| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Betulin targets various molecular targets involved in inflammation, viral replication, and cancer cell survival. It inhibits pro-inflammatory cytokine expression and NF-κB signaling activation through STAT3 signaling. Betulin exhibits anti-malarial, anti-inflammatory, and anti-HIV activity. Its nanoparticles powder shows an excellent hypoglycemic effect compared with raw Betulin. Betulin's multi-targeted mechanism makes it a valuable compound for studying triterpenoid pharmacology.
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| ln Vitro |
Among the many biological and pharmacological characteristics of betulin (BE), its anticancer and chemopreventive actions have garnered a lot of interest. It has been demonstrated that BE inhibits phospholipid growth to produce anti-cancer effects. With IC50 values ranging from 2.8 to 3.4 μM, consistent with established significantly reduced compared to the cell lines, BE was found to exhibit quite different antiproliferative activities depending on the type of cell, ranging from a weak inhibition of cell proliferation of a human erythroid cell line (K562) to a strong inhibition of human neuroblastoma (SK-N-AS). Moreover, significant toxicity was also observed in primary liver cancer cultures isolated from specimen tumors of patients with ovarian cancer, cervical cancer, and astroblastoma. The cytotoxic activity of human (EPG85-257) and human pancreatic cancer (EPP85-181) drug-sensitive and complementary (daunorubicin and mitoxantrone) cell lines was compared using crude birch bark extract, contracted betulin, and betulinic acid [1]. Depending on the molecule utilized, there are notable changes between cell lines per se, indicating that both betulinic acid and betulinic acid may be considered potential leads for the treatment of cancer [2].
In vitro, betulin exhibits anti-malarial, anti-inflammatory, and anti-HIV activity, as well as cytotoxicity towards a number of tumor cell lines. It alleviated LPS-induced acute lung injury in cell-based models. Betulin inhibited pro-inflammatory cytokine expression and NF-κB signaling activation through STAT3 signaling. In cell-based assays, betulin treatment results in reduced inflammation, inhibition of viral replication, and induction of apoptosis in cancer cells. These studies confirm the compound's diverse pharmacological activities. |
| ln Vivo |
Betulin dramatically changed basic learning performance and improved intolerance. Bentolin treatment dramatically decreased the amount of MDA in the hippocampal tissue and increased SOD activity. Additionally, betulin markedly lowered the hippocampal and serum levels of inflammatory cytokines. Furthermore, BE treatment successfully inhibited NF-κB and IκB phosphorylation while upregulating the levels of Nrf2 and HO-1. In conclusion, BE may prevent STZ-induced diabetic rats' cognitive deterioration by loading HO-1/Nrf-2/NF-κB [3].
In vivo, betulin has been studied for its anti-inflammatory, anti-diabetic, and anti-cancer activities. Its nanoparticles powder shows an excellent hypoglycemic effect compared with raw Betulin. Betulin alleviated LPS-induced acute lung injury. It exhibits anti-malarial activity. However, detailed in vivo efficacy data are limited. Betulin is a natural product used as a precursor for betulinic acid and other bioactive compounds. Comprehensive in vivo studies are ongoing. |
| Enzyme Assay |
In vitro enzyme assays for betulin involve measuring its anti-inflammatory activity by assessing the inhibition of pro-inflammatory cytokine production or NF-κB activation. The compound's antioxidant activity is assessed using DPPH or ABTS assays. Its anti-HIV activity is assessed using HIV replication assays. Cytotoxicity towards tumor cell lines is assessed using MTT or CellTiter-Glo assays. These assays confirm the compound's multi-targeted mechanism.
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| Cell Assay |
In vitro cell-based assays for betulin evaluate its anti-inflammatory, anti-cancer, and anti-viral activities. Cells such as macrophages, cancer cells, and HIV-infected cells are cultured and treated with betulin. Inflammatory responses are evaluated by measuring cytokine production. Cancer cell viability and apoptosis are assessed using MTT or flow cytometry. Anti-viral activity is assessed by measuring viral replication. These assays confirm the compound's functional activity.
