1. GPCR/G Protein
  2. Endothelin Receptor
  3. Bosentan (hydrate)

Bosentan (hydrate) 

Cat. No.: HY-A0013A Purity: 99.71%
Handling Instructions

Bosentan hydrate 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 (hydrate) Chemical Structure

Bosentan (hydrate) Chemical Structure

CAS No. : 157212-55-0

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10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
50 mg USD 84 In-stock
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100 mg USD 144 In-stock
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200 mg USD 264 In-stock
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500 mg USD 360 In-stock
Estimated Time of Arrival: December 31
1 g USD 600 In-stock
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5 g USD 960 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Bosentan (hydrate):

Top Publications Citing Use of Products

    Bosentan (hydrate) 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 hydrate 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].

    Clinical Trial
    Molecular Weight

    569.63

    Formula

    C₂₇H₃₁N₅O₇S

    CAS No.

    157212-55-0

    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.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 : ≥ 100 mg/mL (175.55 mM)

    Ethanol : 50 mg/mL (87.78 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7555 mL 8.7776 mL 17.5553 mL
    5 mM 0.3511 mL 1.7555 mL 3.5111 mL
    10 mM 0.1756 mL 0.8778 mL 1.7555 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

    • 5.

      Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.71%

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    Keywords:

    Bosentan (hydrate)Endothelin ReceptorInhibitorinhibitorinhibit

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    Product Name:
    Bosentan (hydrate)
    Cat. No.:
    HY-A0013A
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