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JP1302 

Cat. No. M30631
JP1302  Structure
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Biological Activity

JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research.

Chemical Information
Molecular Weight 368.47
Formula C24H24N4
CAS Number 80259-18-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Dylan C Mitchell, et al. Nat Biotechnol. A proteome-wide atlas of drug mechanism of action

[2] Xiaoyu Chen, et al. Cell Rep. Molecular Mechanism for Ligand Recognition and Subtype Selectivity of α2C Adrenergic Receptor

[3] Hidenobu Tsutsui, et al. Eur J Pharmacol. Inhibition of α2C-adrenoceptors ameliorates cisplatin-induced acute renal failure in rats

[4] Joanna Raczak-Gutknecht, et al. Dose Response. Are Alpha-2D Adrenoceptor Subtypes Involved in Rat Mydriasis Evoked by New Imidazoline Derivatives: Marsanidine and 7-Methylmarsanidine?

[5] Michiko Nakamura, et al. J Neurochem. α(2A) adrenoceptor-mediated presynaptic inhibition of GABAergic transmission in rat tuberomammillary nucleus neurons

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