| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
TLR4 (toll-like receptor 4). Stepharine is a natural alkaloid that directly interacts with TLR4 and binds to the TLR4/MD2 complex, functioning as a TLR4 inhibitor. By inhibiting TLR4 signaling, it suppresses the upregulation of TLR4 expression and downstream inflammatory pathways. Stepharine also exhibits multiple pharmacological activities including anti-aging, anti-viral, anti-hypertensive, antispasmodic, and neuroprotective effects.
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| ln Vitro |
In LPS-activated BV-2 cells, streptomycin (10, 30 μM) significantly reduces the release of nitric oxide (NO) as well as the mRNA and protein expression of pro-inflammatory mediators [inducible nitric oxide synthase, interleukin (IL)-6, tumor necrosis factor (TNF)-α, IL-1β][1]. Stepharine (10, 30 μM) suppresses the upregulation of TLR4 expression, phosphorylation of IκBα, and nuclear translocation of NF-κB p65 produced by LPS[1]. Stepharine has neuroprotective effects on SH-SY5Y cells grown in conditioned media exposed with lipopolysaccharide (LPS). In vitro cholinesterase inhibition has also been demonstrated by stepharine[1].
Stepharine suppresses the upregulation of TLR4 expression, phosphorylation of IκBα, and nuclear translocation of NF-κB p65 produced by LPS at concentrations of 10 and 30 μM. This demonstrates its ability to inhibit TLR4-mediated inflammatory signaling. Stepharine also possesses anti-aging, anti-viral, anti-hypertensive, antispasmodic, and neuroprotective effects. |
| ln Vivo |
In the MCAO ischemic cortex, stepharine (500 μg/kg) prevented the loss of NeuN+ cells and the growth of Iba-1+ cells[1].
In vivo, Stepharine is being studied for its potential in treating neurological disorders such as Parkinson's disease. Its anti-hypertensive, antispasmodic, and neuroprotective effects suggest potential therapeutic applications in cardiovascular and neurological conditions. The compound's ability to inhibit TLR4 signaling may also contribute to its anti-inflammatory effects in vivo. |
| Enzyme Assay |
In vitro binding assays for Stepharine are used to characterize its interaction with TLR4. These assays typically involve surface plasmon resonance or ELISA-based binding studies to measure the compound's direct binding to TLR4 or the TLR4/MD2 complex. Competition assays with known TLR4 ligands can confirm specific binding to the receptor.
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| Cell Assay |
Cellular assays for Stepharine involve treating TLR4-expressing cells (such as macrophages) with the compound and measuring inhibition of LPS-induced inflammatory responses. Readouts include inhibition of TLR4 expression, IκBα phosphorylation, NF-κB nuclear translocation, and pro-inflammatory cytokine production (IL-6, TNF-α, IL-1β). These assays confirm the compound's ability to inhibit TLR4-mediated signaling in a cellular context.
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| Animal Protocol |
Animal/Disease Models: Middle cerebral artery occlusion (MCAO) rat model[1].
Doses: 500 μg/kg ( 20 μL). Route of Administration: Intranasally injected into rats 1h after MCAO. Experimental Results: Attenuated the neuronal loss induced by MCAO (MCAO+ stepharine) group. In vivo efficacy of Stepharine would be evaluated in animal models of inflammation, hypertension, and neurodegenerative diseases. The compound could be administered orally or via injection, and its effects on blood pressure, inflammation, and neuroprotection would be assessed. Its potential for treating Parkinson's disease and other neurological disorders is an area of ongoing research. |
| ADME/Pharmacokinetics |
Stepharine has a molecular formula of C18H19NO3 and a molecular weight of 297.35. It is a natural aporphine alkaloid extracted from Stephania plants. The compound is supplied as a powder. It is for research use only and is not intended for human therapeutic use.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for Stepharine. As a natural alkaloid, its safety profile would be an important consideration. Potential toxicities could be related to its pharmacological effects on TLR4 signaling and other targets. Standard preclinical safety studies would be required to evaluate its safety for potential therapeutic applications.
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| References | |
| Additional Infomation |
According to reports, Stephania yunnanensis, Stephania cephalantha, and other organisms with available data have been found to contain Stephania yunnanensis.
Stepharine (CAS#: 2810-21-1) is a natural aporphine alkaloid extracted from plants of the Stephania genus. It has a molecular formula of C18H19NO3 and a molecular weight of 297.35. Stepharine directly interacts with TLR4 and binds to the TLR4/MD2 complex as a TLR4 inhibitor. It possesses anti-aging, anti-viral, anti-hypertensive, antispasmodic, and neuroprotective effects. It is a research tool and is not approved for clinical use. |
| Molecular Formula |
C18H19NO3
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|---|---|
| Molecular Weight |
297.35
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| Exact Mass |
297.136
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| CAS # |
2810-21-1
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| PubChem CID |
98455
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| Appearance |
Pale purple to purple solid powder
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| Density |
1.27g/cm3
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| Boiling Point |
487.1ºC at 760 mmHg
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| Flash Point |
248.4ºC
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| Vapour Pressure |
1.22E-09mmHg at 25°C
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| Index of Refraction |
1.632
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| LogP |
2.556
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
510
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C2=C3[C@@H](CC24C=CC(=O)C=C4)NCCC3=C1)OC
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| InChi Key |
OGJKMZVUJJYWKO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H19NO3/c1-21-14-9-11-5-8-19-13-10-18(6-3-12(20)4-7-18)16(15(11)13)17(14)22-2/h3-4,6-7,9,13,19H,5,8,10H2,1-2H3
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| Chemical Name |
10,11-dimethoxyspiro[5-azatricyclo[6.3.1.04,12]dodeca-1(12),8,10-triene-2,4'-cyclohexa-2,5-diene]-1'-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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 25 mg/mL (84.08 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 | 3.3630 mL | 16.8152 mL | 33.6304 mL | |
| 5 mM | 0.6726 mL | 3.3630 mL | 6.7261 mL | |
| 10 mM | 0.3363 mL | 1.6815 mL | 3.3630 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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