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Spirapril hydrochloride

Cat. No. M30960
Spirapril hydrochloride Structure
Synonym:

SCH 33844 hydrochloride

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Biological Activity

Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure.

Chemical Information
Molecular Weight 503.07
Formula C22H31ClN2O5S2
CAS Number 94841-17-5
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
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] Ramón C Hermida, et al. Chronobiol Int. Administration-time-dependent effects of spirapril on ambulatory blood pressure in uncomplicated essential hypertension

[2] Michael Schürer, et al. Arzneimittelforschung. Drug interaction of spirapril hydrochloride monohydrate and hydrochlorothiazide. A clinical study to compare the pharmacokinetics after administration of spirapril hydrochloride monohydrate tablets, hydrochlorothiazide tablets and fixed combination bi-lay䲧癐Ỵ癑㧀

[3] K Hayduk, et al. J Cardiovasc Pharmacol. Efficacy and safety of spirapril in mild-to-moderate hypertension

[4] C Guitard, et al. Cardiovasc Drugs Ther. Comparison of efficacy of spirapril and enalapril in control of mild-to-moderate hypertension

[5] S Noble, et al. Drugs. Spirapril. A preliminary review of its pharmacology and therapeutic efficacy in the treatment of hypertension

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Keywords: Spirapril hydrochloride, SCH 33844 hydrochloride supplier, ACE, inhibitors, activators


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