| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Yangambin targets voltage-gated Ca2+ channels and the platelet-activating factor (PAF) receptor. As a calcium channel inhibitor, it reduces intracellular calcium levels in vascular smooth muscle cells, promoting peripheral vasodilation. As a selective PAF receptor antagonist, it inhibits the cardiovascular effects of PAF. Yangambin also exhibits antiallergic activity by inhibiting β-hexosaminidase release and anti-inflammatory properties.
|
|---|---|
| ln Vitro |
In vitro, Yangambin functions as a calcium channel inhibitor, targeting voltage-gated Ca2+ channels. It effectively reduces intracellular calcium levels in vascular smooth muscle cells, promoting peripheral vasodilation. Yangambin exhibits antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and anti-inflammatory activity with an IC50 of 37.4 μM. It is a selective antagonist of the cardiovascular effects of PAF.
|
| ln Vivo |
In vivo, Yangambin has a hypotensive effect, which probably involves the inhibition of Ca2+ influx. It constitutes a potential therapeutic agent in different shock states where abnormal PAF release is supposed to play an important role. The compound also has central nervous system activity. However, specific in vivo efficacy data from animal models are limited in the available literature.
|
| Enzyme Assay |
In vitro enzyme or receptor binding assays for Yangambin involve studying its binding to voltage-gated Ca2+ channels and the PAF receptor. Radioligand binding assays are performed using membrane preparations from cells expressing the PAF receptor or Ca2+ channels. The compound is incubated with a radiolabeled ligand, and the displacement of the ligand is measured to determine the affinity. Calcium flux assays are used to measure the inhibition of Ca2+ influx.
|
| Cell Assay |
In vitro cell-based assays for Yangambin are performed using vascular smooth muscle cells. Cells are treated with the compound, and intracellular calcium levels are measured using fluorescent dyes. The compound's effects on cell viability and function are also assessed. Antiallergic activity is assessed by measuring β-hexosaminidase release from mast cells. Anti-inflammatory activity is measured by assessing cytokine production.
|
| Animal Protocol |
In vivo animal experiments for Yangambin are limited in the available literature. The compound has been shown to have a hypotensive effect in animal models. It has been studied for its potential therapeutic applications in shock states where abnormal PAF release plays a role. However, specific detailed protocols for in vivo studies are not well-documented.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of Yangambin indicate that it has a molecular weight of 446.49 and a molecular formula of C24H30O8. It is a solid powder with a purity of ≥98%. The compound should be stored in a dry, dark place at -20°C for up to 1 year. The chemical name is (1S,3aR,4S,6aR)-1,4-bis(3,4,5-trimethoxyphenyl)-hexahydrofuro[3,4-c]furan.
|
| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for Yangambin are limited. As a natural lignan, it is generally considered safe at moderate doses. However, its safety profile in the context of therapeutic use requires further evaluation. The compound is for research use only and not for human therapeutic use.
|
| References | |
| Additional Infomation |
Yangambin is a lignan. It has been reported in Laurelia novae-zelandiae, Tinospora sinensis, and other organisms with available data.
Other information: Yangambin is a furofuran lignan isolated from various plants. It is a selective PAF receptor antagonist and a calcium channel inhibitor. The compound exhibits antiallergic, anti-inflammatory, and hypotensive activities. Its CAS number is 13060-14-5. |
| Molecular Formula |
C24H30O8
|
|---|---|
| Molecular Weight |
446.490208148956
|
| Exact Mass |
446.194
|
| CAS # |
13060-14-5
|
| PubChem CID |
443028
|
| Appearance |
White to off-white solid powder
|
| Density |
1.183g/cm3
|
| Boiling Point |
556.1ºC at 760 mmHg
|
| Flash Point |
221.1ºC
|
| Vapour Pressure |
7.78E-12mmHg at 25°C
|
| Index of Refraction |
1.537
|
| LogP |
3.813
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
32
|
| Complexity |
512
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
O1C[C@@H]2[C@@H](C3C=C(C(=C(C=3)OC)OC)OC)OC[C@@H]2[C@H]1C1C=C(C(=C(C=1)OC)OC)OC
|
| Synonyms |
(+)-Yangabin; Lirioresinol B, dimethyl-; Yangambin
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.2397 mL | 11.1985 mL | 22.3969 mL | |
| 5 mM | 0.4479 mL | 2.2397 mL | 4.4794 mL | |
| 10 mM | 0.2240 mL | 1.1198 mL | 2.2397 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.