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.

Price Stock Quantity  
USD 50 In stock
USD 90 In stock
USD 150 In stock
USD 210 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Betulinic acid Chemical Structure

Betulinic acid Chemical Structure
Molecular Weight: 456.7

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Betulinic acid is available in the following compound libraries:

Product Information

  • Compare Topoisomerase Inhibitors
    Compare Topoisomerase Products
  • Research Area

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
LD50
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]
Features

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
Concentrations
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
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80, pH 4, 10 mg/mL
* 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.

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
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

References

[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.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-16)

NCT Number Recruitment Conditions Sponsor
/Collaborators
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
Formula

C30H48O3

CAS No. 472-15-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Chemical Name Lup-20(29)-en-28-oic acid,3-hydroxy-,(3β)-

Research Area

Tech Support & FAQs

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Topoisomerase Products

  • Voreloxin (SNS-595)

    Voreloxin is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.

  • RG2833 (RGFP109)

    RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.

  • PJ34 HCl

    PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

    Features:Water-soluble PARP1/2 inhibitor with >10,000-fold potentcy vs. 3-aminobenzamide (prototypical PARP inhibitor). Potential uses in cardiovascular diseases (stroke, cerebral ischemia, & myocardial ischemia).

  • Doxorubicin (Adriamycin)

    Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.

  • Etoposide

    Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity.

  • Camptothecin

    Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM. Phase 2.

  • Irinotecan

    Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.

    Features:Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.

  • Topotecan HCl

    Topotecan (NSC 609699) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM, respectively.

    Features:Topotecan is a water-soluble derivative of camptothecin.

  • SN-38

    SN-38 is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.

  • Mitoxantrone

    Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively

Recently Viewed Items

Tags: buy Betulinic acid | Betulinic acid supplier | purchase Betulinic acid | Betulinic acid cost | Betulinic acid manufacturer | order Betulinic acid | Betulinic acid distributor
Contact Us