1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)

ICI 153110 

Cat. No.: HY-100239
Handling Instructions

ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.

For research use only. We do not sell to patients.

ICI 153110 Chemical Structure

ICI 153110 Chemical Structure

CAS No. : 87164-90-7

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1 mg USD 375 Get quote
5 mg USD 601 Get quote
10 mg USD 961 Get quote

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.

IC50 & Target

Phosphodiesterase[1]

In Vivo

ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure. Fourteen animals have died as a direct or indirect consequence of ICI 153110 administration in the high-dose main test and reversibility groups. In the female rat dosed at 10 mg/kg/day ICI 153110 a mild focal arteritis is characterized by a predominantly and diffusely adventitial infiltration of mixed cells and early formation of fibrous tissue. The two rats dosed at 250 mg/kg/day ICI 153110 die prematurely from intratracheal intubation of dosing solution. Arteries from two further animals (dosed at 5 and 250 mg/kg/day ICI 153110) show minimal focal arteritis with medial necrosis, and medial and adventitial inflammation[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.9697 mL 24.8484 mL 49.6968 mL
5 mM 0.9939 mL 4.9697 mL 9.9394 mL
10 mM 0.4970 mL 2.4848 mL 4.9697 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Alderley Park APfSD rats are used in this study. In all, 150 male rats and 150 female rats are assigned to four groups (one control and three treatment) in the two separate studies; 30 per sex representing the main (regular) test groups and 15 per sex for investigating reversibility of effects following treatment at the highest dose employed (withdrawal studies). The dose levels are 5, 10, and 250 mg/kg/day of ICI 153110. All animals are dosed orally, by gavage, using a plastic syringe and a flexible catheter. Equal numbers of animals per sex in the four groups are necropsied necropsied at each of two time points; following at least 28 consecutive days dosing (1 month) and 182 consecutive days of dosing (6 months). All animals are observed at least twice daily for any abnormal signs, all of which are recorded. Body weights, food consumption, water consumption, clinical pathology, and pharmacokinetics are also measured[1].

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

References
Molecular Weight

201.22

Formula

C₁₁H₁₁N₃O

CAS No.

87164-90-7

SMILES

O=C1CCC(/C=C/C2=CC=NC=C2)=NN1

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
ICI 153110
Cat. No.:
HY-100239
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ICI 153110

Cat. No.: HY-100239