L-798106

Names

[ Name ]:
L-798106

[Synonym ]:
(2E)-N-[(5-bromo-2-methoxyphenyl)sulfonyl]-3-[2-(2-naphthalenylmethyl)phenyl]-2-propenamide
Zinterol hydrochloride

Biological Activity

[Description]:

L-798106 is potent and highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM), it also has micromolar activities at the EP4, EP1 and EP2 receptors with Ki values of 916 nM, >5000 nM and >5000 nM at EP4, EP1 and EP2, respectively[1].

[Related Catalog]:

Research Areas >> Cancer

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

[Target]

Ki values: 0.3 nM (EP3 receptor); 916 nM (EP4 receptor); > 5000 nM (EP1/2 receptor)[1]

[References]

[1]. Juteau H, et al. Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor. Bioorg Med Chem. 2001 Aug;9(8):1977-84.

Chemical & Physical Properties

[ Density]:
1.425±0.06 g/cm3(Predicted)

[ Molecular Formula ]:
C₂₇H₂₂BrNO₄S

[ Molecular Weight ]:
536.43700

[ Exact Mass ]:
535.04500

[ PSA ]:
80.85000

[ LogP ]:
7.19170

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Statements ]:
H413

[ RIDADR ]:
NONH for all modes of transport

Articles

Angiogenesis in the primate ovulatory follicle is stimulated by luteinizing hormone via prostaglandin E2.

Biol. Reprod. 92(1) , 15, (2015)

Rapid angiogenesis occurs as the ovulatory follicle is transformed into the corpus luteum. To determine if luteinizing hormone (LH)-stimulated prostaglandin E2 (PGE2) regulates angiogenesis in the ovu...

Mechanisms for proteinase-activated receptor 1-triggered prostaglandin E2 generation in mouse osteoblastic MC3T3-E1 cells.

Biol. Chem. 396(2) , 153-62, (2015)

We analyzed signaling mechanisms for prostaglandin E2 (PGE2) production following activation of proteinase-activated receptor-1 (PAR1), a thrombin receptor, in preosteoblastic MC3T3-E1 cells. PAR1 sti...

6-Substituted 9-fluoroquino[3,2-b]benzo[1,4]thiazines display strong antiproliferative and antitumor properties.

Eur. J. Med. Chem. 89 , 411-20, (2014)

6-Substituted 9-fluoroquino[3,2-b]benzo[1,4]thiazines - a new type of tetracyclic azaphenothiazines-were obtained from of 6H-9-fluoroquinobenzothiazine by the introduction of appropriate substituents ...