2. Immunology/Inflammation
  3. PGE synthase
  4. 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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Zomepirac

Zomepirac Chemical Structure

CAS No. : 33369-31-2

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Zomepirac Related Antibodies

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Description

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[1][2][3][4].

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.

Zomepirac Related Antibodies
In Vivo

Zomepirac (p.o.) exhibits potent non-narcotic analgesic activity in the Acetylcholine-induced writhing test in mice, with an oral ED50 of 0.84 mg/kg, and lacks narcotic-like activity in mouse tail pinch and hot plate tests[3].
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.

Animal Model: Mice (Naloxone challenge jumping model)[3]
Dosage: 5 mg/kg
Administration: p.o.; 3 times daily; 3 days
Result: Showed no jumping after naloxone challenge, whereas morphine-pretreated mice showed significant jumping behavior.
Animal Model: Cats[3]
Dosage: 0.3 mg/kg; 3 mg/kg
Administration: i.v.
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.
Animal Model: Monkeys[3]
Dosage: 2 mg/kg; 6 mg/kg
Administration: i.v.
Result: Produced a substantial reduction in spinothalamic tract cell responses to mechanical, thermal, and algesic chemical stimuli.
Animal Model: Monkeys[3]
Dosage: 20 mg/kg
Administration: i.v.
Result: Had little effect on renal blood flow, and no effect on inulin clearance or urinary excretion of sodium and potassium.
Animal Model: Monkeys[3]
Dosage: 10 mg/kg; 40 mg/kg
Administration: p.o.; daily for 12 months
Result: Caused multifocal nephritis characterised by interstitial scarring at 40 mg/kg daily; caused milder interstitial nephritis and oedema at 10 mg/kg daily.
Molecular Weight

291.73

Formula

C15H14ClNO3
CAS No.
SMILES

O=C(O)CC1=CC(C)=C(C(C2=CC=C(Cl)C=C2)=O)N1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Zomepirac Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zomepirac33369-31-2McN-2783-21-98PGE synthaseProstaglandin E synthasemiceopiate receptorsratsprostaglandin synthetaseprostaglandin synthesishuman serum albuminhuman plasma albuminplatelet aggregationacyl glucuronide metabolitesrhesus monkeysInhibitorinhibitorinhibit

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