays, with an IC₅₀ of ~50 µg/mL. It does not affect cell proliferation at doses up to 500 µg/mL. |
| ln Vivo |
The high content of chordoriin sulfate in the aggregated protein plays an important role in enabling cartilage to resist tensile stress under various loading conditions, providing resistance and elasticity to the tissue. Studies have shown that chordoriin sulfate interferes with the progression of structural changes in joint tissue and is used to treat patients with osteoarthritis [3]. Chondroitin sulfate is mainly administered orally at a dose of 800 to 1200 mg/day. Chondroitin sulfate is rapidly absorbed from the gastrointestinal tract. The absorbed chordoriin sulfate reaches the blood compartment in the form of 10% chordoriin sulfate and 90% depolymerized low molecular weight derivatives [5].
In vivo, oral administration of chondroitin sulfate (300‑1200 mg/day in humans) has demonstrated moderate efficacy in reducing pain and improving joint function in osteoarthritis. In animal models (rodents, dogs), intra‑articular or oral administration reduces cartilage degradation and synovitis. In a guinea pig osteoarthritis model, oral dosing at 100 mg/kg/day reduces the histological severity of cartilage lesions by approximately 30‑40% over 3 months. Its slow absorption and accumulation in joint tissues are key to its effect. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays: competitive binding to CD44 can be assayed by immobilising recombinant CD44 on ELISA plates, adding chondroitin sulfate (0.1‑1000 µg/mL) and biotinylated hyaluronan, then detecting with streptavidin‑HRP. IC₅₀ for displacement is typically 10‑50 µg/mL. For ADAMTS‑5 inhibition, the enzyme (10 nM) is incubated with aggrecan substrate and chondroitin sulfate (1‑500 µg/mL), and released GAG fragments are quantified by DMMB (dimethylmethylene blue) staining. Inhibition is expressed as % of control.
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| Cell Assay |
Cell‑based assays: primary human chondrocytes are cultured in monolayer or alginate beads. Cells are treated with chondroitin sulfate (10‑200 µg/mL) for 24‑72 h, with or without IL‑1β (10 ng/mL). Supernatants are collected for cytokine ELISA (IL‑6, IL‑8), and RNA is extracted for qPCR analysis of collagen II, aggrecan, and MMP‑13. Cell viability is confirmed by Live/Dead staining. The compound shows anti‑catabolic and anti‑inflammatory effects at ≥50 µg/mL.
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| Animal Protocol |
In vivo animal studies: male Dunkin‑Hartley guinea pigs (spontaneous osteoarthritis model) are given chondroitin sulfate sodium in drinking water (100 mg/kg/day) for 10 weeks. After sacrifice, knee joints are dissected, and cartilage is stained with safranin O and graded using the OARSI scoring system. Blood samples are collected for serum biomarker analysis (CTX‑II). For pharmacokinetic studies, rats are gavaged with 500 mg/kg of the compound, and blood is drawn at 0‑48 h for GAG analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetics in humans: chondroitin sulfate has a low oral bioavailability of 10‑20% due to its high molecular weight (~10‑50 kDa). After oral administration, it is partially absorbed via the intestinal paracellular route, reaching plasma peak concentrations (Cmax ~2‑4 µg/mL) at 3‑4 h post‑dose. The half‑life is ~5‑8 h. It accumulates in joint tissues (synovium, cartilage) over several weeks. The compound is metabolised by desulfation and depolymerisation, and excreted in urine. There is no significant drug interaction.
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| Toxicity/Toxicokinetics |
Toxicology: chondroitin sulfate sodium has an excellent safety profile. In animal studies, the oral LD₅₀ is >5000 mg/kg. No mutagenicity, carcinogenicity, or reproductive toxicity has been observed. Adverse effects in humans are mild and rare, mainly gastrointestinal upset (nausea, diarrhoea) at high doses (>2 g/day). It is considered a safe dietary supplement; no significant drug interactions are noted, though it may have a mild anticoagulant effect at very high doses, similar to heparins.
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| References |
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| Additional Infomation |
Additional information: Chondroitin sulfate sodium (CAS 9082‑07‑9) from shark cartilage is a pharmaceutical‑grade supplement, approved in many countries for osteoarthritis (e.g., in the EU as a prescription drug, in the US as a dietary supplement). Its efficacy remains debated, with meta‑analyses showing modest benefit, particularly when combined with glucosamine. The compound is a white to off‑white powder, highly soluble in water. It is stable at room temperature. It is also used in ophthalmic solutions and wound dressings. The shark origin raises sustainability issues, leading to interest in biosynthetic alternatives.
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| Exact Mass |
1525.09
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|---|---|
| CAS # |
9082-07-9
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| Appearance |
White to off-white solid powder
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| Density |
1.94g/cm3
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| SMILES |
[C@H]1(O[C@@H]([C@@H](O)[C@H](O[C@H]2[C@H](O)[C@H]([C@H](O[C@@H]3O[C@@H]([C@@H](O)[C@H](O[*])[C@H]3NC(=O)C)COS([O-])(=O)=O)[C@@H](C([O-])=O)O2)O)[C@H]1NC(=O)C)COS([O-])(=O)=O)O[C@H]1[C@H](O)[C@H]([C@H](O[C@H]2[C@H](O)[C@H](O[C@@H](O[C@H]3[C@H](O)[C@H]([C@H](O[*])O[C@@H]3C([O-])=O)O)[C@@H]2NC(=O)C)COS([O-])(=O)=O)O[C@@H]1C([O-])=O)O.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]
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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 and light. |
| 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 :~50 mg/mL (with sonication)
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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.) |
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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