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Belumosudil (SLx-2119)

Cat. No. M9209
Belumosudil (SLx-2119) Structure
Synonym:

KD-025

Size Price Availability Quantity
5mg USD 76.5  USD85 In stock
10mg USD 108  USD120 In stock
25mg USD 180  USD200 In stock
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Quality Control
Biological Activity

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). SLx-2119 (40 µM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC.

In vivo, SLx-2119 (KD-025) (100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 452.51
Formula C26H24N6O2
CAS Number 911417-87-3
Purity 99.60%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
References

Selective ROCK2 Inhibition In Focal Cerebral Ischemia.
Lee JH, et al. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14. PMID: 24466563.

Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin.
Boerma M, et al. Blood Coagul Fibrinolysis. 2008 Oct;19(7):709-18. PMID: 18832915.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Belumosudil (SLx-2119), KD-025 supplier, ROCK, inhibitors

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