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

Bosentan 

Cat. No.: HY-A0013 Purity: 99.98%
COA 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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Solution
10 mM * 1 mL in DMSO USD 101 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 101 In-stock
Solid
50 mg USD 92 In-stock
100 mg USD 158 In-stock
200 mg USD 264 In-stock
500 mg USD 396 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of Bosentan:

Bosentan Related Antibodies

Top Publications Citing Use of Products

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

    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].

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

    Bosentan Related Antibodies
    In Vivo

    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].

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

    551.61

    Appearance

    Solid

    Formula

    C27H29N5O6S
    CAS No.
    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 : ≥ 100 mg/mL (181.29 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.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 2.75 mg/mL (4.99 mM); Clear solution

    • 2.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.75 mg/mL (4.99 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

    • 4.

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

      Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

    • 5.

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

      Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.98%

    COA (255 KB) RP-HPLC (274 KB) LCMS (265 KB)

    Handling Instructions (2659 KB)
    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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    Bosentan Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    • Molarity Calculator

    • Dilution Calculator

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

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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
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    Keywords:

    Bosentan147536-97-8Endothelin ReceptorInhibitorinhibitorinhibit

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