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Chemical Structure| 157212-55-0 Chemical Structure| 157212-55-0

Structure of Bosentan hydrate
CAS No.: 157212-55-0

Chemical Structure| 157212-55-0

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Bosentan hydrate competitively and dually antagonizes endothelin-1 (ET) for the ETA and ETB receptors, with Ki values of 4.7 nM and 95 nM in human SMC, respectively.

Synonyms: Ro 47-0203; Bosentan(hydrate)

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Product Details of Bosentan hydrate

CAS No. :157212-55-0
Formula : C27H31N5O7S
M.W : 569.63
SMILES Code : O=S(C1=CC=C(C(C)(C)C)C=C1)(NC2=NC(C3=NC=CC=N3)=NC(OCCO)=C2OC4=CC=CC=C4OC)=O.[H]O[H]
Synonyms :
Ro 47-0203; Bosentan(hydrate)
MDL No. :MFCD09751188
InChI Key :SXTRWVVIEPWAKM-UHFFFAOYSA-N
Pubchem ID :185462

Safety of Bosentan hydrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H361
Precautionary Statements:P501-P202-P201-P280-P308+P313-P405

Related Pathways of Bosentan hydrate

GPCR

Isoform Comparison

Biological Activity

Target
  • ET-A

    ET-A, Ki:4.7 nM

  • ET-B

    ET-B, Ki:95 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human Pulmonary Microvascular Endothelial Cells (HPMEC) 10 µM 24 hours To investigate the effect of Bosentan hydrate on MMP19-induced endothelial-to-mesenchymal transition (E(nd)MT), results showed that Bosentan hydrate significantly inhibited MMP19-induced E(nd)MT. PMC10009991

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6N mice Bleomycin (BLM)-induced pulmonary fibrosis model Gastric infusion 100 mg/kg Once daily for 13 days To investigate the effect of Bosentan hydrate on MMP19-induced pulmonary fibrosis, results showed that Bosentan hydrate significantly alleviated MMP19-mediated exacerbation of BLM-induced pulmonary fibrosis. PMC10009991

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.78mL

1.76mL

0.88mL

17.56mL

3.51mL

1.76mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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