Darusentan

ChemicalBook > CAS DataBase List > Darusentan

Product Name: Darusentan
CAS No.: 171714-84-4
Chemical Name: Darusentan
Synonyms: HMR4005;HMR-4005;HMR 4005;Darusentan;S-Darusentan;darusentan, CID177236;Darusentan, 10 mM in DMSO;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
CBNumber: CB42485038
Molecular Formula: C22H22N2O6
Formula Weight: 410.42
MOL File: 171714-84-4.mol

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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

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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.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0006252
Product name: Darusentan
Purity: 98.66%
Packaging: 10mg
Price: $220
Updated: 2021/12/16

AK Scientific

Product number: 1783CB
Product name: Darusentan
Packaging: 100mg
Price: $278
Updated: 2021/12/16

ChemScene

Product number: CS-0006252
Product name: Darusentan
Purity: 98.66%
Packaging: 5mg
Price: $130
Updated: 2021/12/16

AK Scientific

Product number: 1783CB
Product name: Darusentan
Packaging: 10mg
Price: $159
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: APO0001331
Product name: DARUSENTAN
Purity: 95.00%
Packaging: 1MG
Price: $593.04
Updated: 2021/12/16

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Darusentan Chemical Properties,Usage,Production

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>

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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).

Darusentan Preparation Products And Raw materials

Raw materials

Preparation Products

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171714-84-4, DarusentanRelated Search:

Amlodipine Levetiracetam Lercanidipine

S-Darusentan

HMR 4005

HMR4005

HMR-4005

LU 135252; LU-135252; LU135252; HMR-4005; HMR 4005; HMR4005; DARUSENTAN

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

darusentan, CID177236

FEJVSJIALLTFRP-LJQANCHMSA-N

Benzenepropanoic acid, α-[(4,6-dimethoxy-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-, (αS)-

vascular,ET-A,Darusentan,Endothelin Receptor,rat,muscle,Inhibitor,Lu 135252,receptor,aortic,endothelin,inhibit,smooth,RAVSMs,Lu135252

Darusentan, 10 mM in DMSO

171714-84-4