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关于此项目
经验公式(希尔记法):
C27H36N2O4
化学文摘社编号:
分子量:
452.59
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
瑞格列奈, ≥98% (HPLC), solid
Quality Level
assay
≥98% (HPLC)
form
solid
color
white
mp
129-130.2 °C
solubility
DMSO: >20 mg/mL
originator
Novo Nordisk
storage temp.
2-8°C
SMILES string
CCOc1cc(CC(=O)N[C@@H](CC(C)C)c2ccccc2N3CCCCC3)ccc1C(O)=O
InChI
1S/C27H36N2O4/c1-4-33-25-17-20(12-13-22(25)27(31)32)18-26(30)28-23(16-19(2)3)21-10-6-7-11-24(21)29-14-8-5-9-15-29/h6-7,10-13,17,19,23H,4-5,8-9,14-16,18H2,1-3H3,(H,28,30)(H,31,32)/t23-/m0/s1
InChI key
FAEKWTJYAYMJKF-QHCPKHFHSA-N
Gene Information
human ... ABCC8(6833), KCNJ1(3758), KCNJ11(3767)
General description
瑞格列奈属于美格替奈类,其与格列本脲的差别在于具有庞大的B位点基团,而不是 A位点基团。
Application
瑞格列奈已被用作乳腺癌细胞系MDA-MB-231中的ATP敏感性钾通道(KATP)抑制剂。它还被用于制备KATP复合物,用于通过冷冻电子显微镜结构分析研究其相互作用。
Biochem/physiol Actions
瑞格列奈(RPG)由于起效快,可预防低血糖症。RPG引起的KATP抑制使胰腺细胞去极化β,从而导致电压门控钙通道激活,触发胰岛素释放。瑞格列奈有利于钙黄绿素通过并改善间隙连接细胞间通讯(GJIC)。从结构上看,瑞格列奈结合跨膜束中的ABC转运蛋白磺脲受体1 (SUR1)。
瑞格列奈是一种有效的短效胰岛素促分泌剂,可通过关闭胰岛β细胞质膜中的ATP敏感性钾(KATP)通道发挥作用。
瑞格列奈是一种有效的短效胰岛素促分泌剂,可通过关闭胰岛β细胞质膜中的ATP敏感性钾(KATP)通道发挥作用。 它是一类新的胰岛素促分泌素,其结构上与磺酰脲无关,专为治疗2型糖尿病而开发。
Features and Benefits
该化合物由Novo Nordisk开发。要浏览其他药物开发化合物和批准的药物/候选药物列表,单击此处。
这种化合物是 ADME 毒性研究的特色产品。点击此处发现更多特色 ADME 毒性产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。
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存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
商品
Discover Bioactive Small Molecules for ADME/Tox
相关内容
Instructions
Mechanism of pharmacochaperoning in a mammalian KATP channel revealed by cryo-EM
Martin GM, et al.
eLife, 8 (2019)
Fatima Maqoud et al.
Pharmaceutics, 13(9) (2021-09-29)
Zoledronic acid (ZOL) is used as a bone-specific antiresorptive drug with antimyeloma effects. Adverse drug reactions (A.D.R.) are associated with ZOL-therapy, whose mechanics are unknown. ZOL is a nitrogen-containing molecule whose structure shows similarities with nucleotides, ligands of ATP-sensitive K+
Thomas M Bodenstine et al.
FEBS letters, 586(1), 27-31 (2011-11-29)
Gap junctional intercellular communication (GJIC) regulates cellular homeostasis by propagating signaling molecules, exchanging cellular metabolites, and coupling electrical signals. In cancer, cells exhibit altered rates of GJIC which may play a role in neoplastic progression. K(ATP) channels help maintain membrane
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| R9028-50MG | 04061832575780 |
| R9028-250MG | 04061832575773 |