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Betulin Fatty Acid Synthase inhibitor

Name: Betulin
Brand: Selleck Chemicals
SKU: S4754
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S4754

Betulin (BE, betulinol, betuline, betulinic alcohol), also known as betulinol, betuline, or betulinic alcohol, is a pentacyclic lupane-type triterpenoid naturally distributed in many plants and displays a broad spectrum of biological and pharmacological properties such as anticancer and chemopreventive activity. This compound (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line.

Chemical Structure

Molecular Weight: 442.72

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Quality Control

Batch: Purity: 99.51%

99.51

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Fatty Acid Synthase Inhibitors	Denifanstat (TVB-2640) TVB-3664 FT113 Fatostatin C75 C75 trans Desoxyrhaponticin trans-Chalcone IPI-9119 Eicosapentaenoic acid ethyl ester

Solubility

In vitro
Batch:

DMSO : 7 mg/mL (15.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.175mg/ml (0.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.175mg/ml (0.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	442.72	Formula	C₃₀H₅₀O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	473-98-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	betulinol, betuline, betulinic alcohol			Smiles	CC(=C)C1CCC2(C1C3CCC4C5(CCC(C(C5CCC4(C3(CC2)C)C)(C)C)O)C)CO

Mechanism of Action

In vitro	Betulin significantly inhibits cell viability in cervix carcinoma HeLa cells, hepatoma HepG2 cells, lung adenocarcinoma A549 cells, and breast cancer MCF-7 cells with IC50 values ranging from 10 to 15 mg/mL. While this compound exhibits only moderate anticancer activity in other human cancer cells such as hepatoma SK-HEP-1 cells, prostate carcinoma PC-3, and lung carcinoma NCI-H460, with IC50 values ranging from 20 to 60 mg/mL, it shows minor growth inhibition in human erythroleukemia K562 cells (IC50>100 mg/mL). This compound does not directly trigger mitochondrial cytochrome c release in isolated mitochondria. Bax and Bak are rapidly translocated to the mitochondria 30 min after betulin treatment. In vitro, it inhibits LPS-induced tumor necrosis factor α (TNF-α) and (interleukin) IL-6 levels and up-regulates the level of IL-10. Also this chemical suppresses the phosphorylation of nuclear factor-kB (NF-kB) p65 protein in LPS-stimulated RAW 264.7 cells.
In vivo	In vivo, Betulin alleviates LPS-induced acute lung injury. Treatment with this compound diminishes pro-inflammatory cytokines, myeloperoxidase activity and bacterial loads in lung tissue during gramnegative pneumonia. In HFD-fed apoE^−/− mice, this compound administration significantly reduces lesions in en face aortas and aortic sinuses. Furthermore, this compound administration significantly increases ABCA1 expression and suppresses macrophage positive areas in the aortic sinuses. Moreover, this compound administration improves plasma lipid profiles and enhances fecal cholesterol excretion in the mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20564340/ [2] https://pubmed.ncbi.nlm.nih.gov/25173422/ [3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5057233/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01657292	Completed	Burns	Birken AG\|Amryt Pharma	August 2012	Phase 3

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