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Oxidized Nifedipine

Cat. No. M8840
Oxidized Nifedipine Structure
Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 180  USD180 In stock
50mg USD 420  USD420 In stock
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Quality Control & Documentation
Biological Activity

Dehydro Nifedipine is the main metabolite of nifedipine in human plasma. Dehydro Nifedipine inhibits glucose uptake in PC-12 cells with an IC50 value of 130 μM. Nifedipine is an antianginal and antihypertensive agent. Oxidized nifedipine has been used for apoptotic signaling studies in dopaminergic neurons.

Chemical Information
Molecular Weight 344.32
Formula C17H16N2O6
CAS Number 67035-22-7
Solubility (25°C) DMSO 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] Michael Ikechukwu Oraebosi, et al. Chronopharmacology of the alpha-lipoic acid/nifedipine/glimepiride combination in the amelioration of retinopathy in rats

[2] So-Hui Choe, et al. Effect of nifedipine, a calcium channel blocker, on the generation of nitric oxide and interleukin-1β by murine macrophages activated by lipopolysaccharide from Prevotella intermedia

[3] Hong-Jaan Wang, et al. Shenmai-Yin decreased the clearance of nifedipine in rats: The involvement of time-dependent inhibition of nifedipine oxidation

[4] Yunhong Li, et al. Research advances in pathogenesis and prophylactic measures of acute high altitude illness

[5] David M Haas, et al. Nifedipine pharmacokinetics are influenced by CYP3A5 genotype when used as a preterm labor tocolytic

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