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HA-1004

Cat. No. M42037
HA-1004 Structure
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Biological Activity

HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation.

Chemical Information
Molecular Weight 293.34
Formula C12H15N5O2S
CAS Number 91742-10-8
Form Solid
Storage Powder -20°C 3 years
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] A Zimmermann et al. Anticancer Res. Shape changes and chemokinesis of Walker carcinosarcoma cells: effects of protein kinase inhibitors (HA-1004, polymyxin B, sangivamycin and tamoxifen) and an inhibitor of diacylglycerol kinase (R 59022)

[2] M Takayasu et al. J Neurosurg. The effects of HA compound calcium antagonists on delayed cerebral vasospasm in dogs

[3] T Ishikawa et al. J Pharmacol Exp Ther. Relaxation of vascular smooth muscle by HA-1004, an inhibitor of cyclic nucleotide-dependent protein kinase

[4] R W Chapman et al. Pharmacology. Antibronchoconstrictor activity of the intracellular calcium antagonist HA 1004 in guinea pigs

[5] H M Goodman et al. Endocrinology. The isoquinoline sulfonamide inhibitors of protein phosphorylation, H-7, H-8, and HA-1004, also inhibit RNA synthesis: studies on responses of adipose tissue to growth hormone

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  Catalog
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