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
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)
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 |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/6141286Curator'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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6141286
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
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1827 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8120866 |
500.0 nM [IC50] | ||
Target ID: CHEMBL2094125 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2985781 |
16000.0 nM [Ki] | ||
Target ID: CHEMBL2095150 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2985781 |
9500.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/1981187
Male Wistar rats were treated with MY-5445 (50 mkg/paw) as a single dose.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6141286
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
Edited
Sat Dec 16 04:48:54 UTC 2023
by
admin
on
Sat Dec 16 04:48:54 UTC 2023
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Record UNII |
F8CSS73B6A
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Record Status |
Validated (UNII)
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Record Version |
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DTXSID70229009
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MY-5445
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1348
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