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Gliclazide

Name: Gliclazide
Brand: TargetMol
SKU: T1527
Price: 186 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.63%

货号 T1527Cas号 21187-98-4

别名 格列齐特, SE1702, S1702

Gliclazide (SE1702) 是一种有效的全细胞的 β 细胞 ATP 敏感型钾流阻断剂，IC50为 184 nM，用作降糖药。

Gliclazide

一键复制产品信息

很棒

纯度: 99.63%

货号 T1527 别名 格列齐特, SE1702, S1702Cas号 21187-98-4

Gliclazide (SE1702) 是一种有效的全细胞的 β 细胞 ATP 敏感型钾流阻断剂，IC50为 184 nM，用作降糖药。

规格	价格	库存
100 mg	¥ 186	现货
500 mg	¥ 413	现货
1 mL x 10 mM (in DMSO)	¥ 455	现货

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产品介绍

Gliclazide AI Summary

Gliclazide exhibits multifaceted biological activities, prominently demonstrating significant antihyperglycemic and antidiabetic properties. In sucrose-loaded and streptozotocin-induced diabetic Sprague-Dawley rats, it reduces blood glucose levels by 40.4% and 27.7%, respectively, at an oral dosage of 100 mg/kg. It also shows similar activity in various other hyperglycemic and diabetic animal models, including a 44.8% glucose reduction in sucrose-challenged Charles Foster/Wistar rats and a 17.4% reduction in C57BL/Ks db/db mice. Additionally, it modulates human MRP2-mediated estradiol-17-beta-glucuronide transport with an activity level of 174.0%. The compound impacts various enzymes and cellular functions, inhibiting ALDH1A1 (39810.7 nM), lipid storage modulation in Drosophila cells (4.6 nM), Bacillus subtilis PPTase (31622.8 nM), Fructose-1,6-bisphosphate Aldolase (8912.5 nM), and others. It also attenuates virus entry, showing moderate antiviral activity against SARS-CoV-2 and Marburg Virus with potencies greater than 20000.0 nM and 3548.1 nM, respectively. Pharmacokinetically, Gliclazide has a pKa of 5.98, low plasma protein binding (logFu = 0.09), and a moderate volume of distribution (Vdss = 0.36 L.kg-1). However, it poses a moderate hepatotoxicity risk with elevated hepatic function markers and a combined HepSE score of 4.0, indicating potential liver injury. It affects various physiological parameters such as liver and kidney function, electrolyte balance, and lipid metabolism. Additionally, Gliclazide stimulates glucose-stimulated insulin secretion in rat INS1 cells, highlighting a notable effect on insulin secretion and potentially beneficial metabolic impacts. Despite these positive activities, its bioactivity against certain human BSEP, MRP transporters, and select enzymes like AKR1C1 and AKR1C2 remains negligible, with IC50 values generally exceeding 1000000.0 nM..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Gliclazide (SE1702), an oral antihyperglycemic agent, belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating beta-cells of the pancreas to release insulin.
靶点活性	K+ channel:184 nM
别名	格列齐特, SE1702, S1702

化学信息

分子量	323.41
分子式	C₁₅H₂₁N₃O₃S
CAS No.	21187-98-4
Smiles	CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN1CC2CCCC2C1
密度	1.35 g/cm3
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 45 mg/mL (139.14 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.18 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0921 mL	15.4603 mL	30.9205 mL	154.6025 mL
5 mM	0.6184 mL	3.0921 mL	6.1841 mL	30.9205 mL
10 mM	0.3092 mL	1.5460 mL	3.0921 mL	15.4603 mL
20 mM	0.1546 mL	0.7730 mL	1.5460 mL	7.7301 mL
50 mM	0.0618 mL	0.3092 mL	0.6184 mL	3.0921 mL
100 mM	0.0309 mL	0.1546 mL	0.3092 mL	1.5460 mL