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Cat. No. M1951
Ambrisentan Structure

BSF 208075; LU 208075

Size Price Availability Quantity
10mg USD 80 In stock
50mg USD 200 In stock
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Quality Control
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 >98%
Solubility DMSO 60 mg/mL
Ethanol 20 mg/mL
Storage at -20°C

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.

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Keywords: Ambrisentan, BSF 208075; LU 208075 supplier, Endothelin Receptor, inhibitors

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