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ChemicalBook >> CAS DataBase List >>MF-63

MF-63

CAS No.
892549-43-8
Chemical Name:
MF-63
Synonyms
MF-63;CS-2773;MF 63; MF-63;2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-1,3-Benzenedic;2-(6-chloro-1H-phenanthro-[9,10-d]iMidazol-2-yl)isophthalonitrile;2-(9-Chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-1,3-benzenedicarbonitrile;2-(9-Chloro-1H-phenanthro[9, 10-d]imidazol-2-yl)benzene-1, 3-dicarbonitrile;1,3-Benzenedicarbonitrile, 2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-
CBNumber:
CB22512521
Molecular Formula:
C23H11ClN4
Molecular Weight:
378.81
MDL Number:
MFCD18384972
MOL File:
892549-43-8.mol
MSDS File:
SDS
Last updated:2024-07-02 08:55:03

MF-63 Properties

Boiling point 709.7±70.0 °C(Predicted)
Density 1.49
storage temp. Store at -20°C
solubility Soluble in DMSO
form crystalline solid
pka 11.34±0.30(Predicted)
color Light yellow to yellow
FDA UNII 7TU641M876

MF-63 price More Price(18)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 13217 MF63 ≥98% 892549-43-8 1mg $34 2024-03-01 Buy
Cayman Chemical 13217 MF63 ≥98% 892549-43-8 5mg $100 2024-03-01 Buy
Cayman Chemical 13217 MF63 ≥98% 892549-43-8 10mg $183 2024-03-01 Buy
Cayman Chemical 13217 MF63 ≥98% 892549-43-8 25mg $371 2024-03-01 Buy
Usbiological 456183 MF 63 892549-43-8 5mg $368 2021-12-16 Buy
Product number Packaging Price Buy
13217 1mg $34 Buy
13217 5mg $100 Buy
13217 10mg $183 Buy
13217 25mg $371 Buy
456183 5mg $368 Buy

MF-63 Chemical Properties,Uses,Production

Description

Microsomal prostaglandin E2 synthase-1 (mPGES-1) is the terminal enzyme in the biosynthesis of PGE2. MF63 is a potent, selective, and orally active inhibitor of human mPGES-1 (IC50 = 1.3 nM). It displays greater than 1,000-fold selectivity over other prostanoid synthases. MF63 also potently inhibits guinea pig mPGES-1 (IC50 = 0.9 nM) but not mouse or rat mPGES-1. In guinea pigs or in mice expressing human mPGES-1, MF63 prevents LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain. It does not produce the gastrointestinal toxicity that is caused by non-selective COX inhibitors, although it markedly suppresses PGE2 synthesis in the stomach.

Uses

MF 63 is a microsomal prostaglandin E2 synthase-1 (mPGES-1) the final enzyme in the synthesis of PGE2. Prevents LPS-induced hyperglasia. Anti-inflammatory, analgesic, anti-cancer agent.

in vitro

mf63 was found to be significantly more potent than those previously reported mpges-1 inhibitors with an intrinsic inhibitory potency on the recombinant human mpges-1 enzyme. furthermore, mf63 showed a pge2 whole cell inhibition in a549 cells and a human whole blood activity [1].

in vivo

in rodent species, mf63 inhibited guinea pig mpges-1 strongly but not the mouse or rat enzyme. when tested in the guinea pig and a knock-in (ki) mouse expressing human mpges-1, mf63 suppressed the synthesis of pge2 selectively, but not other prostaglandins that were inhibitable by nonsteroidal anti-inflammatory drugs (nsaid), yet remaided nsaid-like efficacy at inhibiting lipopolysaccharide-induced hyperalgesia, pyresis, and iodoacetate-induced osteoarthritic pain. additionally, mf63 did not cause nsaid-like gastrointestinal toxic effects, such as mucosal erosions or leakage in the ki mice or nonhuman primates, although mf63 markedly inhibited pge2 synthesis in the ki mouse stomach [1].

IC 50

0.9 and 1.3 nm for pig mpges-1 and human mpges-1

References

[1] xu d,rowland se,clark p,giroux a,cté b,guiral s,salem m,ducharme y,friesen rw,méthot n,mancini j,audoly l,riendeau d. mf63 [2-(6-chloro-1h-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a selective microsomal prostaglandin e synthase-1 inhibitor, relieves pyresis and pain in preclinical models of inflammation. j pharmacol exp ther.2008 sep;326(3):754-63.

MF-63 Preparation Products And Raw materials

Raw materials

Preparation Products

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CONIER CHEM AND PHARMA LIMITED
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MF-63 2-(9-Chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-1,3-benzenedicarbonitrile 2-(6-chloro-1H-phenanthro-[9,10-d]iMidazol-2-yl)isophthalonitrile 2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-1,3-Benzenedic MF 63; MF-63 CS-2773 1,3-Benzenedicarbonitrile, 2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)- 2-(9-Chloro-1H-phenanthro[9, 10-d]imidazol-2-yl)benzene-1, 3-dicarbonitrile 892549-43-8 C23H11ClN4