| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Sparstolonin B targets Toll-like receptors 2 (TLR2) and 4 (TLR4), which are key mediators of innate immune responses. It acts as a selective antagonist of these receptors. By blocking TLR2 and TLR4, it inhibits the inflammatory signaling pathways activated by these receptors, reducing the production of pro-inflammatory cytokines.
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| ln Vitro |
Neuroblastoma cells are inhibited in their growth and viability by sparstolonin B (1–20 µM; 2-4 days) [3]. In mouse macrophages, sparstolonin B suppresses the production of cytokines triggered by TLR ligands. The recruitment of MyD88 to TLR4 and TLR2 is inhibited by sparstolonin B[1]. In neuroblastoma cells, sparstolonin B produces reactive oxygen species (ROS). N-myc expression is decreased in neuroblastoma cells by sparstolonin B [3].
In vitro, sparstolonin B acts as a selective TLR2 and TLR4 antagonist. It inhibits TLR ligand-induced cytokine expression in mouse macrophages. It has anti-HIV and anticancer activities. These activities have been demonstrated in cell-based assays using macrophages and other cell types. |
| ln Vivo |
Sparstolonin B (100 μg/mouse; intraperitoneal injection) can reduce LPS-induced inflammation in mice [1].
In vivo, sparstolonin B has anti-inflammatory and anticancer activities. By blocking TLR2- and TLR4-mediated inflammatory signaling, it may have therapeutic potential for inflammatory and infectious diseases. However, specific details of in vivo efficacy studies are not extensively detailed in the available literature. |
| Enzyme Assay |
The in vitro receptor binding/functional assay for sparstolonin B measures its ability to inhibit TLR2- and TLR4-mediated signaling. These assays typically use cells expressing TLR2 or TLR4 and measure the activation of downstream signaling pathways, such as NF-κB or MAPK, in response to TLR ligands. The compound's inhibitory potency is determined by measuring the reduction in signaling.
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: SH-SY5Y, IMR-32, NGP, SKNF-1 and SK-N-BE(2) Cell Tested Concentrations: 1 µM, 5 µM, 10 µM or 20 µM Incubation Duration: 2- 4-day Experimental Results: 2-day (SH-SY5Y and IMR-32), 3-day (NGP cells), or 4-day (SKNF-1 and SK-N-BE(2) cells) treatment. In vitro cellular assays for sparstolonin B assess its anti-inflammatory effects. Macrophages or other immune cells are treated with sparstolonin B and then stimulated with TLR2 or TLR4 ligands. The production of pro-inflammatory cytokines is measured. These assays demonstrate the compound's ability to inhibit TLR-mediated inflammatory responses. |
| Animal Protocol |
Animal/Disease Models: 5-6 weeks old male C57Bl/6 mice (weight 18-20 g) [1]
Doses: 100 μg/mouse Route of Administration: intraperitoneal (ip) injection Experimental Results: LPS-induced expression levels of TNFα and IL-1β were Dramatically Dramatically reduce sepsis in a mouse model. In vivo animal studies for sparstolonin B have been conducted in models of inflammation and cancer to evaluate its efficacy. However, specific details of these studies are not extensively detailed in the available literature. It is a research compound and is not approved for clinical use. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for sparstolonin B are not extensively detailed in the available literature. As a natural product, its oral bioavailability may be limited. However, its in vivo efficacy suggests that it reaches sufficient systemic concentrations. The compound's pharmacokinetic properties would be important for its development as a therapeutic agent.
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| Toxicity/Toxicokinetics |
Specific toxicity data for sparstolonin B are not extensively detailed in the available literature. As a natural product, it is generally considered to have low toxicity. However, comprehensive toxicological studies would be required to establish its safety profile for therapeutic use. It is intended for research purposes only.
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| References |
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| Additional Infomation |
Sparstolonin B is an isocoumarin natural product that acts as a selective TLR2 and TLR4 antagonist. It has anti-inflammatory, anti-HIV, and anticancer activities. It inhibits TLR ligand-induced cytokine expression. It is a research compound and is not approved for clinical use.
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| Molecular Formula |
C15H8O5
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|---|---|
| Molecular Weight |
268.221024513245
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| Exact Mass |
268.037
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| CAS # |
1259330-61-4
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| PubChem CID |
135659042
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
20
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| Complexity |
622
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C2C=CC(=CC=2C2=COC(=C3C(C=CC1=C23)=O)O)O
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| InChi Key |
KUPDHLFGNQEASI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H8O5/c16-7-1-3-11-8(5-7)9-6-19-15(18)14-10(17)2-4-12(20-11)13(9)14/h1-6,16,18H
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| Chemical Name |
4,14-dihydroxy-8,15-dioxatetracyclo[7.7.1.02,7.013,17]heptadeca-1(16),2(7),3,5,9(17),10,13-heptaen-12-one
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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) |
DMSO : ~10 mg/mL (~37.28 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (18.64 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7283 mL | 18.6414 mL | 37.2828 mL | |
| 5 mM | 0.7457 mL | 3.7283 mL | 7.4566 mL | |
| 10 mM | 0.3728 mL | 1.8641 mL | 3.7283 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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