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米格列奈钙

米格列奈钙

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?米格列奈钙名称


















中文名

米格列奈钙
英文名

Calcium 2-benzyl-4-((3aR,7aS)-hexahydro-1H-isoindol-2(3H)-yl)-4-oxobutanoate
中文别名


米格列奈




|



双(2S)-2-苄基-3-(顺式全氢异吲哚-2-羰基)丙酸单钙盐



英文别名
更多





?米格列奈钙生物活性












































描述
Mitiglinide(KAD-1229; S21403)是KATP通道拮抗剂,具有抗2型糖尿病活性。
相关类别



溶解度

体外:

DMSO:5 mg / mL(14.95 mM;需要超声波)

体内:1。逐个添加每种溶剂:10%DMSO 90%玉米油溶解度:≥0.5mg / mL(1.50 mM);澄清溶液2.逐个添加每种溶剂:10%DMSO 40%PEG300 5%吐温-80 45%盐水溶解度:≥0.5mg/ mL(1.50mM);澄清溶液3.逐个加入各溶剂:10%DMSO 90%(20%SBE-β-CD在盐水中)溶解度:≥0.5mg/ mL(1.50mM);明确解决方案

储备液

1 mM 2.9901 mL 14.9504 mL 29.9007 mL
5 mM 0.5980 mL 2.9901 mL 5.9801 mL
10 mM 0.2990 mL 1.4950 mL 2.9901 mL


存储

粉末 -20℃下 3年
4℃下 2年
在溶剂中 -80℃下 6个月
-20℃下 1个月


运输

室温;可能会有所不同
SMILES

O=C([O-])[C@H](CC(N1C[C@](CCCC2)([H])[C@]2([H])C1)=O)CC3=CC=CC=C3.[0.5Ca2+]
参考文献

[1]. Kiyoshi Ichikawa, Tokuhisa Yamato, Kazuma Ojima, et al. Effect Of Kad-1229, A Novel Hypoglycaemic Agent, On Plasma Glucose Levels After Meal Load In Type 2 Diabetic Rats. Clinical and Experimental Pharmacology and Physiology. 2002, 29 (5-6): 423-427

[2]. Sunaga Y, Gonoi T, Shibasaki T, et al. The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide.European Journal of Pharmacology.2001, 431(1):119

[3]. Kiyoshi Ichikawa, Kazuyasu Maruyama, Makoto Murakami, et al. Absence of exacerbation of myocardial stunning in anesthetized dogs treated with KAD-1229, a novel hypoglycemic agent. European Journal of Pharmacology.2001, 3(23): 331-338

[4]. Ohnota H, Kitamura T, Kinukawa M, et al. A rapid- and short-acting hypoglycemic agent KAD-1229 improves post-prandial hyperglycemia and diabetic complications in streptozotocin-induced non-insulin-dependent diabetes mellitus rats. Japanese Journal of Phar

[5]. Hideo Mogamia, Hiroshi Shibataa, Romi Nobusawaa, et al. Inhibition of ATP-sensitive K+ channel by a non-sulfonylurea compound KAD-1229 in a pancreatic β-cell line, MIN 6 cell.. European Journal of Pharmacology: Molecular Pharmacology. 1994, 269(3): 293-29


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(20s)人参皂苷 Rg3



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Endoxifen Z-异构体盐酸盐



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3-肟-6,7-二氯-1H-吲哚-2,3-二酮



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奎宁






?米格列奈钙物理化学性质






































密度 1.175
沸点 519.6?C at 760 mmHg
熔点 146-148?C
分子式 C19H24NO3Ca0.5
分子量 334.44
闪点 268?C
PSA 102.45000
LogP 5.59450
外观性状 白色晶体粉末
蒸汽压 1.27E-11mmHg at 25°C
储存条件 room temp






?米格列奈钙安全信息
























危害码 (欧洲)
Xi
风险声明 (欧洲)
R36/37/38
安全声明 (欧洲)
36
危险品运输编码 NONH for all modes of transport
海关编码 2942000000











?米格列奈钙海关









海关编码 2942000000








?米格列奈钙文献26

更多文献














Efficacy and safety of mitiglinide versus nateglinide in newly diagnose patients with type 2 diabetes mellitus: a randomized double blind trial.

Diabetes Obes. Metab. 14(2) , 187-9, (2012)

This study was performed to examine the efficacy and safety of mitiglinide in type 2 diabetes patients (T2DM). Enrolled patients had received treatment with diet and exercise in the previous 3 months …





Comparison of the rapidity of onset of the therapeutic effect between nateglinide and mitiglinide by PK/PD analysis in rats.

Eur. J. Drug Metab. Pharmacokinet. 37(1) , 9-15, (2012)

Nateglinide and mitiglinide are immediate short-acting insulinotropic agents. Both are administered preprandially to control postprandial hyperglycemia. Glinide drugs are characterized by immediate on…





Variations in tissue selectivity amongst insulin secretagogues: a systematic review.

Diabetes Obes. Metab. 14(2) , 130-8, (2012)

Insulin secretagogues promote insulin release by binding to sulfonylurea receptors on pancreatic β-cells (SUR1). However, these drugs also bind to receptor isoforms on cardiac myocytes (SUR2A) and vas…









?米格列奈钙英文别名






























Mitiglinide


Mitiglinide calcium


MFCD08458378


(aS,3aR,7aS)-Octahydro-g-oxo-a-(phenylmethyl)-2H-isoindole-2-butanoic acid calcium salt


[2(S)-cis]-Octahydro-g-oxo-a-(phenylmethyl)-2H-isoindole-2-butanoic acid calclium salt


Mitiglinide hemicalcium salt


Mitiglinide (Calcium)








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