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氨来呫诺

氨来呫诺用途

AmLexanox 是特异性的 IKKε 和 TBK1 抑制剂,IC50 值为 1-2 μM。

氨来呫诺名称

[ CAS 号 ]:
68302-57-8

[ 中文名 ]:
氨来占诺

[ 英文名 ]:
Amlexanox

[中文别名 ]:

[英文别名 ]:

氨来呫诺生物活性

[ 描述 ]:

AmLexanox 是特异性的 IKKε 和 TBK1 抑制剂,IC50 值为 1-2 μM。

[ 相关类别 ]:

信号通路 >> NF-κB信号通路 >> IKK
研究领域 >> 代谢疾病

[ 靶点 ]

IKKε:1-2 μM (IC50)

TBK1:1-2 μM (IC50)


[体外研究]

AmLexanox增加3T3-L1脂肪细胞中Ser172上TBK1的磷酸化,并阻断聚胞苷:聚胞苷酸(poly I:C)刺激的干扰素反应因子-3(IRF3)的磷酸化,这是IKKε和TBK1的假定底物[1]。 AmLexanox在体外环境中有效抑制肥大细胞,嗜碱性粒细胞和中性粒细胞释放组胺和白三烯,可能通过增加炎症细胞内细胞内环AMP含量,降低膜内稳定作用或抑制钙内流[2]。在原代骨髓衍生的巨噬细胞(BMM)中,amLexanox抑制破骨细胞形成和骨吸收。在分子水平上,amLexanox抑制RANKL诱导的核因子-κB(NF-κB),丝裂原活化蛋白激酶(MAPKs),c-Fos和NFATc1的激活。 AmLexanox降低破骨细胞特异性基因的表达,包括TRAP,MMP9,组织蛋白酶K和NFATc1 [3]。

[体内研究]

AmLexanox(100 mg/kg,po)预防和逆转饮食诱导或遗传性肥胖,并在肥胖小鼠中产生可逆的体重减轻。 AmLexanox还导致这些小鼠的脂肪组织质量显着降低,并且循环脂联素增加。 AmLexanox(25 mg/kg)显着改善已建立DIO的小鼠的胰岛素敏感性,治疗4周后,amLexanox可显着改善葡萄糖[1]。 AmLexanox在第一次施用糊剂之前和之后已经显示出抑制立即和之后的评价。分类量表也是迟发型超敏反应[2]。 AmLexanox(20 mg/kg)可增强BMSCs的成骨细胞分化。在卵巢切除(OVX)小鼠模型中,amLexanox通过抑制破骨细胞活性来预防OVX诱导的骨丢失[3]。

[激酶实验]

通过将纯化的激酶(IKKε或TBK1)在含有25mM Tris(pH7.5),10mM MgCl 2,1mM DTT和10μMATP的激酶缓冲液中于30℃温育30分钟来进行体外激酶测定。每个样品存在0.5μCiγ-[32P] -ATP和1μgMBP作为底物。通过加入4x十二烷基硫酸钠(SDS)样品缓冲液并在95℃下煮沸5分钟来终止激酶反应。通过SDS-聚丙烯酰胺凝胶电泳分离上清液,转移至硝酸纤维素,并使用Typhoon 9410磷成像仪通过放射自显影分析。

[细胞实验]

为了检查细胞增殖,根据制造商的说明使用细胞计数试剂盒-8。将BMM以5×10 3个细胞/孔的密度接种在96孔板中。 24小时后,在M-CSF(30ng / mL)存在下,每2天用不同浓度的AmLexanox(0,1.5,3,6,12,25μM)处理细胞7天。在1,3,5和7天后,用含有10%CCK-8的培养基替换培养基,并将细胞在37℃下再培养2小时。然后在ELX800吸光度酶标仪上在450nm波长下测量吸光度。

[动物实验]

向野生型雄性C57BL / 6小鼠喂食HFD,其由来自8周龄的脂肪的45%卡路里组成,持续12-24周,而ND C57BL / 6对照维持在由4.5%脂肪组成的正常食物饲料上。饲喂含有ω-3脂肪酸的C57BL / 6日粮。通过在已经在HFD上持续16周的小鼠中将化合物添加到饮食中来施用罗格列酮治疗三周。每只小鼠平均每天消耗3.5mg / kg罗格列酮。 AmLexanox通过每日口服强饲法给药。对于预防组,amLexanox(25mg / kg或100mg / kg)与8周龄HFD喂养同时开始。对于治疗组,在HFD 12周后,在20周龄时开始每公斤25mg amLexanox治疗。为了测试amLexanox戒断的效果,在amLexanox处理8周后,处理组中的小鼠从amLexanox管饲法转换为载体对照。对照组和ob / ob小鼠用正常饲料喂养,并在10周龄时开始用100mg / kg amLexanox或载体对照饲养。将动物饲养在无特定病原体的设施中,12小时光照/ 12小时黑暗循环,并自由获取食物和水。

[参考文献]

[1]. Reilly SM, et al. An inhibitor of the protein kinases TBK1 and IKK-e improves obesity-related metabolic dysfunctions in mice. Nat Med. 2013 Mar;19(3):313-21.

[2]. Bell, J. AmLexanox for the treatment of recurrent aphthous ulcers. Clin Drug Investig, 2005. 25(9): p. 555-66.

[3]. Zhang Y, et al. AmLexanox Suppresses Osteoclastogenesis and Prevents Ovariectomy-Induced Bone Loss. Sci Rep. 2015 Sep 4;5:13575.


