R9028
瑞格列奈
≥98% (HPLC), K-ATP channel blocker, solid
别名:
(S)-(+)-2-乙氧基-4- [N- [1-（2-哌啶苯基）-3-甲基-1-丁基] 氨基羰基甲基] 苯甲酸, Novonorm, Prandin
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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
SMILES string
CCOc1cc(CC(=O)N[C@@H](CC(C)C)c2ccccc2N3CCCCC3)ccc1C(O)=O
InChI key
FAEKWTJYAYMJKF-QHCPKHFHSA-N
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
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
Quality Level
Gene Information
human ... ABCC8(6833), KCNJ1(3758), KCNJ11(3767)
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相关类别
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。
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）。
Features and Benefits
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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。
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)
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+
Carolina Säll et al.
Drug metabolism and disposition: the biological fate of chemicals, 40(7), 1279-1289 (2012-03-28)
Repaglinide is presently recommended by the U.S. Food and Drug Administration as a clinical CYP2C8 probe, yet current in vitro and clinical data are inconsistent concerning the role of this enzyme in repaglinide elimination. The aim of the current study
Rania N El-Shaheny
Journal of fluorescence, 22(6), 1587-1594 (2012-07-04)
A simple and highly sensitive spectrofluorimetric method was developed and validated for determination of the antidiabetic agent repaglinide (RG) in tablets. The proposed method is based on measurement of the native fluorescence of RG in 0.1 M H(2)SO(4)/methanol medium at
Carlos del Pozo-Fernández et al.
Nefrologia : publicacion oficial de la Sociedad Espanola Nefrologia, 32(3), 367-373 (2012-05-18)
In this paper we analyse the discrepancies that exist in the widespread prescription of metformin in patients with type 2 diabetes and the lack of guidelines concerning its prescription in the different stages of renal failure. This cross-sectional study includes
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