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| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| D426448-1ml |
1ml |
现货 ![]() |
|
| 别名 | AMPK 抑制剂 | 多索吗啡肽 |
|---|---|
| 英文别名 | BML-275 | 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine | AC-27419 | SY256013 | AM20061004 | Dorsomorphin, >=98% (HPLC) | NCGC00165869-01 | 6-[4-(2-Piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine | HMS2 |
| 规格或纯度 | Moligand™, 2mM in DMSO |
| 英文名称 | Dorsomorphin |
| 生化机理 | 多索吗啡是骨形态发生蛋白(BMP)信号传导的选择性抑制剂。研究发现,它能抑制胚胎发育所需的 BMP 信号,并促进人类多能干细胞(hPSC)系的神经分化。多索吗啡还是 AMPK(AMP 激活蛋白激酶)的一种强效、选择性、可逆和 ATP 竞争性抑制剂;在 5 μM ATP 存在和 AMP 不存在的情况下,Ki = 109 nM)。抑制 AICAR 和二甲双胍诱导的 AMPK 激活。骨形态发生蛋白(BMP)I 型受体(ALK2、ALK3 和 ALK6)的选择性抑制剂。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | EPH 受体 A2 的抑制剂;酪氨酸激酶 1 的抑制剂;酪氨酸激酶 3 的抑制剂;激酶插入域受体的抑制剂;LCK 原癌基因的抑制剂;Src 家族酪氨酸激酶;MAPK 相互作用丝氨酸/苏氨酸激酶 1 抑制剂;核糖体蛋白 S6 激酶 A1 抑制剂;SRC 原癌基因抑制剂;非受体酪氨酸激酶 |
| 产品介绍 |
BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and Fatty Acid Synthase inhibitor. Phosphorylation of AMPK occurs in vivo when energy sources are low and in-turn suppresses expression of SREBP-1. SREBP-1 is a key lipogenic transcription factor, and its suppression allows glucose production by hepatocytes. In mouse studies it has been reported that BML-275 rapidly reduces the level of the phosphorylated AMPK α subunit in the hypothalamus, in an ATP-competitive manner, therefore altering energy perception and affecting the physiological energy sensor of the body. Over-activation of AMPK has also been found to be deleterious in ischemic stroke conditions and inhibition of AMPK by BML-275 may provide a small level of neuroprotection. Additional research on zebrafish has shown that BML-275 also inhibits bone morphogenetic protein signals required for iron metabolism and embryogenesis. BML-275 is an inhibitor of ACTR-I, BMPR-IA and BMPR-IB. BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and Fatty Acid Synthase inhibitor. Phosphorylation of AMPK occurs in vivo when energy sources are low and in-turn suppresses expression of SREBP-1. SREBP-1 is a key lipogenic transcription factor, and its suppression allows glucose production by hepatocytes. In mouse studies it has been reported that BML-275 rapidly reduces the level of the phosphorylated AMPK α subunit in the hypothalamus, in an ATP-competitive manner, therefore altering energy perception and affecting the physiological energy sensor of the body. Over-activation of AMPK has also been found to be deleterious in ischemic stroke conditions and inhibition of AMPK by BML-275 may provide a small level of neuroprotection. Additional research on zebrafish has shown that BML-275 also inhibits bone morphogenetic protein signals required for iron metabolism and embryogenesis. BML-275 is an inhibitor of ACTR-I, BMPR-IA and BMPR-IB. |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine |
| INCHI | 1S/C24H25N5O/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20/h4-11,16-18H,1-3,12-15H2 |
| InChi Key | XHBVYDAKJHETMP-UHFFFAOYSA-N |
| Smiles | C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3 |
| Isomeric SMILES | C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3 |
| 关联CAS | 1219168-18-9 |
| 分子量 | 399.49 |
| Reaxy-Rn | 11725482 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11725482&ln= |
| 敏感性 | 对光及空气敏感 |
|---|---|
| 分子量 | 399.500 g/mol |
| XLogP3 | 3.400 |
| 氢键供体数Hydrogen Bond Donor Count | 0 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 6 |
| 精确质量Exact Mass | 399.206 Da |
| 单同位素质量Monoisotopic Mass | 399.206 Da |
| 拓扑极表面积Topological Polar Surface Area | 55.600 Ų |
| 重原子数Heavy Atom Count | 30 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 514.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 象形图 | GHS07 |
|---|---|
| 信号词 | 警告 |
| 危险声明 |
H302: 吞食有害 H312: 皮肤接触有害 H332: 吸入有害 |
| 预防措施声明 |
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P264: 处理后要彻底洗手。 P270: 使用本产品时,请勿进食、饮水或吸烟。 P271: 仅在室外或通风良好的地方使用。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P321: 特殊处理(请参阅此标签上的...)。 P330: 漱口 P302+P352: 如皮肤沾染:用水充分清洗。 P304+P340: 如误吸入:将人转移到空气新鲜处,保持呼吸舒适体位。 P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。 P501: 将内容物/容器处理到。。。 P301+P317: 如果被吞咽:请寻求医疗帮助。 P317: 寻求紧急医疗救助。 |
| WGK Germany | 3 |
| 个人防护装备 | dust mask type N95 (US), Eyeshields, Gloves |
| 1. Chao Tian, Yuchao Feng, Tianhua Chen, Zuyang Zhang, Xiaojie He, Liangdong Jiang, Mingjiang Liu. (2023) EGCG Restores Keratinocyte Autophagy to Promote Diabetic Wound Healing through the AMPK/ULK1 Pathway. Frontiers in Bioscience-Landmark, 28 (12): (324). [PMID:38179734] [10.31083/j.fbl2812324] |
| 2. Xuan Ren, Jianchun Xu, Qingsong Xue, Yi Tong, Tairan Xu, Jinli Wang, Ting Yang, Yuan Chen, Deshun Shi, Xiangping Li. (2024) BRG1 enhances porcine iPSC pluripotency through WNT/β-catenin and autophagy pathways. THERIOGENOLOGY, 215 (10). [PMID:38000125] [10.1016/j.theriogenology.2023.11.014] |
| 3. Yixin Sun, Danyang Guo, Saiding Yue, Mingyan Zhou, Dongxu Wang, Fengjiao Chen, Lingling Wang. (2023) Afzelin protects against doxorubicin-induced cardiotoxicity by promoting the AMPKα/SIRT1 signaling pathway. TOXICOLOGY AND APPLIED PHARMACOLOGY, (116687). [PMID:37703929] [10.1016/j.taap.2023.116687] |
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| 5. Xingru Chen, Xiaolan Zhou, Xiaoqing Cheng, Liting Lin, Qi Wang, Ruoting Zhan, Qingguang Wu, Sijun Liu. (2023) Protective Effect of Ferulic Acid on Lipopolysaccharide-Induced BV2 Microglia Inflammation via AMPK/mTOR Signaling Pathway. MOLECULES, 28 (8): (3482). [PMID:37110714] [10.3390/molecules28083482] |
| 6. Haixu Wang, Yan Li, Chuang Liu, Tianxiang Lu, Qian Zhai, Hongna Wang, Jianfang Zhang. (2023) Inhibition of VDAC1 prevents oxidative stress and apoptosis induced by bisphenol A in spermatogonia via AMPK/mTOR signaling pathway. JOURNAL OF TOXICOLOGICAL SCIENCES, [PMID:36858637] [10.2131/jts.48.109] |
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