Picotamide monohydrate
Picotamide monohydrate is an orally active TXA2 receptor and TXA2 synthase inhibitor. Picotamide monohydrate inhibits ADP (HY-W010918)-, Arachidonic acid (HY-109590)-, and Collagen (HY-NP003)-induced platelet aggregation, reduces TXA2 production during coagulation, and does not inhibit PGI2 synthesis in endothelial cells. Picotamide monohydrate inhibits contractions induced by α1-adrenergic receptor agonism, TXA2 mediation, and neurogenic (electrical field stimulation-induced) factors in human prostatic smooth muscle, and broadly inhibits agonist-induced contractions of porcine interlobar renal and coronary arteries. Picotamide monohydrate can be used in research related to thromboembolic diseases, atherosclerosis, and lower urinary tract symptoms.
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- No. CAS: 80530-63-8
- Fòrmula: C21H22N4O4
- Peso molecular:394.42
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
TXA2/TP |
In Vitro
Picotamide (10-80 μM; 48 h) monohydrate decreased the cell viability of L929 cells in a dose-dependent manner[1].
Picotamide (10-100 μM; 48 h) monohydrate exhibits dose-dependent cytotoxicity against L929 mouse fibroblasts[4].
Picotamide (3 μM) monohydrate inhibits α1-adrenergic contractions in human prostatic tissue strips when cyclooxygenase activity is blocked by Indomethacin (HY-14397)[3].
Picotamide monohydrate inhibits EFS-induced contraction in human prostate tissue[3].
Picotamide (0.325-1.3 μM; 2 min) monohydrate exhibited antiplatelet aggregation activity in rabbit PRP, with an IC50 value of 0.47 μM for ADP-induced aggregation and an IC50 value of 0.34 μM for AA-induced aggregation[4].
Picotamide (300 μM; 30 min) monohydrate inhibited U46619-induced contraction of porcine renal interlobar arteries without a rightward shift or a significant increase in EC50 values[5].
Picotamide (300 μM; 30 min) monohydrate competitively inhibits Noradrenaline (HY-13715)-, Phenylephrine (HY-B0769)-, and Methoxamine (HY-B1298A)-induced contraction of porcine renal interlobar arteries, increasing EC50 without affecting Emax[5].
Picotamide (300 μM; 30 min) monohydrate inhibits Serotonin (HY-B1473A)-induced contraction in porcine renal interlobar arteries, characterized by a rightward shift and an increase in EC50[5].
Picotamide (300 μM; 30 min) monohydrate inhibits α,β-methylene-ATP (HY-134440A)-induced contraction of porcine renal interlobar arteries at high agonist concentrations[5].
Picotamide (300 μM; 30 min) monohydrate has minimal effect on weak ATP (HY-B2176)-induced contraction in porcine renal interlobar arteries[5].
Picotamide (300 μM; 30 min) monohydrate inhibits Angiotensin-II-induced contraction of porcine renal interlobar arteries without a significant change in EC50[5].
Picotamide (300 μM; 30 min) monohydrate inhibits Endothelin-1 (HY-P0202)-induced contraction in porcine renal interlobar arteries[5].
Picotamide (300 μM; 30 min) monohydrate inhibited U46619 (HY-108566)-induced contraction of porcine coronary arteries, without a rightward shift or a significant increase in EC50 values[5].
Picotamide (300 μM; 30 min) monohydrate inhibits Phenylephrine-induced contraction of porcine coronary arteries, without competitive characteristics or changes in EC50[5].
Picotamide (300 μM; 30 min) monohydrate inhibits Methoxamine-induced contraction of porcine coronary arteries without competitive characteristics or a significant change in EC50[5].
Picotamide (300 μM; 30 min) monohydrate inhibited Methacholine-induced contraction in porcine coronary arteries without causing consistent changes in EC50[5].
Picotamide (300 μM; 30 min) monohydrate inhibits Carbachol (HY-B1208)-induced contraction in porcine coronary arteries, with no consistent change in EC50[5].
Picotamide (300 μM; 30 min) monohydrate inhibits Serotonin-induced contraction in porcine coronary arteries, manifested as a rightward shift and an increase in EC50[5].
Picotamide (300 μM; 30 min) monohydrate inhibits Angiotensin-II-induced contraction in porcine coronary arteries without a significant change in EC50[5].
Picotamide (300 μM; 30 min) monohydrate inhibits Endothelin-1-induced contraction in porcine coronary arteries[5].
Picotamide (30-300 μM; 30 min) monohydrate dose-dependently inhibited EFS-induced contractions in porcine renal interlobar arteries without affecting Ef50[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L929
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Concentration:10, 20, 40, 80 μM
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Incubation Time:48 h
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Result:Reduced cell survival rates to 81.38% at 10 μM, 69.31% at 20 μM, 55.17% at 40 μM, and 40.69% at 80 μM.
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Cell Line:L929 mouse fibroblast cells
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Concentration:10 μM; 100 μM
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Incubation Time:48 h
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Result:Resulted in a cell survival rate of 55.56% with an average absorbance of 0.126 at 10 μM.
Resulted in a cell survival rate of 44.44% with an average absorbance of 0.125 at 100 μM.
Chemical Information
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No. CAS 80530-63-8
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Peso molecular 394.42
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Fòrmula C21H22N4O4
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SMILES
O=C(C1=CC=C(OC)C(C(NCC2=CC=CN=C2)=O)=C1)NCC3=CC=CN=C3.O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Picotamide monohydrate Related Classifications
HY-B1735A Related Classifications
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