Betulinic acid

Catalog No.S3603

Betulinic acid, a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Phase 1/2.

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Betulinic acid Chemical Structure

Betulinic acid Chemical Structure
Molecular Weight: 456.7

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Betulinic acid, a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Phase 1/2.
Targets HIV-1 [1] Eukaryotic topoisomerase I [3] Aminopeptidase N [2]
IC50 1.4 μM(EC50) 5 μM 7.3 μM
In vitro Betulinic acid shows anti-HIV activity by blocking HIV replication in H9 lymphocytes with an EC50 value of 1.4 μM and inhibiting uninfected H9 cell growth with an IC50 value of 13 μM. [1] Betulinic acid also acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 μM. [2] In addition, Betulinic acid inhibits eukaryotic topoisomerase I activity with IC50 of 5 μM and can be exploited as a strong candidate for anti-tumor drug. [3]
In vivo Betulinic acid inhibits prostate cancer cell and tumor (xenograft) growth in athymic nude mice bearing LNCaP cells and this is due, in part, to proteasome-dependent downregulation of Sp1, Sp3, Sp4 and several Sp-regulated genes. [4]

Protocol(Only for Reference)

Kinase Assay: [3]

Topoisomerase I-DNA interaction Annealed 25-mer duplex of oligonucleotide-1 and oligonicleotide-2 is incubated with 25 or 50 units of rat liver topoisomerase I at 8 °C for 15 min in the presence or absence of betulinic acid in binding buffer. After incubation the reaction mixtures are electrophoresed in 7% non-denaturing polyacrylamide gel at 4 °C in 0.167 × TBE buffer and DNA bands are stained with ethidium bromid

Cell Assay: [1]

Cell lines H9 lymphocytes
Incubation Time 3 days
Method H9 lymphocytes ( 1 × 107 cells/ml) are incubated in the presence or absence of HIV-1 (IIIB isolate) for 1 h at 37 °C. Cells are washed thoroughly to remove unadsorbed virions and resuspended in culture medium. Betulinic acid (diluted in test medium) is added to the culture medium. After incubation for 3 days at 37 °C, the cell densities of uninfected cultures are determined to assess toxicity of betulinic acid. A p24 antigen capture assay is used to determine the level of HIV infection in HIV-treated culture

Animal Study: [4]

Animal Models LNCaP tumor xenograft model
Formulation Diluted in corn oil containing 1% DMSO
Dosages 10 and 20 mg/kg/d
Administration Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Fujioka T, et al. J Nat Prod, 1994, 57(2), 243-247.

[2] Melzig MF, et al. Planta Med, 1998, 64(7), 655-657.

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Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT00346502 Suspended Dysplastic Nevus Syndrome University of Illinois at Chicago January 2006 Phase 1|Phase 2

Chemical Information

Download Betulinic acid SDF
Molecular Weight (MW) 456.7


CAS No. 472-15-1
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms ALS-357
Solubility (25°C) * In vitro DMSO 20 mg/mL (43.79 mM)
Ethanol 10 mg/mL (21.89 mM)
Water <1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Lup-20(29)-en-28-oic acid, 3-hydroxy-, (3β)-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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