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Chemical Structure| 923359-38-0 Chemical Structure| 923359-38-0

Structure of SAR407899
CAS No.: 923359-38-0

Chemical Structure| 923359-38-0

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

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Product Details of SAR407899

CAS No. :923359-38-0
Formula : C14H16N2O2
M.W : 244.29
SMILES Code : O=C1NC=CC2=C1C=CC(OC3CCNCC3)=C2
MDL No. :MFCD28335199
InChI Key :IPEXHQGMTHOKQV-UHFFFAOYSA-N
Pubchem ID :15604510

Safety of SAR407899

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of SAR407899

GPCR
cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mouse podocytes 1 µM 24 hours To study the effect of mechanical stretch on podocytes, results showed that stretch activated RhoA and Rac-1, leading to TGFβ-mediated apoptosis and phenotype switch, while SAR407899 inhibited these responses. PLoS One. 2013 Nov 7;8(11):e80328

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rabbits Diabetic rabbit model Intravenous and oral 0.3, 1, 3, 10 mg/kg (i.v.); 1, 3, 10, 30 mg/kg (oral) Single dose, observation up to 360 minutes SAR407899 dose-dependently induced penile erection in rabbits, with oral 3 mg/kg and 10 mg/kg showing significantly greater potency and duration than sildenafil 6 mg/kg, and maintained efficacy in diabetic rabbits J Transl Med. 2012 Mar 23;10:59
SV129 mice 5/6 nephrectomy model Oral administration via drinking water 50 mg/L Continued for 8 weeks To investigate the effect of SAR407899 on the progression of chronic renal failure, results showed that SAR407899 significantly attenuated albuminuria and glomerular damage, and the combination with ACE inhibitor was more effective. PLoS One. 2013 Nov 7;8(11):e80328

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.09mL

0.82mL

0.41mL

20.47mL

4.09mL

2.05mL

40.93mL

8.19mL

4.09mL

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