L-798106

L-798106用途

L-798106 是强效且高度选择性的前列腺素类 EP3 受体拮抗剂 (Ki=0.3 nM),它在 EP4,EP1 和 EP2 受体上也具有微摩尔活性,针对 EP4,EP1,EP2 的 Ki 值分别为 916 nM,>5000 nM 和 >5000 nM。

L-798106名称

[ CAS 号 ]:
244101-02-8

[ 中文名 ]:
(2E)-N-[(5-溴-2-甲氧基苯基)磺酰基]-3-[2-(2-萘甲基)苯基]-2-丙烯酰胺

[ 英文名 ]:
L-798106

[英文别名 ]:

Zinterol hydrochloride

L-798106生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体

[ 靶点 ]

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

[参考文献]

[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.

L-798106物理化学性质

[ 密度 ]:
1.425±0.06 g/cm3(Predicted)

[ 分子式 ]:
C₂₇H₂₂BrNO₄S

[ 分子量 ]:
536.43700

[ 精确质量 ]:
535.04500

[ PSA ]:
80.85000

[ LogP ]:
7.19170

[ 储存条件 ]:
2-8°C

L-798106MSDS

详细MSDS(安全技术说明书)

L-798106安全信息

[ 危害声明 ]:
H413

[ 危险品运输编码 ]:
NONH for all modes of transport

L-798106文献

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 ...

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