Darusentan
- CAS No.
- 171714-84-4
- Chemical Name:
- Darusentan
- 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
- CBNumber:
- CB42485038
- Molecular Formula:
- C22H22N2O6
- Molecular Weight:
- 410.42
- MDL Number:
- MOL File:
- 171714-84-4.mol
| 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 |
| FDA UNII | 33JD57L6RW |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
Darusentan price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0006252 | Darusentan 98.66% | 171714-84-4 | 10mg | $220 | 2021-12-16 | Buy |
| AK Scientific | 1783CB | Darusentan | 171714-84-4 | 100mg | $278 | 2021-12-16 | Buy |
| ChemScene | CS-0006252 | Darusentan 98.66% | 171714-84-4 | 5mg | $130 | 2021-12-16 | Buy |
| AK Scientific | 1783CB | Darusentan | 171714-84-4 | 10mg | $159 | 2021-12-16 | Buy |
| American Custom Chemicals Corporation | APO0001331 | DARUSENTAN 95.00% | 171714-84-4 | 1MG | $593.04 | 2021-12-16 | Buy |
Darusentan Chemical Properties,Uses,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>
| 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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32836 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Shanghai Acmec Biochemical Technology Co., Ltd. | +undefined18621343501 | product@acmec-e.com | China | 33350 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| SHANGHAI KEAN TECHNOLOGY CO., LTD. | +8613817748580 | cooperation@kean-chem.com | China | 40067 | 58 |