A ROCK1 and ROCK2 inhibitor
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Ripasudil (hydrochloride hydrate)

Item No. 19920

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-isoquinoline, monohydrochloride, dihydrate
CAS Number
887375-67-9
Synonyms
  • K-115
Molecular Formula
C15H18FN3O2S • HCl [2H2O]
Formula Weight
395.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: Slightly solubleDMSO: 30 mg/mlPBS (pH 7.2): 0.5 mg/ml
λmax
211, 278, 324 nm
SMILES
FC1=C2C(C=CC=C2S(N3CCCNC[C@@H]3C)(=O)=O)=CN=C1.Cl.O.O
InChi Code
InChI=1S/C15H18FN3O2S.ClH.2H2O/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;1H;2*1H2/t11-;;;/m0.../s1
InChi Key
CMDJNMACGABCKQ-XVSRHIFFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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    1 mg

    $44

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    5 mg

    $164

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    10 mg

    $263

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    25 mg

    $493

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    Product Description

    Ripasudil is an inhibitor of Rho-associated kinase 1 (ROCK1) and ROCK2 (IC50s = 51 and 19 nM, respectively).1 It is selective for ROCK1 and ROCK2 over protein kinase A catalytic subunit α (PKACα) and PKC (IC50s = 2,100 and >10,000 nM, respectively). Ripasudil (0.4%) reduces intraocular pressure in cynomolgus monkey to a greater extent than the prostaglandin FP receptor agonist latanoprost (Item No. 16812). It increases the outflow facility of the aqueous humor in rabbit eyes when administered in a 0.4% solution. Ripasudil (0.4%) decreases intraocular pressure, retinal ganglion cell death, and thinning of inner retinal layers, as well as improves retinal function, in an excitatory amino acid transporter 1 (EAAT1) knockout mouse model of normal tension glaucoma.2 Formulations containing ripasudil have been used in the treatment of glaucoma and ocular hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Isobe, T., Mizuno, K., Kaneko, Y., et al. Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits. Curr. Eye Res. 39(8), 813-822 (2014).

    2. Akaiwa, K., Namekata, K., Azuchi, Y., et al. Topical ripasudil suppresses retinal ganglion cell death in a mouse model of normal tension glaucoma. Invest. Ophthalmol. Vis. Sci. 59(5), 2080-2089 (2018).