Mitiglinide calcium hydrate|207844-01-7|-陌孚医药/Medlife

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Mitiglinide calcium hydrate

目录号: PL09934 纯度: ≥99%

CAS No. :207844-01-7

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中文名称	Mitiglinide calcium hydrate
中文别名	米格列奈钙;(2S)-2-苄基-3-(顺式全氢异吲哚-2-羰基)丙酸钙二水合物;米格列奈钙水合物;他克莫司;米格列奈(钙盐,水合物)
英文名称	Mitiglinide calcium hydrate
英文别名	Mitiglinide Calcium;(S)-2-Benzyl-4-oxo-4-(cis-perhydroisoindol-2-yl)butyric acid calcium salt dihydrate;(aS,3aR,7aS)-Octahydro-gamma-oxo-alpha-(phenylmethyl)-2H-isoindole-2-butanoic acid calcium salt dihydrate;KAD-1229 Calcium Hydrate;KAD-1229 CALCIUM HYDRATE,WHITE SOLID;Mitiglinide Calcium Hydrate;3006 MITIGLINIDE CALCIUM HYDRATE;Mitiglinide calciuM salt dihydrate;S-21403 calcium hydrate;Mitiglinide calcium dihydrate;Glufast;9651C21W3Z;calcium;(2S)-4-[(3aR,7aS)-1,3,3a,4,5,6,7,7a-octahydroisoindol-2-yl]-2-benzyl-4-oxobutanoate;dihydrate;Glinsuna;Glufast (TN);DSSTox_CID_26728;DSSTox_RID_81858;DSSTox_GSID_46728;Mitiglinide calcium hydr
Cas No.	207844-01-7
分子式	C₃₈H₅₂CaN₂O₈
分子量	704.91
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Mitiglinide calcium hydrate (KAD-1229) 属于促胰岛素化合物，是一种 ATP 敏感的 K⁺ 通道 (K_ATP channel) 拮抗剂。Mitiglinide Calcium hydrate 对 Kir6.2/SUR1 复合物 (胰腺-细胞 K_ATP 通道) 具有高度特异性。Mitiglinide Calcium hydrate 可用于 2 型糖尿病的研究。

生物活性

Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K (K ATP ) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K ATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes.

性状

Solid

IC50 & Target[1][2]

KATP channel

体外研究(In Vitro)

Mitiglinide calcium hydrate inhibits the Kir6.2/SUR1 channel currents in a dose-dependent manner (IC50 value, 100 nM) but does not significantly inhibit either Kir6.2/SUR2A or Kir6.2/SUR2B channel currents even at high doses (more than 10 μM) in COS-1 cells.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Mitiglinide Calcium hydrate (1-3 mg/kg; p.o.) suppresses the increase in plasma glucose levels seen after a meal load and the area under the curve for plasma glucose levels (AUCglucose) up to 5 h after the meal load.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Y Sunaga, 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. Eur J Pharmacol. 2001 Nov 9;431(1):119-25.
[2]. Kiyoshi Ichikawa, et al. Effect of KAD-1229, a novel hypoglycaemic agent, on plasma glucose levels after meal load in type 2 diabetic rats. Clin Exp Pharmacol Physiol. May-Jun 2002;29(5-6):423-7.

溶解度数据	In Vitro: DMSO : 25 mg/mL (70.93 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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