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BW 245C

BW 245C用途

BW 245C 是一种有效的前列腺素类DP受体prostanoid DP-receptor (DP1)激动剂,常用于中风等疾病的研究。

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BW 245C名称

[ CAS 号 ]:
72814-32-5

[ 中文名 ]:
BW 245C

[ 英文名 ]:
BW 245C

[英文别名 ]:

BW 245C生物活性

[ 描述 ]:

BW 245C 是一种有效的前列腺素类DP受体prostanoid DP-receptor (DP1)激动剂,常用于中风等疾病的研究。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体

研究领域 >> 心血管疾病

[ 靶点 ]

DP/DP1 Receptor

[体外研究]

BW245C(0.01-1μM)在Th2细胞中以剂量依赖性方式抑制TGF-β诱导的胶原分泌。 BW245C(0.01-1μM)也可增加肺成纤维细胞中的细胞内cAMP [3]。 BW245C(0.1-3μmol/ L)剂量依赖性地增加跨内皮电阻并降低人脐静脉内皮细胞的FITC-葡聚糖渗透性。 BW245C(0.3μmol/ L)可增加细胞内cAMP水平和随后的蛋白激酶A(PKA)活性[4]。

[体内研究]

WT小鼠中的BW245C(0.02,0.2和2.0mg/kg)导致CBF的显着增加,但是这种治疗的这种作用在DP1 -/-小鼠中不存在。 BW245C减轻中风后的功能缺陷。 BW245C显着逆转了神经功能缺损显着增强的这些条件,而WT小鼠中风后运动活性显着降低。中风后1小时BW245C(0.2mg/kg)注射导致WT小鼠脑梗塞显着减少,而在DP1 -/-小鼠中未观察到该治疗的效果。 BW245C在中风期间和之后改善CBF。与媒介物治疗组相比,BW245C导致出血明显延长[1]。 BW 245C(100 nM)不会显着增加OVA致敏豚鼠的食管上皮中MBP阳性嗜酸性粒细胞[2]。

[动物实验]

小鼠未经处理或ip注射载体（1％DMSO）或0.2mg / kg BW245C。注射后30分钟，将小鼠麻醉并置于温控垫上以维持体温，并切下3mm的尾尖。将尾巴立即浸入温热的PBS（37.0±0.5℃）中，记录可见的停止出血的时间。

[参考文献]

[1]. Ahmad AS, et al. PGD₂ DP1 receptor stimulation following stroke ameliorates cerebral blood flow and outcomes. Neuroscience. 2014 Oct 24;279:260-8.

[2]. Zhang S, et al. Prostaglandin D₂ receptor D-type prostanoid receptor 2 mediates eosinophil trafficking into the esophagus. Dis Esophagus. 2014 Aug;27(6):601-6.

[3]. Ayabe S, et al. Prostaglandin D₂ inhibits collagen secretion from lung fibroblasts by activating the DP receptor. J Pharmacol Sci. 2013;121(4):312-7. Epub 2013 Mar 29.

[4]. Kobayashi K, et al. Prostaglandin D₂-DP signaling promotes endothelial barrier function via the cAMP/PKA/Tiam1/Rac1 pathway. Arterioscler Thromb Vasc Biol. 2013 Mar;33(3):565-71.

[相关活性小分子]

BW 245C物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 分子式 ]:
C₁₉H₃₂N₂O₅

[ 分子量 ]:
368.468

[ 精确质量 ]:
368.231110

[ PSA ]:
106.94000

[ LogP ]:
2.12

[ 折射率 ]:
1.521

[ 储存条件 ]:
-20°C，密闭，干燥

BW 245CMSDS

详细MSDS(安全技术说明书)

BW 245C安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ WGK德国 ]:
3

BW 245C文献

Genetic validation of a therapeutic target in a mouse model of ALS.

Sci. Transl. Med. 6(248) , 248ra104, (2014)

Neurons produced from stem cells have emerged as a tool to identify new therapeutic targets for neurological diseases such as amyotrophic lateral sclerosis (ALS). However, it remains unclear to what e...

Functional antagonism of IL-1alpha induced gene expression profiles define the cAMP/PKA pathway as a unique regulator of IL-1alpha signaling networks.

J. Recept. Signal Transduct. Res. 29(5) , 246-56, (2009)

Interleukin-1 (IL-1alpha) induced inflammatory and pro-fibrotic responses in human lung fibroblasts are mediated by activation of MAPK and NFkappaB pathways. The purpose of the present study was to br...

Prostaglandin D2 causes preferential induction of proinflammatory Th2 cytokine production through an action on chemoattractant receptor-like molecule expressed on Th2 cells.

J. Immunol. 175(10) , 6531-6, (2005)

PGD2, produced by mast cells, has been detected in high concentrations at sites of allergic inflammation. It can stimulate vascular and other inflammatory responses by interaction with D prostanoid re...

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