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DK-AH 269

Cat. No. M7768
DK-AH 269 Structure
Synonym:

DK-AH 269

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Biological Activity

DK-AH 269 (Cilobradine) is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.

Chemical Information
Molecular Weight 519.07
Formula C28H38N2O5 · HCl
CAS Number 186097-54-1
Solubility (25°C) Water: ~20 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] Dongyang Li, et al. Involvement of Hyperpolarization-Activated Cyclic Nucleotide-Gated Channel 3 in Oxytocin Neuronal Activity in Lactating Rats With Pup Deprivation

[2] Josef G Trapani, et al. Mechanism of spontaneous activity in afferent neurons of the zebrafish lateral-line organ

[3] Jun-Li Cao, et al. Mesolimbic dopamine neurons in the brain reward circuit mediate susceptibility to social defeat and antidepressant action

[4] A Raes, et al. Use-dependent block of Ih in mouse dorsal root ganglion neurons by sinus node inhibitors

[5] D Janigro, et al. Preferential inhibition of Ih in rat trigeminal ganglion neurons by an organic blocker

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Keywords: DK-AH 269, DK-AH 269 supplier, HCN Channel, inhibitors, activators


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