Ripasudil
- CAS No.
- 223645-67-8
- Chemical Name:
- Ripasudil
- Synonyms
- CS-1564;Ripasudil;k115 free base;K-115, Ripasudil;RIPASUDIL HYDROCHLOIDE;RIPASUDIL FREE BASE;K 115 FREE BASE;K115 FREE BASE;(S)-4-Fluoro-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline;4-Fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline;Isoquinoline, 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-
- CBNumber:
- CB92722374
- Molecular Formula:
- C15H18FN3O2S
- Molecular Weight:
- 323.39
- MDL Number:
- MFCD28291829
- MOL File:
- 223645-67-8.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| K-115 | CSN16953 | 5mg | $154 |
| K-115freebase 98+% | CD31002611 | 250mg | $515 |
| K-115 | CSN16953 | 25mg | $557 |
| (S)-4-fluoro-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline 98% | CM146182 | 100mg | $880 |
| K-115freebase 98+% | CD31002611 | 1g | $1290 |
| More product size | |||
| 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 |
| pka | 9.70±0.40(Predicted) |
| form | powder |
| color | white to beige |
| Water Solubility | H2O: 2mg/mL, clear |
| InChI | 1S/C15H18FN3O2S/c1-11-8-17-6-3-7-19(11)22(20,21)14-5-2-4-12-9-18-10-13(16)15(12)14/h2,4-5,9-11,17H,3,6-8H2,1H3/t11-/m0/s1 |
| InChIKey | QSKQVZWVLOIIEV-NSHDSACASA-N |
| SMILES | Fc1c2c(cnc1)cccc2[S](=O)(=O)N3[C@H](CNCCC3)C |
| FDA UNII | 11978226XX |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
| WGK Germany | WGK 3 |
| Storage Class | 11 - Combustible Solids |
Ripasudil price More Price(5)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| CSNpharm | CSN16953 | K-115 | 223645-67-8 | 5mg | $154 | 2021-12-16 | Buy |
| Crysdot | CD31002611 | K-115freebase 98+% | 223645-67-8 | 250mg | $515 | 2021-12-16 | Buy |
| CSNpharm | CSN16953 | K-115 | 223645-67-8 | 25mg | $557 | 2021-12-16 | Buy |
| Chemenu | CM146182 | (S)-4-fluoro-5-((2-methyl-1,4-diazepan-1-yl)sulfonyl)isoquinoline 98% | 223645-67-8 | 100mg | $880 | 2021-12-16 | Buy |
| Crysdot | CD31002611 | K-115freebase 98+% | 223645-67-8 | 1g | $1290 | 2021-12-16 | Buy |
Ripasudil Chemical Properties,Uses,Production
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
Ripasudil (K-115) reduces intraocular pressure (IOP) in a concentration-dependent manner at concentrations between 0.1% and 0.4% in monkey eyes and 0.0625% to 0.5% in rabbit eyes, respectively[1]. Ripasudil (K-115; 1 mg/kg, p.o. daily) shows a neuroprotective effect on retinal ganglion cells (RGCs) after nerve crush (NC). Ripasudil also inhibits the oxidative stress induced by axonal injury in mice. Ripasudil suppresses the time-dependent production of ROS in RGCs after NC injury[3].
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 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shenzhen Nexconn Pharmatechs Ltd | +86-755-89396905 +86-15013857715 | admin@nexconn.com | China | 10404 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30227 | 58 |
| Shanxi Xuanran Import and Export Trade Co., Ltd. | +8617735180244 | mike_yan@xuanranglobal.com | CHINA | 4017 | 58 |
| AFINE CHEMICALS LIMITED | +86-0571-85134551 | sales@afinechem.com | China | 15079 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471; | sales@sarms4muscle.com | China | 10473 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39040 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8615965530500 | nickzhang@hangyubiotech.com | China | 8614 | 58 |
| HANGZHOU LEAP CHEM CO., LTD. | +86-571-87711850 | market18@leapchem.com | China | 43333 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131957 | 58 |
