SAR407899 free base
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MedKoo CAT#: 526770

CAS#: 923359-38-0 (free base)

Description: SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity. SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. SAR407899 is equipotent against human and rat-derived Rho-kinase 2 with inhibition constant values of 36 nM and 41 nM, respectively. SAR407899 is approximately 8-fold more active than fasudil. SAR407899 potently (mean IC(50) values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds. The antihypertensive effect of SAR407899 was superior to that of fasudil and Y-27632.


Price and Availability

Size
Price

10mg
USD 90
500mg
USD 1250
Size
Price

25mg
USD 150
1g
USD 1950
Size
Price

100mg
USD 450
5g
USD 5250

SAR407899, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 2 g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526770
Name: SAR407899 free base
CAS#: 923359-38-0 (free base)
Chemical Formula: C14H16N2O2
Exact Mass: 244.1212
Molecular Weight: 244.294
Elemental Analysis: C, 68.83; H, 6.60; N, 11.47; O, 13.10


Related CAS #: 923262-96-8 (HCl)   923359-38-0 (free base)  

Synonym: SAR407899; SAR 407899; SAR-407899; SAR407899 HCl

IUPAC/Chemical Name: 6-(piperidin-4-yloxy)isoquinolin-1(2H)-one

InChi Key: IPEXHQGMTHOKQV-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H16N2O2/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)

SMILES Code: O=C1NC=CC2=C1C=CC(OC3CCNCC3)=C2


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

Related CAS#
CAS#923262-96-8 (HCl);
CAS#923359-38-0 (free base).


References

1: Löhn M, Plettenburg O, Kannt A, Kohlmann M, Hofmeister A, Kadereit D, Monecke P, Schiffer A, Schulte A, Ruetten H, Ivashchenko Y. End-organ protection in hypertension by the novel and selective Rho-kinase inhibitor, SAR407899. World J Cardiol. 2015 Jan 26;7(1):31-42. doi: 10.4330/wjc.v7.i1.31. PubMed PMID: 25632317; PubMed Central PMCID: PMC4306204.

2: Babelova A, Jansen F, Sander K, Löhn M, Schäfer L, Fork C, Ruetten H, Plettenburg O, Stark H, Daniel C, Amann K, Pavenstädt H, Jung O, Brandes RP. Activation of Rac-1 and RhoA contributes to podocyte injury in chronic kidney disease. PLoS One. 2013 Nov 7;8(11):e80328. doi: 10.1371/journal.pone.0080328. eCollection 2013. PubMed PMID: 24244677; PubMed Central PMCID: PMC3820652.

3: Guagnini F, Ferazzini M, Grasso M, Blanco S, Croci T. Erectile properties of the Rho-kinase inhibitor SAR407899 in diabetic animals and human isolated corpora cavernosa. J Transl Med. 2012 Mar 23;10:59. doi: 10.1186/1479-5876-10-59. PubMed PMID: 22444253; PubMed Central PMCID: PMC3328245.

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

5: 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. Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor. Hypertension. 2009 Sep;54(3):676-83. doi: 10.1161/HYPERTENSIONAHA.109.134353. Epub 2009 Jul 13. PubMed PMID: 19597037.