Cofttek holdings limited

PKC&ROCK

SAR407899 HCL (923262-96-8)

SAR407899 Hcl is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively…

Not Intended for Therapeutic Use. For research use only.

CAS: 923262-96-8 Category

SAR407899 HCL (923262-96-8) Description

SAR407899 hydrochloride is a potent and ATP-competitive ROCK inhibitor, with Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 inhibits ROCK-2 better than ROCK-1, with IC50s of 102±19 nM and 276±26 nM, respectively, in the presence of 40 μM ATP. SAR407899 also less potently inhibits PKC-Δ and MSK-1, with IC50s of 5.4 and 3.1 μM, respectively. SAR407899 (0.1, 0.3, 1.0, and 3.0 μM) specifically inhibits the ROCK-mediated phosphorylation of MYPTT696 in HeLa cells stimulated with PHEN, and shows such effects at 1 μM and 10 μM in primary rat aortic smooth muscle cells. SAR407899 (3 μM) completely blocks thrombin-induced shrinkage of human umbilical vein endothelial cells (HUVECs) and stress fiber formation. SAR407899 concentration-dependently inhibits 5-bromodeoxyuridine incorporation into the cells with an IC50 of 5.0±1.3 μM. SAR407899 also effectively inhibits THP-1 migration with an IC50 of 2.5±1.0 μM. SAR407899 shows a potent vasorelaxant activity in a broad variety of isolated arteries taken from different vascular beds and species, with a range of IC50 values between 122 and 280 nM[1]. SAR407899 dose-dependently relaxes the phenylephrine pre-contracted smooth muscle, with IC50s of 0.07 and 0.05 μM, respectively.

 

SAR407899 HCL (923262-96-8) Specifications

Product Name SAR407899 hcl
Synonym SAR-407899; SAR407899 HCl
Chemical Name SAR407899 hydrochloride; 6-(piperidin-4-yloxy)isoquinolin-1(2H)-one hydrochloride; KMNVOGVCCZNVNU-UHFFFAOYSA-N;6-(piperidin-4-yloxy)isoquinolin-1(2H)-one hydrochloride;
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number  923262-96-8
Molecular Formula C14H17ClN2O2
Molecular Weight 280.75
Monoisotopic Mass 280.098g/mol
MDL number N/A
InChIKey KMNVOGVCCZNVNU-UHFFFAOYSA-N
InChi Code InChI=1S/C14H16N2O2.ClH/c17-14-13-2-1-12(9-10(13)3-8-16-14)18-11-4-6-15-7-5-11;/h1-3,8-9,11,15H,4-7H2,(H,16,17);1H
SMILES O=C1NC=CC2=C1C=CC(OC3CCNCC3)=C2.[H]Cl
Form Powder
Color white to off-white
Solubility  Soluble in DMSO
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling N/A
Application A potent, ATP-competitive ROCK inhibitor

 


=

RIDADR NONH for all modes of transport

References:

[1]. Guagnini F, et al. Erectile properties of the Rho-kinase inhibitor SAR407899 in diabetic animals and human isolated corpora cavernosa. J Transl Med. 2012 Mar 23;10:59.

[2]. Chen W, et al. Screening RhoA/ROCK inhibitors for the ability to prevent chronic rejection of mouse cardiac allografts.Transpl Immunol. 2018 Jun 6. pii: S0966-3274(18)30029-7.

[3]. Erectile properties of the Rho-kinase inhibitor SAR407899 in diabetic animals and human isolated corpora cavernosa.Guagnini F, Ferazzini M, Grasso M, Blanco S, Croci T. J Transl Med. 2012 Mar 23;10:59. doi: 10.1186/1479-5876-10-59. PMID: 22444253

[4]. The Rho kinase inhibitor SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. Grisk O, Schlüter T, Reimer N, Zimmermann U, Katsari E, Plettenburg O, Löhn M, Wollert HG, Rettig R. J Hypertens. 2012 May;30(5):980-9. doi: 10.1097/HJH.0b013e328351d459. PMID: 22388233

[5]. Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor. Löhn M, Plettenburg O, Ivashchenko Y, Kannt A, Hofmeister A, Kadereit D, Schaefer M, Linz W, Kohlmann M, Herbert JM, Janiak P, O’Connor SE, Ruetten H. Hypertension. 2009 Sep;54(3):676-83. doi: 10.1161/HYPERTENSIONAHA.109.134353. Epub 2009 Jul 13. PMID: 19597037

1 review for SAR407899 HCL (923262-96-8)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The SAR407899 HCL (923262-96-8) is high purity,also customer service is pretty nice !gotta try!!

Add a review

Your email address will not be published. Required fields are marked *