SLx-2119

Cas：911417-87-3

Product Information：

SLx-2119, also known as KD-025, is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively).

Chemical Formula: C26H24N6O2

Exact Mass: 452.1961

Molecular Weight: 452.518

Elemental Analysis: C, 69.01; H, 5.35; N, 18.57; O, 7.07

Synonym:

KD 025

Belumosudil

Chemical Name: 2-[3-[4-(1H-indazol-5-ylamino)-2-quinazolinyl]phenoxy]-N-(1-methylethyl)-acetamide

InChi Key:

GKHIVNAUVKXIIY-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H24N6O2/c1-16(2)28-24(33)15-34-20-7-5-6-17(13-20)25-30-23-9-4-3-8-21(23)26(31-25)29-19-10-11-22-18(12-19)14-27-32-22/h3-14,16H,15H2,1-2H3,(H,27,32)(H,28,33)(H,29,30,31)

Smiles Code:

O=C(NC(C)C)COC1=CC=CC(C2=NC(NC3=CC4=C(NN=C4)C=C3)=C5C=CC=CC5=N2)=C1

Technical Data：

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

In Vitro：

Belumosudil (SLx-2119; 40 µM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC. The microarray hybridized with aRNA from HMVEC treated with Belumosudil, shows a 5-times higher background than the other arrays.

In Vivo：

Belumosudil (KD-025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. Belumosudil is at least as efficacious in aged, diabetic or female mice, as in normal adult males.

References：

1. Lee JH, Zheng Y, von Bornstadt D, Wei Y, Balcioglu A, Daneshmand A, Yalcin N,

Yu E, Herisson F, Atalay YB, Kim MH, Ahn YJ, Balkaya M, Sweetnam P, Schueller O, Poyurovsky MV, Kim HH, Lo EH, Furie KL, Ayata C. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14. PubMed PMID: 24466563; PubMed Central PMCID: PMC3900310.

2. Boerma M, Fu Q, Wang J, Loose DS, Bartolozzi A, Ellis JL, McGonigle S,

Paradise E, Sweetnam P, Fink LM, Vozenin-Brotons MC, Hauer-Jensen M. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin. Blood Coagul Fibrinolysis. 2008 Oct;19(7):709-18. doi: 10.1097/MBC.0b013e32830b2891. PubMed PMID: 18832915; PubMed Central PMCID: PMC2713681.

Products are for research use only. Not for human use.