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.
For research use only. We do not sell to patients.
- CAS No.: 80530-63-8
- Formula: C21H22N4O4
- Molecular Weight:394.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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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CAS No. 80530-63-8
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Molecular Weight 394.42
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Picotamide monohydrate Related Classifications
HY-B1735A Related Classifications
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