Bosentan-d4

• Description :

  Bosentan-d4 is the deuterium labeled Bosentan. 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.

• UNSPSC :

  12352005

• Hazard Statement :

  H302

• Target :

  Endothelin Receptor

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein

• Field of Research :

  Cardiovascular Disease; Endocrinology

• Solubility :

  10 mM in DMSO

• Smiles :

  O=S(C1=CC=C(C(C)(C)C)C=C1)(NC2=NC(C3=NC=CC=N3)=NC(OC([2H])([2H])C([2H])([2H])O)=C2OC4=CC=CC=C4OC)=O

• Molecular Formula :

  C27H25D4N5O6S

• Molecular Weight :

  555.64

• Precautions :

  P264-P270-P330-P501

• References & Citations :

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]Dhillon S, et al. Bosentan: a review of its use in the management of mildly symptomatic pulmonary arterial hypertension. Am J Cardiovasc Drugs. 2009;9 (5) :331-50.; Akamata K, et al. Bosentan reverses the pro-fibrotic phenotype of systemic sclerosis dermal fibroblasts via increasing DNA binding ability of transcription factor Fli1. Arthritis Res Ther. 2014 Apr 3;16 (2) :R86.; Iglarz M, et al. Comparison of pharmacological activity of macitentan and bosentan in preclinical models of systemic and pulmonary hypertension. Life Sci. 2014 Nov 24;118 (2) :333-9.; Son GY, et al. Endothelin Regulates Porphyromonas gingivalis-Induced Production of Inflammatory Cytokines. PLoS One. 2016 Dec 28;11 (12) :e0167713.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• CAS Number :

  [1065472-77-6]