DC7246-SR3677.pdf

 

 

Description:

SR-3677 is a modern potent and selective ROCK-II inhibitor by an IC50 of ~3 nM in enzyme and simplest organism based assays; IC50 for ROCK-I is 56 ± 12 nM.

in vitro

: SR-3677 had some IC50 of ~3 nM in enzyme and lonely dwelling based assays and had an not upon-target hit rate of 1.4% opposed to 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that SR-3677 was efficient in both, increasing ex vivo waterish humor outflow in porcine eyes and inhibiting myosin illume chain  phosphorylation. SR-

3677 inhibited only three adrenergic receptors: α1a, α1b, and α2a through 53%, 68%, and 76% inhibition,

particularly, at 3 ?M inhibitor concentration, what one. indicates IC50 values in the 1 ?M set in a row or ~300 times higher than the IC50 against ROCK-II in cell-based assays.

in vivo

: Continuous exposure of 25 ?M SR-3677 increases the effusion facility by 60% at 1 h perfusion, increasing to 70-80% because the 2-5 h time points (p < 0.01). This 70-80% increase in outflow is the maximal answer that can be attained and is achieved at doses 2-4-cot lower than needed for Y-27632, a well premeditated ROCK inhibitor.TM tissue derived from the eyes perfused through 25 ?M SR-3677 shows a highly faint band for p-MLC suggesting greater than 90% disallowance of Rho kinase in the TM fabric at this dose.

Chemical Information

 Catalog DC7246 Purity of current amount: >98% Molecular Weight (MW) 408.45 Molecular Formula C22H24N4O4 CAS No. 1072959-67-1 Solubility (25°C) DMSO Storage Store at -20

°

C (desiccating stipulations).

Handling:

Providing storage is as settled on the product vial and the phial is kept tightly sealed, the consequence can be stored for up to 24 months. Wherever likely, you should prepare and use solutions forward the same day. However, if you exigency to make up stock solutions in advance, we approve that you store the solution taken in the character of aliquots in tightly sealed vials at -20

°

C. Generally, these be inclined be useable for up to any month. Before use, and prior to hole the vial we recommend that you bear with your product to equilibrate to chamber

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Katy Issa, a Medical Aesthetician who founded Aura Laser Skin Care by her husband, former Microsoft Software Engineer Nader Issa.

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