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

Bosentan 

Cat. No.: HY-A0013 Purity: 99.69%
Handling Instructions

Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.

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

Bosentan Chemical Structure

Bosentan Chemical Structure

CAS No. : 147536-97-8

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10 mM * 1 mL in DMSO USD 92 In-stock
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100 mg USD 144 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Bosentan:

Top Publications Citing Use of Products

    Bosentan purchased from MCE. Usage Cited in: Phytomedicine. 2019 Mar 15;56:175-182.

    Representative Western blots for P-gp、BCRP、MRP2 in LS-180 treated with six active compounds in liquorice. C: control, P-1: Rifampicin, P-2: Bosentan, S-1: Liquiritin, S-2: Liquiritigenin, S-3: Isoliquiritin, S-4: Isoliquiritigenin, S-5: Glycyrrhetinic acid, S-6: Licochalcone A.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.

    IC50 & Target

    Ki: 4.7 nM (ETA receptor, in human SMC), 95 nM (ETA receptor, in human SMC)[1]

    In Vitro

    Bosentan (BOS) competitively and specifically antagonizes binding of 125I-labelled ET-1 to ETA receptors on human smooth muscle cells (SMC) and ETB receptors on human placenta cells. The in vitro binding affinity of Bosentan to ETA receptors on human SMC is 4.7 nM and to ETB receptors on human SMC or placenta cells is 41 or 95 nM. Bosentan has 67-fold greater selectivity for ETA than ETB receptors (mean IC50=7.1 vs 474.8 nM) in an in vitro 125I-labeling assay[1].

    In Vivo

    Single-dose Bosentan 62.5 mg significantly (p<0.01 vs baseline) plasma ET-1 levels by 2-fold in 7 pts with WHO class II or III idiopathic or CTD-associated PAH, with peak levels achieved at 8 h[1]. In hypertensive rats, Macitentan 30 mg/kg further decreases mean arterial blood pressure (MAP) by 19 mm Hg when given on top of Bosentan 100 mg/kg. Conversely, Bosentan given on top of Macitentan fails to induce an additional MAP decrease. In pulmonary hypertensive rats, Macitentan 30 mg/kg further decreases mean pulmonary artery pressure (MPAP) by 4 mm Hg on top of Bosentan, whereas a maximal effective dose of Bosentan given on top of Macitentan does not cause any additional MPAP decrease[3].

    Molecular Weight

    551.61

    Formula

    C₂₇H₂₉N₅O₆S

    CAS No.

    147536-97-8

    SMILES

    O=S(NC1=NC(C2=NC=CC=N2)=NC(OCCO)=C1OC3=CC=CC=C3OC)(C4=CC=C(C(C)(C)C)C=C4)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 275 mg/mL (498.54 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8129 mL 9.0644 mL 18.1287 mL
    5 mM 0.3626 mL 1.8129 mL 3.6258 mL
    10 mM 0.1813 mL 0.9064 mL 1.8129 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Bosentan is prepared fresh every day as a suspension in 5% gum arabic[4].

    References
    Cell Assay
    [2]

    Cell viability is evaluated by the trypan blue exclusion test. Human dermal fibroblasts are treated with the indicated concentration of Bosentan (10, 20 and 40 μM). Cell viability is examined at 24 and 48 hours. Stained (dead) and unstained (viable) cells are counted with a hematocytometer[2].

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

    Animal Administration
    [3]

    Rats[3]
    Two-month-old DSS rats and two-month-old Wistar rats are used. Pharmacological effects on mean arterial pressure (MAP) or mean pulmonary arterial pressure (MPAP) and heart rate (HR) are measured up to 120 h after a single gavage at doses ranging from 0.1 to 100 mg/kg (Macitentan) or 3 to 600 mg/kg (Bosentan). To determine whether Macitentan can provide superior pharmacological activity vs. Bosentan, a study is designed in which: 1) Macitentan is administered on top of the maximal effective dose of Bosentan established by the dose-response curve. 2) the same dose of Bosentan is administered on top of the maximal effective dose of Macitentan. The maximal effective dose of the second compound is administered at Tmax of the first tested compound.

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

    References
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    Product Name:
    Bosentan
    Cat. No.:
    HY-A0013
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