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Enalapril is an anti-hypertension "prodrug" (i.e., a drug precursor) that is inactive until the ethyl ester (arrow in figure) is hydrolyzed by esterases present in blood plasma. The active drug is the dicarboxylic acid ("enalaprilat") that results from this hydrolysis reaction. ▾ Enalapril is administered in pill form, but enalaprilat must be administered intravenously. Why do you suppose enalapril works as a pill, but enalaprilat does not? Submit Part B O Enalaprilat has a larger mass than enalapril and cannot cross membranes to get from the gut to circulation. O Enalaprilat is not flexible enough to get into pores, whereas enalapril can cross membranes to get from the gut to circulation. O Enalaprilat has a larger size than enalapril and cannot cross membranes to get from the gut to circulation. O Enalaprilat is too polar to cross membranes, whereas enalapril can cross membranes to get from the gut to circulation. Request Answer μA K₁ = Value 7 Enalaprilat is a competitive inhibitor of the angiotensin-converting enzyme (ACE), which cleaves the blood-pressure regulating peptide angiotensin I. ACE has a KM = 52 M for angiotensin I, which is present in plasma at a concentration of 71 μM. When enalaprilat is present at 2.0 nM, the activity of ACE in plasma is 15% of its uninhibited activity. What is the value of K₁ for enalaprilat? Express your answer to two significant figures and include the appropriate units. PX? EtOOC Units -NH O B CH₂ N HOOC Enalapril

Enalapril is an anti-hypertension "prodrug" (i.e., a drug precursor) that is inactive until the ethyl ester (arrow in figure) is hydrolyzed by esterases present in blood plasma. The active drug is the dicarboxylic acid ("enalaprilat") that results from this hydrolysis reaction. ▾ Enalapril is administered in pill form, but enalaprilat must be administered intravenously. Why do you suppose enalapril works as a pill, but enalaprilat does not? Submit Part B O Enalaprilat has a larger mass than enalapril and cannot cross membranes to get from the gut to circulation. O Enalaprilat is not flexible enough to get into pores, whereas enalapril can cross membranes to get from the gut to circulation. O Enalaprilat has a larger size than enalapril and cannot cross membranes to get from the gut to circulation. O Enalaprilat is too polar to cross membranes, whereas enalapril can cross membranes to get from the gut to circulation. Request Answer μA K₁ = Value 7 Enalaprilat is a competitive inhibitor of the angiotensin-converting enzyme (ACE), which cleaves the blood-pressure regulating peptide angiotensin I. ACE has a KM = 52 M for angiotensin I, which is present in plasma at a concentration of 71 μM. When enalaprilat is present at 2.0 nM, the activity of ACE in plasma is 15% of its uninhibited activity. What is the value of K₁ for enalaprilat? Express your answer to two significant figures and include the appropriate units. PX? EtOOC Units -NH O B CH₂ N HOOC Enalapril

Biochemistry
Biochemistry
9th Edition
ISBN:9781319114671
Author:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
Publisher:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
Chapter1: Biochemistry: An Evolving Science
Section: Chapter Questions
Problem 1P
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Enalapril is an anti-hypertension "prodrug" (i.e., a drug precursor) that is inactive until the ethyl ester (arrow in figure) is hydrolyzed by esterases present in blood plasma. The active drug is the dicarboxylic acid ("enalaprilat") that results from this hydrolysis reaction. Enalapril is administered in pill form, but enalaprilat must be administered intravenously. Why do you suppose enalapril works as a pill, but enalaprilat does not? Enalaprilat has a larger mass than enalapril and cannot cross membranes to get from the gut to circulation. Enalaprilat is not flexible enough to get into pores, whereas enalapril can cross membranes to get from the gut to circulation. Enalaprilat has a larger size than enalapril and cannot cross membranes to get from the gut to circulation. Enalaprilat is too polar to cross membranes, whereas enalapril can cross membranes to get from the gut to circulation. Submit Part B K₁ = Request Answer Enalaprilat is a competitive inhibitor of the angiotensin-converting enzyme (ACE), which cleaves the blood-pressure regulating peptide angiotensin I. ACE has a KM = 52 μM for angiotensin I, which is present in plasma at a concentration of 71 μM. When enalaprilat is present at 2.0 nM, the activity of ACE in plasma is 15% of its uninhibited activity. What is the value of K₁ for enalaprilat? Express your answer to two significant figures and include the appropriate units. Submit HA Value EtOOC -NH O 33 CH3 HOOC Enalapril Request Answer Units
Transcribed Image Text:Enalapril is an anti-hypertension "prodrug" (i.e., a drug precursor) that is inactive until the ethyl ester (arrow in figure) is hydrolyzed by esterases present in blood plasma. The active drug is the dicarboxylic acid ("enalaprilat") that results from this hydrolysis reaction. Enalapril is administered in pill form, but enalaprilat must be administered intravenously. Why do you suppose enalapril works as a pill, but enalaprilat does not? Enalaprilat has a larger mass than enalapril and cannot cross membranes to get from the gut to circulation. Enalaprilat is not flexible enough to get into pores, whereas enalapril can cross membranes to get from the gut to circulation. Enalaprilat has a larger size than enalapril and cannot cross membranes to get from the gut to circulation. Enalaprilat is too polar to cross membranes, whereas enalapril can cross membranes to get from the gut to circulation. Submit Part B K₁ = Request Answer Enalaprilat is a competitive inhibitor of the angiotensin-converting enzyme (ACE), which cleaves the blood-pressure regulating peptide angiotensin I. ACE has a KM = 52 μM for angiotensin I, which is present in plasma at a concentration of 71 μM. When enalaprilat is present at 2.0 nM, the activity of ACE in plasma is 15% of its uninhibited activity. What is the value of K₁ for enalaprilat? Express your answer to two significant figures and include the appropriate units. Submit HA Value EtOOC -NH O 33 CH3 HOOC Enalapril Request Answer Units
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