1. GPCR/G Protein
  2. Endothelin Receptor
  3. Atrasentan

Atrasentan (Synonyms: ABT-627; (+)-A 127722; A-147627)

Cat. No.: HY-15403
Handling Instructions

Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.

For research use only. We do not sell to patients.

Atrasentan Chemical Structure

Atrasentan Chemical Structure

CAS No. : 173937-91-2

Size Price Stock
5 mg USD 216 Ask For Quote & Lead Time
10 mg USD 360 Ask For Quote & Lead Time
50 mg USD 1087 Ask For Quote & Lead Time

* Please select Quantity before adding items.

Other In-stock Forms of Atrasentan:

Other Forms of Atrasentan:

Top Publications Citing Use of Products

    Atrasentan purchased from MCE. Usage Cited in: Department Veterinary Clinical Medicine. University of Illinois. 2015.

    Effects of ET-1 and ABT-627 on the expression levels of pAkt and Akt in serum starved Abrams and HMPOS cells. Increased phosphorylation of Akt in HMPOS cells treated with ET-1 and 10% FBS can be seen visually with darkening of the bands. Cells treated with ABT-627 and the combination of ABT-627 and ET-1 show decreased band weight.

    Atrasentan purchased from MCE. Usage Cited in: J Vet Intern Med. 2015 Nov;29(6):1584-94.

    In the HMPOS cell line, membranous cleavage of bone alkaline phosphatase is reduced following exposure to ABT-627 alone or in combination with endothelin-1.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA[1].

    IC50 & Target

    IC50: 0.055 nM (ETA)

    In Vitro

    Atrasentan (ABT-627, 0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. ABT-627 in conbination with Taxotere elicits a significantly greater loss of viable prostate cancer cells relative to either agent alone and shows greater degree of down-regulation of the NF-κB DNA binding activity[2]. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It is a moderate P-gp inhibitor (IC50 in P388/dx cells=15.1±1.6 μM) and a weak BCRP inhibitor (IC50 in MDCKII-BCRP cells=59.8±11 μM)[3].

    In Vivo

    Atrasentan (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats[1]. Aatrasentan (ABT-627, 10 mg/kg, i.p.) as well as Taxotere alone inhibited the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model[2].

    Clinical Trial
    Molecular Weight

    542.69

    Formula

    C₂₉H₃₈N₂O₆S

    CAS No.

    173937-91-2

    SMILES

    O=C([[email protected]]1[[email protected]](C2=CC=C(OC)C=C2)N(CC(N(CCCC)CCCC)=O)C[[email protected]@H]1C3=CC=C(OCO4)C4=C3)O.[S].[R].[R]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    Kinase Assay
    [2]

    Cells are incubated and treated with Atrasentan. They are then washed twice with PBS and lysed in ice-cold lysis buffer [20 mM Tris (pH 7.4), 150 mM NaCl, 1% Triton X-100, 1 mM EDTA, 1 mM EGTA, 2.5 mM sodium PPi, 1 mM β-glycerophosphate, 1 mM sodium orthovanadate, 1 μg/mL leupeptin, and 1 mM PMSF]. The extracts are centrifuged to remove cellular debris, and the protein content of the supernatants is determined using the bicinchoninic acid (BCA) protein assay reagent. Proteins (150 μg) are incubated with gentle rocking at 4°C overnight with immobilized Akt antibody cross-linked to agarose hydrazide beads. After the Akt is selectively immunoprecipitated from the cell lysates, the immunoprecipitated products are washed twice with lysis buffer and twice with kinase assay buffer [25 mM Tris (pH 7.5), 10 mM MgCl2, 5 mM β-glycerol phosphate, 0.1 mM sodium orthovanadate, 2 mM DTT] and then resuspended in 40 μL of kinase assay buffer containing 200 μM ATP and 1 μg GSK-3α/β fusion protein. The kinase assay reaction is allowed to proceed at 30°C for 30 min and stopped by the addition of Lamelli SDS sample buffer. Reaction products are resolved by 10% SDS-PAGE, followed by Western blotting with antiphosphorylated GSK-3α/β antibody. For analysis of the total amount of Akt, 40 μg of protein from the lysate samples are resolved by 10% SDS-PAGE, followed by Western blotting with anti-Akt antibody.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    All three prostate cancer cell lines (LNCaP, C4-2b, and PC-3 cells) are seeded at a density of 3 × 103 cells per well in 96-well microtiter culture plates. After overnight incubation, the medium is removed and replaced with a fresh medium containing different concentrations of ABT-627 (0-50 μM) diluted from a 10-mM stock. After 72 h of incubation with drug, 20 μL of MTT solution (5 mg/mL in PBS) are added to each well and incubated further for 2 h. Upon termination, the supernatant is aspirated and the MTT formazan formed by metabolically viable cells is dissolved in isopropanol (100 μL). The plates are mixed for 30 min on a gyratory shaker, and the absorbance is measured at 595 nm on a plate reader.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    YM598 (0.3, 1, and 3 mg/kg), atrasentan (0.3, 1, and 3 mg/kg), or 0.5% methyl cellulose as vehicle is orally administered to rats with a dosing cannula. Dosing volume of the test substances and vehicle is set at 5 mL/kg. Approximately 20 min after administration of compounds, the rats are anesthetized with sodium pentobarbital, and then pithed and ventilated 30 min after dosing. Approximately 1 h after oral administration of compounds, big endothelin-1 (1 nmol/kg) is intravenously administered, and blood pressure is measured. In these two experiments, the dose of test compound that cause 50% inhibition (ID50) of the big endothelin-1-induced increase in diastolic blood pressure is determined by linear regression analysis.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    AtrasentanABT-627(+)-A 127722A-147627ABT627ABT 627A147627A 147627Endothelin ReceptorInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product name:
    Atrasentan
    Cat. No.:
    HY-15403
    Quantity:
    MCE Japan Authorized Agent: