G117
格列吡嗪
solid
别名:
1-环己基-3-{4-[2-(5-甲基吡嗪-2-甲酰胺基)乙基]苯磺酰基}脲
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关于此项目
经验公式（希尔记法）:
C21H27N5O4S
化学文摘社编号:
分子量:
445.54
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
EC Number:
249-427-6
MDL number:
InChI key
ZJJXGWJIGJFDTL-UHFFFAOYSA-N
InChI
1S/C21H27N5O4S/c1-15-13-24-19(14-23-15)20(27)22-12-11-16-7-9-18(10-8-16)31(29,30)26-21(28)25-17-5-3-2-4-6-17/h7-10,13-14,17H,2-6,11-12H2,1H3,(H,22,27)(H2,25,26,28)
SMILES string
Cc1cnc(cn1)C(=O)NCCc2ccc(cc2)S(=O)(=O)NC(=O)NC3CCCCC3
form
solid
color
white
solubility
methanol: 1.9 mg/mL, DMSO: 48 mg/mL
Quality Level
Gene Information
human ... ABCC8(6833), KCNJ1(3758), KCNJ11(3767)
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General description
钾内向整流通道，亚家族J，成员1（KCNJ1）可编码肾外髓质钾通道（ROMK1，Kir1.1）。 格列吡嗪是一种抗糖尿病药，可用于治疗II型糖尿病。（5）
Application
格列吡嗪已被用于：
- 雏鸡卵黄囊膜（YSM）和绒膜尿囊膜（CAM）检测
- 在绒毛膜尿囊膜（CAM）上进行的MCF-7乳腺癌检测
- 转移测定
- 大鼠主动脉环测定
- 体内基质胶塞测定
- 3-（4,5-二甲基噻唑-2-基）-2,5-二苯基溴化四氮唑（MTT）测定
- 流式细胞术
- 蛋白印迹
Biochem/physiol Actions
钾内向整流通道，亚家族J，成员1（KCNJ1）在钾平衡中起着至关重要的作用。 它是一种ATP依赖的K+通道阻断剂。其所编码的蛋白质负责消除钾，以交换钠被上皮钠通道（ENaC）吸收。 KCNJ1中的突变与多种疾病有关，例如产前Bartter综合征和糖尿病。 格列吡嗪通过预防血管生成，有助于抑制肿瘤的发展和转移。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
KCNJ1 inhibits tumor proliferation and metastasis and is a prognostic factor in clear cell renal cell carcinoma
Guo Z, et al.
Tumour Biology : the Journal of the International Society For Oncodevelopmental Biology and Medicine, 36(2), 1251-1259 (2015)
Glipizide suppresses prostate cancer progression in the TRAMP model by inhibiting angiogenesis
Qi C, et al.
Scientific reports, 6(20), 27819-27819 (2016)
Association of KCNJ1 variation with change in fasting glucose and new onset diabetes during HCTZ treatment
Karnes JH, et al.
The Pharmacogenomics Journal, 13(5), 430-430 (2013)
Greg L Plosker
Drugs, 72(17), 2289-2312 (2012-11-23)
Dapagliflozin (Forxiga®) is the first in a novel class of glucose-lowering agents known as sodium-glucose co-transporter-2 (SGLT2) inhibitors and is used in the treatment of patients with type 2 diabetes. By inhibiting the transporter protein SGLT2 in the kidneys, dapagliflozin
Korbinian Löbmann et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 81(1), 159-169 (2012-02-23)
The objective of this study was to prepare a co-amorphous drug/drug combination between two BCS class II drugs, simvastatin (SVS) and glipizide (GPZ). This pharmacologically relevant combination of two drugs could produce a promising candidate for formulations intended for combination
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