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Zofenopril calcium

Cat. No. M3758
Zofenopril calcium Structure
Synonym:

SQ26991

Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 110  USD110 In stock
50mg USD 450  USD450 In stock
100mg USD 720  USD720 In stock
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Quality Control & Documentation
Biological Activity

Zofenopril is a long-lasting, lipophilic ACE inhibitor with cardioprotective properties indicated for the treatment of hypertension. Zofenopril is also an inhibitor of PEPT2, the predominant peptide transporter in kidney and choroid plexus. zofenopril increases SR calcium cycling and stimulates active calcium uptake into the SR. In small studies, zofenopril appeared significantly more effective than the older antihypertensives atenolol and enalapril, and was associated with fewer adverse effects.

Chemical Information
Molecular Weight 428.54
Formula C22H22NO4S2
CAS Number 81938-43-4
Solubility (25°C) DMSO ≥ 1 mg/mL (Need ultrasonic)
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] Frascarelli S, et al. J Cardiovasc Pharmacol. Effects of zofenopril on cardiac sarcoplasmic reticulum calcium handling.

[2] Ali Murat Kalender, et al. J Brachial Plex Peripher Nerve Inj. Effect of Zofenopril on regeneration of sciatic nerve crush injury in a rat model

[3] Lozano R, et al. J Pharm Biomed Anal. Temperature, pH and agitation rate as dissolution test discriminators of zofenopril calcium tablets.

[4] Morrison RA, et al. Pharm Res. Sites of first-pass bioactivation (hydrolysis) of orally administered zofenopril calcium in dogs.

[5] A. Subissi, et al. Cardiovascular Drug Reviews. Preclinical Profile of Zofenopril: An Angiotensin Converting Enzyme Inhibitor with Peculiar Cardioprotective Properties

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