[相关活性小分子]

白藜芦醇 | N-[3-[[5-环丙基-2-[[3-(4-吗啉基甲基)苯基]氨基]-4-嘧啶基]氨基]丙基]环丁烷甲酰胺 | N-(1,8-二甲基咪唑并[1,2-A]喹喔啉-4-基)-1,2-乙二胺盐酸盐 | N-(6-氯-7-甲氧基-9h-吡啶并[3,4-b]吲哚-8-基)-2-甲基-3-吡啶羧酰胺 | ACHP盐酸盐 | TPCA-1 | IKK-16,选择性IKK抑制剂 | IMD-0354 | LY2409881 | 4-氨基-[2,3']联噻吩-5-甲酰胺 | BI605906 | 海湾65-1942盐酸盐 | IKK(epsilon)-IN-1 (IKKE-IN-1) | AZD3264 | PS-1145

氨来呫诺物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
570.0±50.0 °C at 760 mmHg

[ 熔点 ]:
>3000C

[ 分子式 ]:
C16H14N2O4

[ 分子量 ]:
298.293

[ 闪点 ]:
298.5±30.1 °C

[ 精确质量 ]:
298.095367

[ PSA ]:
106.42000

[ LogP ]:
3.74

[ 外观性状 ]:
白色结晶固体

[ 蒸汽压 ]:
0.0±1.6 mmHg at 25°C

[ 折射率 ]:
1.669

[ 储存条件 ]:
-20°C Freezer

氨来呫诺MSDS

氨来呫诺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DJ3102000
CHEMICAL NAME :
5H-(1)Benzopyrano(2,3-b)pyridine-3-carboxylic acid, 2-amino-7-(1-methylethyl)-5-oxo-
CAS REGISTRY NUMBER :
68302-57-8
LAST UPDATED :
199612
DATA ITEMS CITED :
9
MOLECULAR FORMULA :
C16-H14-N2-O4
MOLECULAR WEIGHT :
298.32

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 :
10 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,6405,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,6405,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1400 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,6405,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
2320 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,6405,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
450 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,6405,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
3310 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,6405,1985 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
35 gm/kg/5W-I
TOXIC EFFECTS :
Gastrointestinal - other changes Liver - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,4843,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
54600 mg/kg/26W-C
TOXIC EFFECTS :
Liver - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,6411,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
3500 mg/kg/5W-C
TOXIC EFFECTS :
Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13,7123,1985

氨来呫诺安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn,Xi

[ 风险声明 (欧洲) ]:
R22:Harmful if swallowed. R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
S26

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

[ WGK德国 ]:
3

[ RTECS号 ]:
XZ3012000

[ 海关编码 ]:
2934999090

氨来呫诺合成路线

氨来呫诺上下游产品

氨来呫诺制备

3-氰基6-异丙基苯并吡喃酮(I)在含吗啉和二甲基甲酰胺的水溶液中,在60℃加热反应,得到化合物(Ⅱ)。再和丙二酸单乙酯酰胺缩合环合,然后水解得到氨来咕诺。

氨来呫诺海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

氨来呫诺文献

Hydroxychloroquine-inhibited dengue virus is associated with host defense machinery.

J. Interferon Cytokine Res. 35(3) , 143-56, (2015)

Hydroxychloroquine (HCQ) is an antimalarial drug also used in treating autoimmune diseases. Its antiviral activity was demonstrated in restricting HIV infection in vitro; however, the clinical implica...

Role of G Protein-Coupled Receptor Kinases 2 and 3 in μ-Opioid Receptor Desensitization and Internalization.

Mol. Pharmacol. 88 , 347-56, (2015)

There is ongoing debate about the role of G protein-coupled receptor kinases (GRKs) in agonist-induced desensitization of the μ-opioid receptor (MOPr) in brain neurons. In the present paper, we have u...

Regulation of T-cell activation and migration by the kinase TBK1 during neuroinflammation.

Nat. Commun. 6 , 6074, (2015)

Development of an immune or autoimmune response involves T-cell activation in lymphoid organs and subsequent migration to peripheral tissues. Here we show that T-cell-specific ablation of the kinase T...


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产品详情:AA-673(Amlexanox)


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¥97.0/250mg ¥168.0/1g ¥543.0/5g ¥1956.0/25g

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产品详情:[Perfemiker]氨来占诺,98%


公司名:上海阿拉丁生化科技股份有限公司

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价格:
¥150.9/1g ¥68.9/250mg ¥205.9/1ml ¥513.9/5g

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氨来呫诺相关知识

氨来呫诺的作用和生物活性

2018-10-30 14:16:55

氨来呫诺是一种抗口疮性溃疡药物。氨来呫诺抑制肥大细胞,中性粒细胞和单核细胞中炎症介质(包括白三烯和组胺)的合成和释放。氨来呫诺还可作为白三烯D4拮抗剂和磷酸二酯酶抑制剂。氨来呫诺减少溃疡愈合的时间以及与溃疡相关的疼痛。一、氨来呫诺的生物活性详解:1)体外活性氨来呫诺可增加3T3-L1脂肪细胞中Se...


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【氨来呫诺】化源网提供氨来呫诺CAS号68302-57-8,氨来呫诺MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询氨来呫诺上化源网,专业又轻松。>>电脑版:氨来呫诺

标题:氨来呫诺_MSDS_用途_密度_氨来呫诺CAS号【68302-57-8】_化源网 地址:https://www.chemsrc.com/amp/cas/68302-57-8_895207.html