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
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
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。
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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)
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+
Mechanism of pharmacochaperoning in a mammalian KATP channel revealed by cryo-EM
Martin GM, et al.
eLife, 8 (2019)
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
Laxmikant Ramvallabh Zawar et al.
Chemical & pharmaceutical bulletin, 60(4), 482-487 (2012-04-03)
The influence of microwave technology on the in vitro dissolution rate and in vivo antihyperglycemic activity of a poorly water soluble drug, repaglinide (RG) was studied. Solid dispersions were prepared by conventional fusion method and microwave method using poloxamer 188.
Boggarapu Prakash Rao et al.
Pakistan journal of pharmaceutical sciences, 26(4), 707-713 (2013-07-03)
The full factorial design was employed to evaluate contribution of drug: polymer and Eudragit RS 100: Eudragit RL 100 on entrapment efficiency, time for maximum drug release, percentage of drug release. Floating microparticles were prepared using spray drying technique. Microparticles
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