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Ibodutant

Cat. No. M9200
Ibodutant Structure
Synonym:

MEN15596

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Biological Activity

Ibodutant (MEN15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1. Ibodutant selectively blocks the tachykinin receptor NK2, with blockade practically complete in nanomolar concentrations.

Chemical Information
Molecular Weight 644.87
Formula C37H48N4O4S
CAS Number 522664-63-7
Solubility (25°C) DMSO
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] Cialdai C, et al. Eur J Pharmacol. MEN15596, a novel nonpeptide tachykinin NK2 receptor antagonist.

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Keywords: Ibodutant, MEN15596 supplier, Neurokinin Receptor, inhibitors, activators


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