| Identification | Back Directory | [Name]
N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide | [CAS]
1072959-67-1 | [Synonyms]
SR3677
CS-1125
CS-2825
SR-3677; SR 3677
SR 3677 hydrochloride
SR 3677 dihydrochloride
N-(2-(2-(Dimethylamino)ethoxy)-4-(1H-pyrazol-4-yl)phenyl)-2,3-dihydrobenzo[b][1,4]dioxine-2-ca
N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide
1,4-Benzodioxin-2-carboxamide, N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-
N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-benzo[b][1,4]dioxin-2-carboxamide
N-(2-(2-(diMethylaMino)ethoxy)-4-(1H-pyrazol-4-yl)phenyl)-2,3-dihydrobenzo[b][1,4]dioxine-2-carboxaMide
N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl-2,3-dihydro-1,4-benzodioxin-2-carboxamidehydrochloride
N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl-2,3-dihydro-1,4-benzodioxin-2-carboxamide dihydrochloride | [Molecular Formula]
C22H24N4O4 | [MDL Number]
MFCD16619390 | [MOL File]
1072959-67-1.mol | [Molecular Weight]
408.45 |
| Chemical Properties | Back Directory | [Boiling point ]
646.9±55.0 °C(Predicted) | [density ]
1.298 | [storage temp. ]
Desiccate at RT | [solubility ]
DMSO: soluble15mg/mL, clear | [form ]
powder | [pka]
11.90±0.70(Predicted) | [color ]
white to light brown |
| Hazard Information | Back Directory | [Uses]
SR 3677 is an ATP-competitive inhibitor of Rho-kinases (ROCK-I/ROCK-II) which reduces amyloid-β production. It’s hypothesized that Alzheimer’s Disease, can be treated with this type of treatment, and delay further progression of the disease. | [Biological Activity]
sr-3677 is a novel, potent and highly selective inhibitor of rho kinase (rock-ii) with the ic50 value of ~0.3nm in enzyme and cell based assays [1].sr-3677 has been reported to selectively inhibit the rock- ii with the ic50 values of ~3nm, ~3nm, 56nm, 3.968μm,1.190μm and 7.491μm for rock-ii，ppmlc, rock-i, pka, mrck and akt1, respectively. in addition, sr-3677 has been shown several key binding elements that contribute to the high potency and selectivity in the docking assay. furthermore, sr-3677 has been revealed to be efficacious in enhancing aqueous humor outflow and in target modulation in the pharmacology studies [1]. | [in vivo]
ExVivo: Pharmacology studies shows that SR-3677 is efficacious in both, increasing ex vivo
aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation. Continuous exposure of 25 μM SR-3677 increases the outflow facility by 60% at 1 h perfusion, increasing to 70–80% for the 2–5 h time points[1]. | [IC 50]
ROCK-II: 3 nM (IC50); ROCK-I: 56 nM (IC50) | [storage]
room temperature (desiccate) | [References]
[1] feng y1, yin y, weiser a, griffin e, cameron md, lin l, ruiz c, schürer sc, inoue t, rao pv, schr?ter t, lograsso p. discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective rho kinase (rock-ii) inhibitors. j med chem. 2008 nov 13;51(21):6642-5. doi: 10.1021/jm800986w. epub 2008 oct 4. |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
parabiochem
|
| Telephone: |
025-83453382-8005 |
| Website: |
www.parabiochem.cn |
|