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| Animal Protocol |
In vivo animal experiments for betulin have been conducted in models of acute lung injury, diabetes, and cancer. Animals are treated with betulin, and inflammatory markers, blood glucose levels, and tumor growth are assessed. The compound's nanoparticles powder shows an excellent hypoglycemic effect. Pharmacokinetic studies are conducted to determine the compound's absorption, distribution, metabolism, and excretion. Comprehensive in vivo studies are ongoing.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for betulin are limited. The compound has a molecular weight of 442.7 g/mol and is a triterpene with low water solubility. It is commonly isolated from birch bark. The compound's metabolic stability, half-life, and bioavailability have not been fully characterized. Nanoparticle formulations may improve its bioavailability.
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| Toxicity/Toxicokinetics |
The toxicity profile of betulin has not been extensively characterized. As a natural triterpene, it is generally considered to have low toxicity. However, the compound should be handled with appropriate safety precautions in the laboratory. For research use only, not for human therapeutic use without proper authorization. Comprehensive toxicological studies are needed.
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| References | |
| Additional Infomation |
Betulin is a pentacyclic triterpenoid belonging to the lupinane family, with a double bond at position 20(29) and substituents of 3β-hydroxyl and 28-hydroxymethyl. It possesses a variety of activities, including as a metabolite, antiviral agent, analgesic, anti-inflammatory agent, and antitumor agent. Betulin is a pentacyclic triterpenoid and also a diol. It is derived from the hydride of lupinane. Betulin has been reported to be found in Acanthus ilicifolius, Bowdichia virgilioides, and several other organisms with relevant data.
Betulin is an abundant, naturally occurring triterpene isolated from birch bark. It exhibits anti-malarial, anti-inflammatory, and anti-HIV activity. Betulin alleviated LPS-induced acute lung injury and inhibited NF-κB signaling. Its nanoparticles show an excellent hypoglycemic effect. Betulin is a precursor for betulinic acid and other bioactive compounds. It is a research tool and has not progressed to clinical trials. |
| Molecular Formula |
C30H50O2
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|---|---|
| Molecular Weight |
442.72
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| Exact Mass |
442.381
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| CAS # |
473-98-3
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| PubChem CID |
72326
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
522.3±23.0 °C at 760 mmHg
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| Melting Point |
256-257 °C(lit.)
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| Flash Point |
210.9±17.2 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.525
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| LogP |
9.01
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
32
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| Complexity |
786
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| Defined Atom Stereocenter Count |
10
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| SMILES |
CC(=C)[C@@H]1CC[C@]2([C@H]1[C@H]3CC[C@@H]4[C@]5(CC[C@@H](C([C@@H]5CC[C@]4([C@@]3(CC2)C)C)(C)C)O)C)CO
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| InChi Key |
FVWJYYTZTCVBKE-ROUWMTJPSA-N
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| InChi Code |
InChI=1S/C30H50O2/c1-19(2)20-10-15-30(18-31)17-16-28(6)21(25(20)30)8-9-23-27(5)13-12-24(32)26(3,4)22(27)11-14-29(23,28)7/h20-25,31-32H,1,8-18H2,2-7H3/t20-,21+,22-,23+,24-,25+,27-,28+,29+,30+/m0/s1
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| Chemical Name |
Lup-20(29)-ene-3β,28-diol
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| Synonyms |
TrocholBetulinAI3-62999 BetulolBetulinolBetuline
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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 : ~3.33 mg/mL (~7.52 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.2 mg/mL (0.45 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.2 mg/mL (0.45 mM) (saturation unknown) in 5% DMSO + 95% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. View More
Solubility in Formulation 3: 3 mg/mL (6.78 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2588 mL | 11.2938 mL | 22.5876 mL | |
| 5 mM | 0.4518 mL | 2.2588 mL | 4.5175 mL | |
| 10 mM | 0.2259 mL | 1.1294 mL | 2.2588 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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