Darusentan
- Product Name
- Darusentan
- CAS No.
- 171714-84-4
- Chemical Name
- Darusentan
- Synonyms
- HMR4005;HMR-4005;HMR 4005;Darusentan;S-Darusentan;Lu-135252 ，S0017;darusentan, CID177236;Darusentan, 10 mM in DMSO;FEJVSJIALLTFRP-LJQANCHMSA-N;LU 135252; LU-135252; LU135252; HMR-4005; HMR 4005; HMR4005; DARUSENTAN
- CBNumber
- CB42485038
- Molecular Formula
- C22H22N2O6
- Formula Weight
- 410.42
- MOL File
- 171714-84-4.mol
Darusentan Property
- Boiling point:
- 587.3±60.0 °C(Predicted)
- Density
- 1.268±0.06 g/cm3(Predicted)
- storage temp.
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0006252
- Product name
- Darusentan
- Purity
- 98.66%
- Packaging
- 10mg
- Price
- $220
- Updated
- 2021/12/16
- Product number
- 1783CB
- Product name
- Darusentan
- Packaging
- 100mg
- Price
- $278
- Updated
- 2021/12/16
- Product number
- CS-0006252
- Product name
- Darusentan
- Purity
- 98.66%
- Packaging
- 5mg
- Price
- $130
- Updated
- 2021/12/16
- Product number
- 1783CB
- Product name
- Darusentan
- Packaging
- 10mg
- Price
- $159
- Updated
- 2021/12/16
- Product number
- APO0001331
- Product name
- DARUSENTAN
- Purity
- 95.00%
- Packaging
- 1MG
- Price
- $593.04
- Updated
- 2021/12/16
Darusentan Chemical Properties,Usage,Production
Uses
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors[1]. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM[2].
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>
| 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). |
References
[1] Frank Enseleit, et al. Darusentan, a selective endothelin A receptor antagonist, for the oral treatment of resistant hypertension. Ther Adv Cardiovasc Dis. 2010 Aug;4(4):231-40. DOI:10.1177/1753944710373785
[2] Liang F, et al. Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries. Can J Physiol Pharmacol. 2010 Aug;88(8):840-9. DOI:10.1139/Y10-061
[3] H H Dao, et al. Norepinephrine-induced aortic hyperplasia and extracellular matrix deposition are endothelin-dependent. J Hypertens. 2001 Nov;19(11):1965-73. DOI:10.1097/00004872-200111000-00006
Darusentan Preparation Products And Raw materials
Raw materials
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