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Pinacidil

Cat. No. M14259
Pinacidil Structure
Synonym:

P-1134

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Biological Activity

Pinacidil is a potent activator of potassium channel. Pinacidil is an antihypertensive agent which hyperpolarises vascular smooth muscle by opening K+-channels. Pinacidil significantly improves the reperfusion function and cardiac compliance. Pinacidil has direct cardioprotective efficacy.

Chemical Information
Molecular Weight 245.32
Formula C13H19N5
CAS Number 60560-33-0
Solubility (25°C) DMSO 90 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] S M Korotkov, et al. Effects of Pinacidil and Calcium on Succinate-Energized Rat Heart Mitochondria in the Presence of Rotenone

[2] Keisuke Iguchi, et al. Pinacidil, a KATP channel opener, stimulates cardiac Na +/Ca 2+ exchanger function through the NO/cGMP/PKG signaling pathway in guinea pig cardiac ventricular myocytes

[3] K E Andersson, et al. Effects of pinacidil on bladder muscle

[4] I Ahnfelt-Rnne. Pinacidil. Preclinical investigations

[5] H A Friedel, et al. Pinacidil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the treatment of hypertension

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Keywords: Pinacidil, P-1134 supplier, Potassium Channel, inhibitors, activators


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