Ripasudil Chemical Properties

Boiling point:

497.2±55.0 °C(Predicted)

Density 

1.293±0.06 g/cm3(Predicted)

storage temp. 

under inert gas (nitrogen or Argon) at 2–8 °C

solubility 

Soluble in DMSO

form 

powder

pka

9.70±0.40(Predicted)

color 

white to beige

Water Solubility 

H2O: 2mg/mL, clear

Ripasudil Usage And Synthesis

Description

Ripasudil (Glanatec TM, Kowa Pharmaceutical), a close derivative of fasudil, is another Rho kinase inhibitor approved in Japan at the end of 2014 for the treatment of glaucoma and ocular hypertensionwhen other therapeutic agents are not effective or cannot be administered. Additionally, ripasudil has been tested in diabetic retinopathy clinical trials and shown to promote corneal endothelial cell proliferation, endothelium regeneration, and wound healing.

Uses

Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.

Definition

ChEBI: Ripasudil is a member of isoquinolines.

in vivo

IC 50

ROCK2: 19 nM (IC₅₀); ROCK1: 51 nM (IC₅₀); CaMKIIa: 370 nM (IC₅₀); PKACa: 2.1 μM (IC₅₀); PKC: 27 μM (IC₅₀)

References

[1] Isobe T, et al. Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits. Curr Eye Res. 2014 Aug;39(8):813-22. DOI:10.3109/02713683.2013.874444
[2] Kaneko Y, et al. Effects of K-115 (Ripasudil), a novel ROCK inhibitor, on trabecular meshwork and Schlemm's canal endothelial cells. Sci Rep. 2016 Jan 19;6:19640. DOI:10.1038/srep19640
[3] Yamamoto K, et al. The novel Rho kinase (ROCK) inhibitor K-115: a new candidate drug for neuroprotective treatment in glaucoma. Invest Ophthalmol Vis Sci. 2014 Oct 2;55(11):7126-36. DOI:10.1167/iovs.13-13842

Ripasudil(223645-67-8)Related Product Information

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