An ETA receptor antagonist
Related Products
Labeled Version(s)
35558Ambrisentan-d3
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Ambrisentan

Item No. 23669

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αS-[(4,6-dimethyl-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-benzenepropanoic acid
CAS Number
177036-94-1
Molecular Formula
C22H22N2O4
Formula Weight
378.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/mlEthanol: slightly solubleMethanol: slightly soluble
SMILES
CC1=NC(O[C@H](C(O)=O)C(OC)(C2=CC=CC=C2)C3=CC=CC=C3)=NC(C)=C1
InChi Code
InChI=1S/C22H22N2O4/c1-15-14-16(2)24-21(23-15)28-19(20(25)26)22(27-3,17-10-6-4-7-11-17)18-12-8-5-9-13-18/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1
InChi Key
OUJTZYPIHDYQMC-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $36

    Add

    5 mg

    $128

    Add

    10 mg

    $203

    Add
    Product Description

    Ambrisentan is a nonpeptide endothelin A (ETA) receptor antagonist (IC50s = 0.251, 0.316, 0.398, 251, and 630 nM for rat preparations of heart, bladder, kidney, lung, and cerebral cortex, respectively).1 It inhibits contraction of isolated rabbit aortic rings induced by endothelin-1 (ET-1; Item No. 24127) by 43.23% when used at a concentration of 1 µM.2 Ambrisentan inhibits ET-1-induced contraction of human pulmonary and radial arteries in vitro (Kd = 0.042 and 0.11 μM, respectively).3 In a rat model of neonatal hyperoxic lung injury, ambrisentan (20 mg/kg per day, s.c.) reduces pulmonary arterial hypertension (PAH) as well as decreases PAH-induced right ventricular hypertrophy (RVH) and peak RV pressure.4 Formulations containing ambrisentan have been used in the treatment of PAH.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yokoyama, Y., Osano, A., Hyashi, H., et al. Endothelin-1 receptors in rat tissues: Characterization by bosentan, ambrisentan and CI-1020. Biol. Pharm. Bull. 37(3), 461-465 (2014).

    2. Xia, J., Song, J., Zhen, L., et al. Synthesis and in vitro evaluation of ambrisentan analogues as potential endothelin receptor antagonists. Bioorg. Med. Chem. Lett. 21(13), 3894-3897 (2011).

    3. Angus, J.A., Soeding, P.F., Hughes, R.J.A., et al. Functional estimation of endothelin-1 receptor antagonism by bosentan, macitentan and ambrisentan in human pulmonary and radial arteries in vitro. Eur. J. Pharmacol. 804, 111-116 (2017).

    4. Wagenaar, G.T., Laghmani, e.H., de Visser, Y.P., et al. Ambrisentan reduces pulmonary arterial hypertension but does not stimulate alveolar and vascular development in neonatal rats with hyperoxic lung injury. Am. J. Physiol. Lung Cell Mol. Physiol. 304(4), L264-L275 (2013).