Mitiglinide (Calcium)

Names

[ Name ]:
Mitiglinide (Calcium)

[Synonym ]:
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)

Biological Activity

[Description]:

Mitiglinide(KAD-1229; S21403) is a drug for the treatment of type 2 diabetes; it is a highly selective KATP channel antagonist. IC50 value:Target: KATP channelMitiglinide is a hypoglycemic agent that closes adenosine triphosphate (ATP)-sensitive potassium channels (KATP channel s) in the pancreatic β-islet cells. Mitiglinide stimulates insulin secretion by stimulating Ca2+ influx.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

Research Areas >> Metabolic Disease

[References]

[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

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.175

[ Boiling Point ]:
519.6ºC at 760 mmHg

[ Melting Point ]:
146-148ºC

[ Molecular Formula ]:
C₁₉H₂₄NO₃Ca_0.5

[ Molecular Weight ]:
334.44

[ Flash Point ]:
268ºC

[ PSA ]:
102.45000

[ LogP ]:
5.59450

[ Vapour Pressure ]:
1.27E-11mmHg at 25°C

[ Storage condition ]:
room temp

Safety Information

[ Hazard Codes ]:
Xi

[ Risk Phrases ]:
R36/37/38

[ Safety Phrases ]:
36

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2942000000

Customs

[ HS Code ]: 2942000000

Articles

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...