GW 627368X|cas 439288-66-1|DC Chemicals

Cas No.:	439288-66-1
Chemical Name:	N-(Benzenesulfonyl)-2-[4-(4,9-diethoxy-3-oxo-1H-benzo[f]isoindol-2-yl)phenyl]acetamide
Synonyms:	GW 627368;GW 627368X;GW-627368;GW-627368X;4-(4,9-Diethoxy-1,3-dihydro-1-oxo-2H-benz[f]isoindol-2-yl)-N-(phenylsulfonyl)benzeneacetamide;GW627368;GW627368X;A9P1ZGY0SE;N-(benzenesulfonyl)-2-[4-(4,9-diethoxy-3-oxo-1H-benzo[f]isoindol-2-yl)phenyl]acetamide;2-(4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl)-N-(phenylsulfonyl)acetamide;2-(4-(4,9-Diethoxy-1-oxo-1H-benzo[f]isoindol-2(3H)-yl)phenyl)-N-(phenylsulfonyl)acetamide;GTPL1953;HMS3650M04;BCP15277;N
SMILES:	S(C1C([H])=C([H])C([H])=C([H])C=1[H])(N([H])C(C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])N1C(C2=C(C3=C([H])C([H])=C([H])C([H])=C3C(=C2C1([H])[H])OC([H])([H])C([H])([H])[H])OC([H])([H])C([H])([H])[H])=O)=O)(=O)=O
Formula:	C₃₀H₂₈N₂O₆S
M.Wt:	544.6181
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

GW627368(GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor(Ki= 100 nM) with additional human TP receptor affinity(Ki= 150 nM).IC50 value: Target: EP4 antagonistin vitro: At recombinant human prostanoid EP4 receptors expressed in HEK293 cells, GW627368X produced parallel rightward shifts of PGE2 concentration-effect (E/[A]) curves resulting in an affinity (pKb) estimate of 7.9 +/- 0.4. GW627368X appears to bind to human prostanoid TP receptors but not the TP receptors of other species. In human washed platelets, GW627368X (10 microM) produced 100% inhibition of U-46619 (EC100)-induced aggregation (approximate pA2 approximately 7.0) [1]. in vivo: Oral administration of GW627368X showed significant tumor regression characterized by tumor reduction and induction of apoptosis. Reduction in prostaglandin E2 synthesis also led to reduced level of VEGF in plasma [2].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC48172	BAY-6672	BAY-6672 is a potent and selective human Prostaglandin F (FP) receptor antagonist with an IC50 value of 11 nM.
DC10475	Grapiprant	Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2)
DC8348	TG6-10-1	TG6-10-1 is a cell-permeable,highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 17.8 nM).
DC9609	Terutroban	Terutroban is a thromboxane/prostaglandin endoperoxide receptor antagonist.
DC8624	Setipiprant(ACT129968)	Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2.
DC8353	PF-04418948	PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).
DC11043	Omidenepag	Omidenepag is a potent, selective agonist human EP2 receptor with binding IC50/EC50 of 10/1.7 nM, >500-fold selectivity over EP1, EP3 and EP4 receptors; Omidenepag is the active form of Omidenepag Isopropyl (OMDI).
DC10437	MRE-269	MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
DC10785	MK-7246	MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.
DC1009	Laropiprant	MK 0524 is a potent, selective DP1 receptor antagonist with Ki values of 0.57 nM and 0.75 µM for the DP1 and DP2 receptors, respectively.

GW-627368X