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Bosentan-d4

$270

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Products Details

Product 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.

Web ID

– HY-115417

Shipping

– Room temperature

Molecular Formula

– C27H25D4N5O6S

References

– [1]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.|[2]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

CAS Number

– 1065472-77-6

Molecular Weight

– 555.64

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

Clinical Information

– No Development Reported

Research Area

– Cardiovascular Disease; Endocrinology

Solubility

– 10 mM in DMSO

Target

– Endothelin Receptor

Pathway

– GPCR/G Protein

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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