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Bosentan-d4

CAT: 0804-HY-115417Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-115417Size:1 mg
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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.
CAS Number
1065472-77-6
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

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