Epirizole

Modify Date: 2024-01-06 16:20:32

Epirizole Structure
Epirizole structure
Common Name Epirizole
CAS Number 18694-40-1 Molecular Weight 234.25400
Density 1.25g/cm3 Boiling Point 444ºC at 760mmHg
Molecular Formula C11H14N4O2 Melting Point 90 - 92ºC
MSDS Chinese USA Flash Point 222.3ºC
Symbol GHS07
GHS07
Signal Word Warning

 Use of Epirizole


Epirizole (Mepirizole) is an orally active NSAID (nonsteroidal anti-inflammatory drug). Epirizole shows anti-inflammatory activity, and can be used in chronic rheumatoid arthritis research[1].

 Names

Name 4-methoxy-2-(5-methoxy-3-methylpyrazol-1-yl)-6-methylpyrimidine
Synonym More Synonyms

 Epirizole Biological Activity

Description Epirizole (Mepirizole) is an orally active NSAID (nonsteroidal anti-inflammatory drug). Epirizole shows anti-inflammatory activity, and can be used in chronic rheumatoid arthritis research[1].
Related Catalog
In Vitro Epirizole (1-1000 μM; 24 h) increases MDR1 mRNA expression in Caco-2 cells[1]. RT-PCR[1] Cell Line: Caco-2 cells Concentration: 1, 10, 100, and 1000 μM Incubation Time: 24 hours Result: Increased the level of MDR1 mRNA expression.

 Chemical & Physical Properties

Density 1.25g/cm3
Boiling Point 444ºC at 760mmHg
Melting Point 90 - 92ºC
Molecular Formula C11H14N4O2
Molecular Weight 234.25400
Flash Point 222.3ºC
Exact Mass 234.11200
PSA 62.06000
LogP 1.29630
Vapour Pressure 0mmHg at 25°C
Index of Refraction 1.601
Storage condition 2-8°C

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UV9290000
CHEMICAL NAME :
Pyrimidine, 4-methoxy-2-(5-methoxy-3-methyl-1H-pyrazol-1-yl)-6-me thyl-
CAS REGISTRY NUMBER :
18694-40-1
BEILSTEIN REFERENCE NO. :
0751084
LAST UPDATED :
199612
DATA ITEMS CITED :
9
MOLECULAR FORMULA :
C11-H14-N4-O2
MOLECULAR WEIGHT :
234.29
WISWESSER LINE NOTATION :
T6N CNJ B- AT5NNJ C1 EO1& DO1 F1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
445 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMGZAI Japan Medical Gazette. (Tokyo, Japan) V.1-18(?), 1964-81. Discontinued. Volume(issue)/page/year: 7(9),5,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
214 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMGZAI Japan Medical Gazette. (Tokyo, Japan) V.1-18(?), 1964-81. Discontinued. Volume(issue)/page/year: 7(9),5,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
208 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 8,494,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
214 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
85IRAK "Modern Pharmaceuticals of Japan, V," Tokyo, Japan Pharmaceutical, Medical and Dental Supply Exporters' Assoc., 1975 Volume(issue)/page/year: -,87,1975
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
740 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 16,1011,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
540 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 16,1011,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
550 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 8,494,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
550 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMGZAI Japan Medical Gazette. (Tokyo, Japan) V.1-18(?), 1964-81. Discontinued. Volume(issue)/page/year: 7(9),5,1970 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
45500 mg/kg/26W-C
TOXIC EFFECTS :
Gastrointestinal - changes in structure or function of salivary glands Liver - changes in liver weight Endocrine - changes in adrenal weight
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 8,524,1977

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H312-H315-H319-H332-H335
Precautionary Statements P261-P280-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes Xn:Harmful;
Risk Phrases R20/21/22;R36/37/38
Safety Phrases S26-S36
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS UV9290000
HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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Role of active oxygen species and lipid peroxidation in mepirizole-induced duodenal ulcers in rats.

Dig. Dis. Sci. 43(8) , 1657-64, (1998)

The role of active oxygen species and lipid peroxidation in the pathogenesis of duodenal ulcers induced by mepirizole was investigated in rats. Oral administration of mepirizole (200 mg/kg) resulted i...

Tobacco cigarette smoke attenuates duodenal ulcer margin hyperemia in the rat. Comparison of IAP clearance and hydrogen gas clearance techniques for measurements of gastrointestinal blood flow.

Dig. Dis. Sci. 40(5) , 1112-7, (1995)

The hyperemia at the duodenal ulcer margin is important for ulcer healing. We studied the effect of tobacco cigarette smoke on the hyperemia at the margin of mepirizole-induced duodenal ulcer. Duodena...

 Synonyms

Mebron
Epirizolum [INN-Latin]
Mepirizole
Mepirizol [German]
4-methoxy-2-(5-methoxy-3-methyl-pyrazol-1-yl)-6-methyl-pyrimidine
1-(4-Methyl-6-methoxy-pyrimidin-2-yl)-3-methyl-5-methoxy-pyrazol
DA-398
Methopyrimazole
4-methoxy-2-(5-methoxy-3-methyl-1H-pyrazol-1-yl)-6-methylpyrimidine
Epirizol [INN-Spanish]
EINECS 242-507-1
epirizole
MFCD00057351
1-(4-Methoxy-6-methyl-2-pyrimidinyl)-3-methyl-5-methoxy-pyrazol
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