| Identification | Back Directory | [Name]
Darusentan | [CAS]
171714-84-4 | [Synonyms]
HMR4005
HMR-4005
HMR 4005
Darusentan
S-Darusentan
darusentan, CID177236
FEJVSJIALLTFRP-LJQANCHMSA-N
LU 135252; LU-135252; LU135252; HMR-4005; HMR 4005; HMR4005; DARUSENTAN
(S)-2-((4,6-dimethoxypyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoic acid
(2S)-2-(4,6-DIMETHOXYPYRIMIDIN-2-YL)OXY-3-METHOXY-3,3-DI(PHENYL)PROPANOIC ACID
Benzenepropanoic acid, α-[(4,6-dimethoxy-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-, (αS)- | [Molecular Formula]
C22H22N2O6 | [MOL File]
171714-84-4.mol | [Molecular Weight]
410.42 |
| Chemical Properties | Back Directory | [Boiling point ]
587.3±60.0 °C(Predicted) | [density ]
1.268±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMF: 10 mg/ml; DMSO: 2 mg/ml; Ethanol: 2 mg/ml; PBS (pH 7.2): insol | [form ]
A solid | [pka]
1.82±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist with Ki of 1.4 nM for ET-A receptor and 184 nM for ET-B receptor , the selectivity of ETA receptors is more than 100 times higher than that of ETB receptors. It competes for binding of radiolabeled endothelin in the membrane of rat aortic vascular smooth muscle cells (RAVSMs) with a Ki of 13 nM. | [in vitro]
Darusentan ((S)-Darusentan) competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a K i =13 nM . In isolated endothelium-denuded rat aortic rings, Darusentan inhibits endothelin-induced vascular contractility with a pA 2 =8.1±0.14. Darusentan ( 0.001-1μM) inhibits ET-1-induced signaling in cultured RAVSMs. | [in vivo]
Darusentan (30 mg/kg per day orally for weeks 3 and 4) reverses aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg per min subcutaneously for 2 and 4 weeks) in male Sprague Dawley rats. < /p> < tr> | Animal Model: | Twenty-four (eight per group) male Sprague Dawley rats weighing 175±200 g | | Dosage: | 30 mg/kg | | Administration: | Administered orally in rat food for weeks 3 and 4 | | Result: | Reversed aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg). | |
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| Company Name: |
LGM Pharma
|
| Tel: |
1-(800)-881-8210 |
| Website: |
www.lgmpharma.com |
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