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Belumosudil mesylate

Cat. No. M9619
Belumosudil mesylate Structure
Synonym:

SLx-2119 mesylate; KD025 mesylate

Size Price Availability
10mg USD 114  USD114 Out of stock
50mg USD 345  USD345 Out of stock
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Quality Control & Documentation
Biological Activity

Belumosudil mesylate (SLx-2119 mesylate) 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). Belumosudil (SLx-2119; 40 µM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC. Belumosudil (KD025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion.

Chemical Information
Molecular Weight 548.61
Formula C27H28N6O5S
CAS Number 2109704-99-4
Solubility (25°C) DMSO ≥ 12 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] No authors listed. Am J Health Syst Pharm. Belumosudil Mesylate

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Keywords: Belumosudil mesylate, SLx-2119 mesylate; KD025 mesylate supplier, ROCK, inhibitors, activators


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