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FPL 66564

FPL 66564 is a short-acting angiotensin-converting enzyme (ACE) inhibitor with an IC₅₀ of 5.7 nM against rabbit ACE. FPL 66564 inhibits ACE activity at the functional level and is hydrolyzed in human blood into inactive hydrophilic metabolites. FPL 66564 modulates angiotensin I-induced pressor responses in anesthetized rats, and its effects rapidly return to baseline after cessation of intravenous infusion. FPL 66564 can be used for research on cardiovascular regulation related to critical illness.

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CAS No.: 140369-78-4
Formule: C₈H₁₄O₄S₂
Masse moléculaire:238.32

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Please store the product under the recommended conditions in the Certificate of Analysis.

FPL 66564 Chemical Structure

CAS No.: 140369-78-4

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
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Activité biologique

Description

IC₅₀ & Target^[1]

ACE

5.7 nM (IC₅₀)

In Vitro

FPL 66564 is degraded in human blood with a half-life of 14 minutes to form inactive, small hydrophilic products^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

FPL 66564 (100-1000 nmoL/kg/min; i.v.; continuous infusion) rapidly achieves sustained, dose-dependent inhibition of angiotensin I pressor responses in urethane-anesthetized rats, with effects that rapidly dissipate after infusion cessation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Rat (anesthetized with urethane)^[2]
Dosage:

100 nmol/kg/min; 300 nmol/kg/min; 1000 nmol/kg/min
Administration:

i.v.; continuous infusion
Result:

Achieved rapid equilibrium of pressor response inhibition, followed by a sustained plateau.
Maintained ~90-95% inhibition of pressor response during infusion at 1000 nmol/kg/min dose.
Maintained ~75-80% inhibition during infusion at 300 nmol/kg/min dose.
Maintained ~60-65% inhibition during infusion at 100 nmol/kg/min dose.
Rapidly dissipated inhibitory effect on cessation of infusion, with all groups returning to near-baseline levels of inhibition (≤25%) by 60 minutes post-infusion.

Chemical Information

CAS No. 140369-78-4
Masse moléculaire 238.32
Formule C₈H₁₄O₄S₂
SMILES

SC[C@@H](C)C(O[C@H](C(O)=O)CSC)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Bodor N, et al. Soft drug design: general principles and recent applications. Med Res Rev. 2000;20(1):58-101. [Content Brief]

[2]. Baxter AJ, et al. (R)-2-(3-mercapto-2 (S)-methyl-1-oxopropoxy)-3-(methylthio) propanoic acid (FPL 66564), the first ultra-short-acting angiotensin converting enzyme inhibitor. Journal of medicinal chemistry. 1992 Oct;35(20):3718-20.

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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