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Praliciguat

Cat. No. M21391
Praliciguat Structure
Synonym:

IW-1973

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Quality Control & Documentation
Biological Activity

Praliciguat (IW-1973) is a potent, orally available promoter of soluble guanylate cyclase, which enhances the NO signaling pathway and is a vasodilator. In HEK-293 cells, Praliciguat (IW-1973) was able to stimulate sGC with an EC50 value of 197 nM.

Chemical Information
Molecular Weight 534.36
Formula C21H14F8N6O2
CAS Number 1628730-49-3
Solubility (25°C) DMSO ≥ 200 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] Kate Kosmac, et al. Circ Res. Praliciguat and Soluble Guanylate Cyclase Stimulators for Peripheral Artery Disease

[2] Ninon Foussard, et al. Circ Res. Praliciguat Promotes Ischemic Leg Reperfusion in Leptin Receptor-Deficient Mice

[3] Chad D Schwartzkopf, et al. Front Pharmacol. Beneficial Metabolic Effects of Praliciguat, a Soluble Guanylate Cyclase Stimulator, in a Mouse Diet-Induced Obesity Model

[4] Christopher J Rush, et al. JAMA Cardiol. Prevalence of Coronary Artery Disease and Coronary Microvascular Dysfunction in Patients With Heart Failure With Preserved Ejection Fraction

[5] Guang Liu, et al. Am J Physiol Renal Physiol. Praliciguat inhibits progression of diabetic nephropathy in ZSF1 rats and suppresses inflammation and apoptosis in human renal proximal tubular cells

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Keywords: Praliciguat, IW-1973 supplier, Guanylate Cyclase, inhibitors, activators


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