Zomepirac
Zomepirac (McN-2783-21-98 free acid) is an orally active prostaglandin synthetase inhibitor. Zomepirac blocks prostaglandin synthesis and inhibits Collagen (HY-P72147)- or Epinephrine (HY-B0447)-induced platelet aggregation. Zomepirac can be used for the research of postoperative pain and osteoarthritis.
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- CAS No.: 33369-31-2
- Formule: C15H14ClNO3
- Masse moléculaire:291.73
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Zomepirac potently inhibits prostaglandin synthesis in homogenised bovine seminal vesicles[3].
Zomepirac potently inhibits Collagen (HY-NP003)-induced aggregation of human platelets in vitro[3].
Zomepirac (0.1-10 μg/mL) is 98.5% bound to human plasma albumin in vitro[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Zomepirac (5 mg/kg; p.o.; 3 times daily; 3 days) shows no physical dependence liability in the mouse Naloxone (HY-17417A) challenge jumping test[3].
Zomepirac (p.o.) exhibits potent acute anti-inflammatory activity in the Carrageenan (HY-125474)-induced paw oedema test in rats, with an oral ED50 of 0.15 mg/kg[3].
Zomepirac (p.o.) exhibits anti-inflammatory activity in the acute adjuvant-induced arthritis test in rats, with an oral ED50 of 3.9 mg/kg[3].
Zomepirac (p.o.) exhibits analgesic activity in the chronic adjuvant-induced arthritis test in rats, with an oral ED50 of 16.6 mg/kg[3].
Zomepirac (p.o.) has ulcerogenic activity in Rattus norvegicus rats, with an oral median ulcerogenic dose (UD50) of 13.9 mg/kg[3].
Zomepirac (0.3-3 mg/kg; i.v.) reduces cerebrospinal fluid prostaglandin E2 concentrations by ~96% in conscious cats, with effects lasting up to 5 days[3].
Zomepirac (2-6 mg/kg; i.v.) substantially reduces spinothalamic tract cell responses to nociceptive stimuli in anaesthetised rhesus monkeys[3].
Zomepirac (20 mg/kg; i.v.) has minimal impact on renal haemodynamics and function in anaesthetised rhesus monkeys[3].
Zomepirac (10-40 mg/kg; p.o.; daily; 12 months) causes interstitial nephritis in monkeys[3].
Zomepirac (p.o.; daily; 24 months) increases the incidence of adrenal tumours and hyperplasia in rats[3].
Zomepirac (p.o.; daily; 18 months) does not cause carcinogenicity in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice (Naloxone challenge jumping model)[3]
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Dosage:5 mg/kg
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Administration:p.o.; 3 times daily; 3 days
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Result:Showed no jumping after naloxone challenge, whereas morphine-pretreated mice showed significant jumping behavior.
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Animal Model:Cats[3]
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Dosage:0.3 mg/kg; 3 mg/kg
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Administration:i.v.
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Result:Reduced cerebrospinal fluid immunoreactive prostaglandin E2 concentrations by approximately 96%.
Concentrations remained depressed for up to 5 days and returned to control values within 7 days.
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Animal Model:Monkeys[3]
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Dosage:2 mg/kg; 6 mg/kg
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Administration:i.v.
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Result:Produced a substantial reduction in spinothalamic tract cell responses to mechanical, thermal, and algesic chemical stimuli.
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Animal Model:Monkeys[3]
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Dosage:20 mg/kg
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Administration:i.v.
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Result:Had little effect on renal blood flow, and no effect on inulin clearance or urinary excretion of sodium and potassium.
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Animal Model:Monkeys[3]
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Dosage:10 mg/kg; 40 mg/kg
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Administration:p.o.; daily for 12 months
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Result:Caused multifocal nephritis characterised by interstitial scarring at 40 mg/kg daily; caused milder interstitial nephritis and oedema at 10 mg/kg daily.
Chemical Information
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CAS No. 33369-31-2
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Masse moléculaire 291.73
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Formule C15H14ClNO3
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SMILES
O=C(O)CC1=CC(C)=C(C(C2=CC=C(Cl)C=C2)=O)N1C
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Synonyms
McN-2783-21-98 free acid
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Zomepirac Related Classifications
HY-B0890A Related Classifications
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