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Ripasudil (K-115) hydrochloride dihydrate - 99%, high purity , Rho-associated protein kinase inhibitor, CAS No.887375-67-9, Rho-associated protein kinase inhibitor

COA

Grade & Purity:

≥99%

Cas Number: 887375-67-9
Molecular Weight: 395.88
PubChem CID: 11625386

In stock

Item Number

R413902

Grouped product items
SKU	Size	Availability	Price
R413902-5mg	5mg	3	$189.90
R413902-10mg	10mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$307.90
R413902-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$688.90
R413902-50mg	50mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$1,175.90
R413902-100mg	100mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$1,899.90

ROCK2 Selective Inhibitors

View related series

Cell Cycle (2830) Cell Cycle/DNA Damage (2602) Cytoskeleton (498) ROCK (71) Stem Cell/Wnt (1019) TGF-beta/Smad (303)

Basic Description

Synonyms	1H-1,4-Diazepine, 1-((4-fluoro-5-isoquinolinyl)sulfonyl)hexahydro-2-methyl-, monohydrochloride, dihydrate, (2S)- \| 4-Fluoro-5-[(2S)-2-methyl-1,4-diazepane-1-sulfonyl]isoquinoline dihydrate hydrochloride \| Ripasudil HCl dihydrate \| Ripasudil hydrochloride
Specifications & Purity	≥99%
Biochemical and Physiological Mechanisms	Ripasudil (K-115) hydrochloride dihydrate is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Action Type	INHIBITOR
Mechanism of action	Rho-associated protein kinase inhibitor
Product Description	Information Ripasudil (K-115) hydrochloride dihydrate is potentROCKinhibitor withIC50of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension. Targets ROCK2 (Cell-free assay); ROCK1 (Cell-free assay) 19 nM; 51 nM In vitro In monkey trabecular meshwork (TM) cells, Ripasudil induces retraction and rounding of cell bodies as well as disruption of actin bundles. In Schlemm\'s canal endothelial (SCE) cells, Ripasudil significantly decreases transendothelial electrical resistance (TEER), increases the transendothelial flux of FITC-dextran, and disrupts cellular localization of ZO-1 expression. In vivo In albino rabbits and monkeys, topical instillation of Ripasudil significantly reduces intraocular pressure (IOP) with maximum IOP reduction of 8.55 mmHg and 4.36 mmHg at 0.5 % and 0.4%, respectively. Ripasudil (1 mg/kg daily, p.o.) exerts a neuroprotective effect on retinal ganglion cell (RGC) after optic nerve crush (NC) by suppressing oxidative stress through pathways involving the Nox family in a mouse model.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
- Superclass Organoheterocyclic compounds
  - Class Isoquinolines and derivatives

Kingdom	Organic compounds
Superclass	Organoheterocyclic compounds
Class	Isoquinolines and derivatives
Subclass	Not available
Intermediate Tree Nodes	Not available
Direct Parent	Isoquinolines and derivatives
Alternative Parents	1,4-diazepanes Pyridines and derivatives Organosulfonamides Benzenoids Aryl fluorides Sulfonyls Heteroaromatic compounds Dialkylamines Azacyclic compounds Organofluorides Organic oxides Hydrochlorides Hydrocarbon derivatives
Molecular Framework	Aromatic heteropolycyclic compounds
Substituents	Isoquinoline - 1,4-diazepane - Diazepane - Aryl fluoride - Aryl halide - Pyridine - Benzenoid - Organosulfonic acid amide - Heteroaromatic compound - Sulfonyl - Organosulfonic acid or derivatives - Organic sulfonic acid or derivatives - Secondary aliphatic amine - Azacycle - Secondary amine - Organonitrogen compound - Organofluoride - Organohalogen compound - Amine - Hydrocarbon derivative - Organic nitrogen compound - Organic oxide - Organic oxygen compound - Organosulfur compound - Hydrochloride - Aromatic heteropolycyclic compound
Description	This compound belongs to the class of organic compounds known as isoquinolines and derivatives. These are aromatic polycyclic compounds containing an isoquinoline moiety, which consists of a benzene ring fused to a pyridine ring and forming benzo[c]pyridine.
External Descriptors	Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61. DOI: 10.1186/s13321-016-0174-y

Product Properties

ALogP	0.739
HBD Count	1
Rotatable Bond	2

Associated Targets(Human)

ROCK1 Tclin Rho-associated protein kinase 1 (4723 Activities)

Discover Target: ROCK1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ROCK2 Tclin Rho-associated protein kinase 2 (6206 Activities)

Discover Target: ROCK2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mechanisms of Action

Mechanism of Action	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	References

Names and Identifiers

IUPAC Name	4-fluoro-5-[[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline;dihydrate;hydrochloride
INCHI	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
InChIKey	CMDJNMACGABCKQ-XVSRHIFFSA-N
Smiles	CC1CNCCCN1S(=O)(=O)C2=CC=CC3=CN=CC(=C32)F.O.O.Cl
Isomeric SMILES	C[C@H]1CNCCCN1S(=O)(=O)C2=CC=CC3=CN=CC(=C32)F.O.O.Cl
PubChem CID	11625386
Molecular Weight	395.88

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

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4 results found

Lot Number	Certificate Type	Date	Item
G2206452	Certificate of Analysis	Apr 07, 2024	R413902
G2206453	Certificate of Analysis	Apr 07, 2024	R413902
G2206442	Certificate of Analysis	Apr 07, 2024	R413902
G2206451	Certificate of Analysis	Apr 07, 2024	R413902

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro Water: 79 mg/mL (199.55 mM); DMSO: 26 mg/mL warmed with 50ºC Water: bath (65.67 mM); Ethanol: 5 mg/mL warmed with 50ºC Water: bath (12.63 mM);
Sensitivity	moisture sensitive
DMSO(mg / mL) Max Solubility	26
DMSO(mM) Max Solubility	65.67646762
Water(mg / mL) Max Solubility	79
Water(mM) Max Solubility	199.5554208
Molecular Weight	395.900 g/mol
XLogP3
Hydrogen Bond Donor Count	4
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	2
Exact Mass	395.108 Da
Monoisotopic Mass	395.108 Da
Topological Polar Surface Area	72.700 Å²
Heavy Atom Count	25
Formal Charge	0
Complexity	482.000
Isotope Atom Count	0
Defined Atom Stereocenter Count	1
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
The total count of all stereochemical bonds	0
Covalently-Bonded Unit Count	4

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