Amtolmetin guacil

Names

[ Name ]:
Amtolmetin guacil

[Synonym ]:
2-Methoxyphenyl N-{[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetyl}glycinate
amtolmetin guacil
Glycine, N-[2-[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetyl]-, 2-methoxyphenyl ester
MFCD00866153

Biological Activity

[Description]:

Amtolmetin guacil is an effective nonsteroidal anti-Inflammatory agent with pain-relieving effects. Amtolmetin guacil inhibits prostaglandin synthesis and cyclooxygenase (COX). Amtolmetin guacil can stimulate capsaicin receptors present on the gastrointestinal wall and also releases gastroprotective nitric oxide (NO). Amtolmetin guacil can be used to research knee osteoarthritis[1][2].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> NO Synthase

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Immunology/Inflammation >> COX

[Target]

Prostaglandin receptor, COX, NO[1][2]

[In Vitro]

Amtolmetin guacil (100 μM; 0-60 min) converts to TMT (Tolmetin, HY-B1799) along with MED5 (1-methyl-5-p-methylbenzoyl-pyrrol-2-acetamido aceticacid) in rat fresh plasma and rat liver microsomal, rapidly converts to MED5 and MED5 methyl ester without yielding TMT in human fresh plasma and human liver microsomes[3].

[In Vivo]

Animal Model: Male Wistar rats[3] Dosage: 50 mg/kg Administration: p.o.; single dosage Result: Pharmacokinetic Parameters of Amtolmetin guacil in male Wistar rats[3]. AUC0-t (ng/mL·h) AUC0-∞ (ng/mL·h) Cmax (μg/mL) Tmax (h) Kel (h-1) t1/2,β (h) TMT followingAmtolmetin guacil dosing 162 ± 21.49 164 ± 22.47 81.62 ± 5.02 0.50 ± 0.00 0.28 ± 0.00 2.41 ± 0.01

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
663.3±55.0 °C at 760 mmHg

[ Melting Point ]:
117-120ºC

[ Molecular Formula ]:
C₂₄H₂₄N₂O₅

[ Molecular Weight ]:
420.458

[ Flash Point ]:
354.9±31.5 °C

[ Exact Mass ]:
420.168518

[ PSA ]:
86.63000

[ LogP ]:
1.98

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.583

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MC0598400

CHEMICAL NAME :: Glycine, N-((1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl)acety l)-, 2-methoxyphenyl ester

CAS REGISTRY NUMBER :: 87344-06-7

LAST UPDATED :: 199512

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C24-H24-N2-O5

MOLECULAR WEIGHT :: 420.50

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 :: 1450 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2115417

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2115417

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2115417

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1370 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2115417

Safety Information

[ Hazard Codes ]:
Xi