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Iptakalim hydrochloride 

Cat. No. M30418
Iptakalim hydrochloride  Structure
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Biological Activity

Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist.

Chemical Information
Molecular Weight 179.73
Formula C9H22ClN
CAS Number 642407-63-4
Form Solid
Solubility (25°C) Water 25 mg/mL (ultrasonic and warming and heat to 70°C)
Storage 4°C, dry, sealed
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] Nan Bai, et al. Clin Pharmacol Drug Dev. Evaluation of the Potential Effect of Iptakalim Hydrochloride on the QT Interval in Single- and Multiple-Ascending-Dose Studies Using Concentration-QTc Analysis

[2] Yun Cai, et al. J Pharm Pharmacol. Single-dose pharmacokinetics and safety of iptakalim hydrochloride in Chinese healthy volunteers

[3] J Hu, et al. Neurosci Lett. Iptakalim inhibits nicotinic acetylcholine receptor-mediated currents in dopamine neurons acutely dissociated from rat substantia nigra pars compacta

[4] Yan-Ling Yang, et al. Brain Res. Iptakalim hydrochloride protects cells against neurotoxin-induced glutamate transporter dysfunction in in vitro and in vivo models

[5] Weiping Xie, et al. Life Sci. Effects of iptakalim hydrochloride, a novel KATP channel opener, on pulmonary vascular remodeling in hypoxic rats

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