MF498 - CAS 915191-42-3
Catalog number:
915191-42-3
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C32H33N3O7S
Molecular Weight:
603.69
COA:
Inquire
Targets:
Prostaglandin Receptor
Description:
MF498 is a novel and selective E prostanoid receptor 4 (EP4 receptor) antagonist, a Gs protein-coupled receptor, with Ki of 0.7 nM. It plays important roles in bone formation and resorption, inflammation, cancer, and atherosclerosis. It has been shown to inhibit inflammation without gastrointestinal toxicity in various animal models for arthritis. It also displays a relatively good selectivity over other prostanoid receptors. It does not compromise the mucosal integrity in the gastrointestinal tract in vitro. It inhibits PGE2-stimulated cAMP accumulation in a dose-dependent manner. It relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis in vivo.
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
Appearance:
Light yellow to yellow Solid
Synonyms:
MF-498;N-[[[4-(5,9-Diethoxy-6,8-dihydro-6-oxo-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylphenyl]methyl]sulfonyl]-2-methoxy-benzeneacetamide;N-[[4-(5,9-diethoxy-6-oxo-8H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylphenyl]methylsulfonyl]-2-(2-methoxyphenyl)acetamide
Solubility:
DMSO: ≥ 31 mg/mL
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
MF498 plays important roles in bone formation and resorption, inflammation, cancer, and atherosclerosis. It has been shown to inhibit inflammation without gastrointestinal toxicity in various animal models for arthritis. It relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis in vivo.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Density:
1.324±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
WVLIUERFVJYBNY-UHFFFAOYSA-N
InChI:
InChI=1S/C32H33N3O7S/c1-5-41-30-23-11-9-15-33-29(23)31(42-6-2)24-18-35(32(37)28(24)30)25-14-13-21(16-20(25)3)19-43(38,39)34-27(36)17-22-10-7-8-12-26(22)40-4/h7-16H,5-6,17-19H2,1-4H3,(H,34,36)
Canonical SMILES:
CCOC1=C2CN(C(=O)C2=C(C3=C1N=CC=C3)OCC)C4=C(C=C(C=C4)CS(=O)(=O)NC(=O)CC5=CC=CC=C5OC)C
1.MF498 [N-{[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and os
Clark P1, Rowland SE, Denis D, Mathieu MC, Stocco R, Poirier H, Burch J, Han Y, Audoly L, Therien AG, Xu D. J Pharmacol Exp Ther. 2008 May;325(2):425-34. doi: 10.1124/jpet.107.134510. Epub 2008 Feb 20.
Previous evidence has implicated E prostanoid receptor 4 (EP4) in mechanical hyperalgesia induced by subplantar inflammation. However, its role in chronic arthritis remains to be further defined because previous attempts have generated two conflicting lines of evidence, with one showing a marked reduction of arthritis induced by a collagen antibody in mice lacking EP4, but not EP1-EP3, and the other showing no impact of EP4 antagonism on arthritis induced by collagen. Here, we assessed the effect of a novel and selective EP4 antagonist MF498 [N-{[4-(5,9-diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide] on inflammation in adjuvant-induced arthritis (AIA), a rat model for rheumatoid arthritis (RA), and joint pain in a guinea pig model of iodoacetate-induced osteoarthritis (OA). In the AIA model, MF498, but not the antagonist for EP1, MF266-1 [1-(5-{3-[2-(benzyloxy)-5-chlorophenyl]-2-thienyl}pyridin-3-yl)-2,2,2-trifluoroethane-1,1-diol] or EP3 MF266-3 [(2E)-N-[(5-bromo-2-methoxyphenyl)sulfonyl]-3-[5-chloro-2-(2-naphthylmethyl)phenyl]acrylamide], inhibited inflammation, with a similar efficacy as a selective cyclooxygenase 2 (COX-2) inhibitor MF-tricyclic.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Prostaglandin Receptor Products


Omidenepag
(CAS: 1187451-41-7)

This active molecular is a prostaglandin receptor agonist and detailed information has not been published yet.

GSK-345931A sodium
(CAS: 869499-38-7)

GSK-345931A is an EP(1) receptor antagonist. It is efficient in preclinical models of inflammatory pain.

