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Ataciguat

Cat. No. M29701
Ataciguat Structure
Synonym:

HMR-1766

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Quality Control & Documentation
Biological Activity

Ataciguat (HMR-1766) is a nitric oxide-independent soluble guanylate cyclase (sGC) activator. Ataciguat is able to activate the ferric heme-iron redox form of sGC that stimulate the production of cyclic GMP (cGMP). Ataciguat exhibits vasodilator effects.

Chemical Information
Molecular Weight 576.49
Formula C21H19Cl2N3O6S3
CAS Number 254877-67-3
Form Solid
Solubility (25°C) DMSO 100 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] Ariane Migliato Martinelli, et al. J Pharm Pharm Sci. In Endothelial Cells, the Activation or Stimulation of Soluble Guanylyl Cyclase Induces the Nitric Oxide Production by a Mechanism Dependent of Nitric Oxide Synthase Activation

[2] Erol Çakmak, et al. Balkan Med J. Comparative Relaxant Effects of Ataciguat and Zaprinast on Sheep Sphincter of Oddi

[3] Johannes-Peter Stasch, et al. Curr Opin Pharmacol. Renal effects of soluble guanylate cyclase stimulators and activators: a review of the preclinical evidence

[4] Andreas Schäfer, et al. Pharmacol Res. Guanylyl cyclase activator ataciguat improves vascular function and reduces platelet activation in heart failure

[5] Zongmin Zhou, et al. Am J Physiol Heart Circ Physiol. Soluble guanylyl cyclase activation by HMR-1766 (ataciguat) in cells exposed to oxidative stress

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Keywords: Ataciguat, HMR-1766 supplier, Guanylate Cyclase, inhibitors, activators


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