Free shipping on all orders over $ 500

Ambrisentan

Cat. No. M1951

Ambrisentan Structure
Size Price Availability Quantity
10mg USD 190 In stock
50mg USD 500 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Ambrisentan is an oral, once-daily endothelin receptor antagonist that is selective for the endothelin type A receptor. Ambrisentan is indicated for the treatment of pulmonary arterial hypertension (PAH). Once daily oral ambrisentan 2.5 to 10 mg/day significantly improved exercise capacity (6-minute walk distance) compared with placebo in two double-blind, multicenter trials (ARIES-1 & ARIES-2). A decrease in dyspnea and a delay in clinical worsening were among the improvements in secondary outcomes generally observed with ambrisentan versus placebo. In ARIES-E, a 2-year extension of ARIES-1 and -2, approved dosages of ambrisentan (5 and 10 mg/day) were associated with a sustained improvement in 6MWD, a generally sustained improvement in dyspnea, and a low risk of clinical worsening and of death. Six months' treatment with ambrisentan 5 mg/day significantly improved 6MWD (primary outcome measure) and dyspnea relative to baseline in an open-label, non-comparative, multicenter study in a diverse population of patients with PAH or non-PAH forms of pulmonary hypertension (ARIES-3 [n = 224]).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 378.42
Formula C22H22N2O4
CAS Number 177036-94-1
Purity >99%
Solubility DMSO 60 mg/mL
Ethanol 20 mg/mL
Storage at -20°C
References

Long-term ambrisentan therapy for the treatment of pulmonary arterial hypertension.
Oudiz RJ, et al. J Am Coll Cardiol. 2009 Nov 17;54(21):1971-81. PMID: 19909879.

Ambrisentan, a non-peptide endothelin receptor antagonist.
Vatter H, et al. Cardiovasc Drug Rev. 2006 Spring;24(1):63-76. PMID: 16939634.

Related Endothelin Receptor Products
Ro-46-2005

Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.

Bosentan

Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.

Bosentan Hydrate

Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.

Macitentan

Macitentan is an orally-active, tissue-targeting dual ET receptor antagonist.

Sitaxsentan sodium

Sitaxsentan (TBC-11251) is an orally active, highly selective antagonist of endothelin A receptors.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ambrisentan supplier, Endothelin Receptor, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.