Fevipiprant
(CAS: 872365-14-5)

Fevipipran is a reversible competitive CRTh2 antagonist with IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human whole blood. ...

AM-211 sodium
(CAS: 1263077-74-2)

This active molecular is a potent Prostaglandin D2 receptor antagonists and has been in phase I clinical trials for both COPD (chronic obstructive pulmonary dis...

CAS 1175526-27-8 AM-211

AM-211
(CAS: 1175526-27-8)

This active molecular is a potent Prostaglandin D2 receptor antagonists and has been in phase I clinical trials for both COPD (chronic obstructive pulmonary dis...

GSK-345931A
(CAS: 869534-13-4)

GSK-345931A is an EP(1) receptor antagonist. It is efficient in preclinical models of inflammatory pain.

CAS 571170-77-9 Laropiprant

Laropiprant
(CAS: 571170-77-9)

Laropiprant is a potent, selective DP1 receptor antagonist (Ki=0.57 nM) used in combination with niacin to reduce blood cholesterol (LDL and VLDL).

CAS 1006036-88-9 MK-2894 Na salt

MK-2894 Na salt
(CAS: 1006036-88-9)

The sodium salt form of MK-2894 that is found to have conceivable potency and selectivity for further study and might be safer than traditional Non-steroidal an...

CAS 439288-66-1 GW 627368X

GW 627368X
(CAS: 439288-66-1)

GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity (Ki values of 100 nM and 158 nM, resp...

PF-4217329
(CAS: 1005549-94-9)

PF-04217329 is a potent and selective EP2 receptor agonist on intraocular pressure in preclinical models of glaucoma. It is a prodrug of CP-544326. It is well t...

CAS 55028-72-3 Cloprostenol sodium

Cloprostenol sodium
(CAS: 55028-72-3)

Cloprostenol sodium is a synthetic and water-soluble aryl-oxymethyl analog of prostaglandin F2α. lt is also a potent inhibitor of rat adipose precursor differen...

CAS 851723-84-7 OC000459

OC000459
(CAS: 851723-84-7)

OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM.

CAS 1369489-71-3 E7046

E7046
(CAS: 1369489-71-3)

E7046 is an orally bioavailable and specific type 4 prostaglandin E2 (PGE2) receptor EP antagonist (IC50= 13.5 nM) (Ki= 23.14 nM), with anti-tumor activities.

CAS 847728-01-2 CJ-42794

CJ-42794
(CAS: 847728-01-2)

CJ-42794 is a selective prostaglandin E receptor subtype 4 (EP4) antagonist. It inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5. It ...

CAS 851204-35-8 EP1-antanoist-1

EP1-antanoist-1
(CAS: 851204-35-8)

A EP1 antagonist (pKi= 7.54) (pIC50= 8.5)

CAS 745-65-3 Prostaglandin-E1

Prostaglandin-E1
(CAS: 745-65-3)

Prostaglandin-E1 is used as a drug in the treatment of erectile dysfunction and has vasodilatory properties. It can be used as a vasodilator agent increasing pe...

MF592
(CAS: 1064195-48-7)

MF592 is a potent and selective antagonists of the EP4 receptor. It has good functional potency and potent inhibition of PGE2 modulated TNFa release in LPS stim...

CAS 1006036-87-8 MK-2894

MK-2894
(CAS: 1006036-87-8)

MK-2894, a nonacylsulfonamide analogue, is a high affinity full antagonist against the EP4 receptor. It is found to have conceivable potency and selectivity for...

CAS 915191-42-3 MF498

MF498
(CAS: 915191-42-3)

MF498 is a novel and selective E prostanoid receptor 4 (EP4 receptor) antagonist, a Gs protein-coupled receptor, with Ki of 0.7 nM. It plays important roles in ...

CAS 143443-90-7 Ifetroban

Ifetroban
(CAS: 143443-90-7)

Ifetroban is a selective Prostaglandin receptor and Thromboxane A2 receptor antagonist under the development of Bristol-Myers Squibb. Phase II clinical trials f...

Chemical Structure

CAS 915191-42-3 MF498

Quick Inquiry

Verification code

Featured Items