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BW-A 78U

BW-A 78U用途

BW-A 78U 是一个 PDE4 抑制剂,其 IC50 值为 3 μM。

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BW-A 78U名称

[ CAS 号 ]:
101155-02-6

[ 中文名 ]:
BW-A 78U

[ 英文名 ]:
BW-A 78U

[英文别名 ]:

bw-a 78u

BW-A 78U生物活性

[ 描述 ]:

BW-A 78U 是一个 PDE4 抑制剂,其 IC50 值为 3 μM。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

研究领域 >> 炎症/免疫

[ 靶点 ]

PDE4:3 μM (IC50)

[体外研究]

BW-A 78U是一种PDE4抑制剂,IC50为3μM。 BW-A 78U未能显着抑制花生四烯酸的释放。 BW-A 78U对抑制脂多糖(LPS)诱导的TNF-α释放无效[1]。

[细胞实验]

将单核细胞与BW-A 78U一起孵育30分钟，浓度为10nM至10μM。然后用脂多糖（10μg/ mL）在37℃，5％CO 2和100％湿度的气氛中刺激细胞过夜。收集无细胞上清液，离心（2000g），并在测定TNF-α之前在-20℃冷冻保存。使用商业试剂盒通过特异性ELISA测定细胞培养上清液中的TNF-α浓度。测定的灵敏度为1pg / mL。用ELISA读数器评估450nm处的吸光度[1]。

[参考文献]

[1]. Boichot E, et al. Anti-inflammatory activities of a new series of selective phosphodiesterase 4 inhibitors derivedfrom 9-benzyladenine. J Pharmacol Exp Ther. 2000 Feb;292(2):647-53.

[相关活性小分子]

BW-A 78U物理化学性质

[ 密度 ]:
1.36g/cm3

[ 沸点 ]:
477.9ºC at 760mmHg

[ 分子式 ]:
C₁₃H₁₂FN₅

[ 分子量 ]:
257.26600

[ 闪点 ]:
242.8ºC

[ 精确质量 ]:
257.10800

[ PSA ]:
55.63000

[ LogP ]:
2.12840

[ 蒸汽压 ]:
2.69E-09mmHg at 25°C

[ 储存条件 ]:
2-8℃

BW-A 78U毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UO7440800

CHEMICAL NAME :: 9H-Purin-6-amine, 9-((2-fluorophenyl)methyl)-N-methyl-

CAS REGISTRY NUMBER :: 101155-02-6

LAST UPDATED :: 199612

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C13-H12-F-N5

MOLECULAR WEIGHT :: 257.30

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Behavioral - ataxia

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 29,1133,1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JHTCAD Journal of Heterocyclic Chemistry. (Hetero Corporation, POB 16000 MH, Tampa, FL 33687) Vol.1- 1964- Volume(issue)/page/year: 25,1255,1988

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 120 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JHTCAD Journal of Heterocyclic Chemistry. (Hetero Corporation, POB 16000 MH, Tampa, FL 33687) Vol.1- 1964- Volume(issue)/page/year: 25,1255,1988