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PET-cGMP

Cat. No. M7998
PET-cGMP Structure
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Biological Activity

cGMP-dependent protein kinase (PKG I and PKG II) activator. Potent membrane permeant activator of both isozymes I α and I β of cGMP-dependent protein kinase. Common stimulators such as 8-Br-cGMP or 8-pCPT-cGMP mainly activate kinase subtype Iα.

Chemical Information
Molecular Weight 467.3
Formula C18H15N5O7PNa
CAS Number 78080-27-0
Solubility (25°C) Water: ~10 mmol
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] Eleonora Vighi, et al. New cGMP analogues restrain proliferation and migration of melanoma cells

[2] Makhala Michell Khammy, et al. PDE1A inhibition elicits cGMP-dependent relaxation of rat mesenteric arteries

[3] Gyrid Nygaard, et al. Time-dependent inhibitory effects of cGMP-analogues on thrombin-induced platelet-derived microparticles formation, platelet aggregation, and P-selectin expression

[4] Ken Breslow, et al. Final PET CGMP regulation

[5] J Y Wei, et al. Identification of competitive antagonists of the rod photoreceptor cGMP-gated cation channel: beta-phenyl-1,N2-etheno-substituted cGMP analogues as probes of the cGMP-binding site

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Keywords: PET-cGMP supplier, inhibitors, activators


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