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Details

Stereochemistry ACHIRAL
Molecular Formula C20H14ClN3
Molecular Weight 331.798
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MY-5445

SMILES

ClC1=CC(NC2=NN=C(C3=CC=CC=C3)C4=CC=CC=C24)=CC=C1

InChI

InChIKey=CEHQLKSLMFIHBF-UHFFFAOYSA-N
InChI=1S/C20H14ClN3/c21-15-9-6-10-16(13-15)22-20-18-12-5-4-11-17(18)19(23-24-20)14-7-2-1-3-8-14/h1-13H,(H,22,24)

HIDE SMILES / InChI

Molecular Formula C20H14ClN3
Molecular Weight 331.798
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: The description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/8120866 | https://www.ncbi.nlm.nih.gov/pubmed/2985781 | https://www.ncbi.nlm.nih.gov/pubmed/2480168 | https://www.ncbi.nlm.nih.gov/pubmed/17606845

MY-5445 is specific inhibitor of cyclic GMP phosphodiesterase with potent platelet anti-aggregation activity. MY-5445 significantly elevated cyclic GMP content in human plateıts but had no effect on cyclic AMP content, suggesting that the drug affects principally the cyclic GMP metabolism in the platelet. MY-5445 significantly increases contractility, measured in the perfused heart and isolated cardiomyocytes, in hypertrophied right ventricle (RVH) but not normal right ventricle (RV).

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
500.0 nM [IC50]
16000.0 nM [Ki]
9500.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
PubMed

PubMed

TitleDatePubMed
Cyclic GMP mediates apoptosis induced by sulindac derivatives via activation of c-Jun NH2-terminal kinase 1.
2000 Oct
Patents

Patents

Sample Use Guides

Male Wistar rats were treated with MY-5445 (50 mkg/paw) as a single dose.
Route of Administration: Other
In Vitro Use Guide
Human citrated PRP containing 5 x 10^6 platelets/mkl was prepared from blood obtained from healthy volunteers. The effect of MY-5445 on platelet aggregation was studied by the turbidimetric method, with an aggregation meter (RAM41; Rikadenki Kogyo Co., Ltd., Japan). MY-5445 (5 mkl) was added to 0.25 ml of PRP and incubated at 37’C with stirring for 2 mm before the addition of aggregating agents (25 zl of collagen, ADP or arachidonic acid). Final concentrations ofeach aggregating agents were 3 mkM ADP, 3 mkg/ml collagen and 100 mkg/ml arachidonic acid. The extent of aggregation was expressed by the maximum change of light transmission for PRP and platelet-poor plasma as a value of 100%. The percent inhibition of aggregation by the test compounds was calculated by dividing the percent aggreıtion in the presence of the test compound by that observed in the control run, and multiplying by 100.
Substance Class Chemical
Created
by admin
on Sat Dec 16 04:48:54 UTC 2023
Edited
by admin
on Sat Dec 16 04:48:54 UTC 2023
Record UNII
F8CSS73B6A
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MY-5445
Common Name English
1-PHTHALAZINAMINE, N-(3-CHLOROPHENYL)-4-PHENYL-
Systematic Name English
Code System Code Type Description
FDA UNII
F8CSS73B6A
Created by admin on Sat Dec 16 04:48:55 UTC 2023 , Edited by admin on Sat Dec 16 04:48:55 UTC 2023
PRIMARY
CAS
78351-75-4
Created by admin on Sat Dec 16 04:48:55 UTC 2023 , Edited by admin on Sat Dec 16 04:48:55 UTC 2023
PRIMARY
EPA CompTox
DTXSID70229009
Created by admin on Sat Dec 16 04:48:55 UTC 2023 , Edited by admin on Sat Dec 16 04:48:55 UTC 2023
PRIMARY
WIKIPEDIA
MY-5445
Created by admin on Sat Dec 16 04:48:55 UTC 2023 , Edited by admin on Sat Dec 16 04:48:55 UTC 2023
PRIMARY
PUBCHEM
1348
Created by admin on Sat Dec 16 04:48:55 UTC 2023 , Edited by admin on Sat Dec 16 04:48:55 UTC 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY