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Olinciguat

Cat. No. M28724
Olinciguat Structure
Synonym:

IW-1701

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Biological Activity

Olinciguat (IW-1701) is an oral guanylate cyclase (sGC) stimulator with concentration-dependent stimulation of sGC in purified rat and human enzyme assays and a whole cell assay.

Chemical Information
Molecular Weight 509.39
Formula C21H16F5N7O3
CAS Number 1628732-62-6
Form Solid
Solubility (25°C) DMSO 125 mg/mL (ultrasonic)
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] Boris Tchernychev, et al. Br J Pharmacol. Olinciguat, a stimulator of soluble guanylyl cyclase, attenuates inflammation, vaso-occlusion and nephropathy in mouse models of sickle cell disease

[2] Peter Sandner, et al. Expert Opin Ther Pat. Soluble guanylate cyclase stimulators and their potential use: a patent review

[3] Daniel P Zimmer, et al. Front Pharmacol. Olinciguat, an Oral sGC Stimulator, Exhibits Diverse Pharmacology Across Preclinical Models of Cardiovascular, Metabolic, Renal, and Inflammatory Disease

[4] E S Buys, et al. Nitric Oxide. Discovery and development of next generation sGC stimulators with diverse multidimensional pharmacology and broad therapeutic potential

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Keywords: Olinciguat, IW-1701 supplier, Guanylate Cyclase, inhibitors, activators


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