Glyburide-d3 (Synonyms:格列本脲-D3氘代内标;格列本脲-D3;格列本脲-d3(甲氧基-d3))
目录号 : KCM10715 CAS No. : 1219803-02-7 纯度 : 98%
Glyburide-d is intended for use as an internal standard for the quantification of glyburide by GC- or LC-MS. Glyburide is a sulfonylurea and an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel K6.2 (IC = 4.3 nM). It binds to microsomes derived from RINm5F pancreatic β-cells (K = 0.3 nM) and inhibits Rb efflux from intact RINm5 cells with a half-maximal inhibition (K) value of 0.06 nM. Glyburide (5 mg/kg) reduces blood glucose levels and increases the activity of hepatic glutathione-S-transferase (GST) and glucose-6-phosphate dehydrogenase (G6PDH) in a rat model of diabetes induced by streptozotocin (STZ; ). It inhibits ATP-induced increases in caspase-1 activation and IL-1β and IL-18 secretion in a concentration-dependent manner in LPS-primed bone marrow-derived macrophages (BMDMs). Glyburide (80 mg/ml) also reduces lesion growth in mice infected with L. mexicana. Formulations containing glyburide have been used in the treatment of type 2 diabetes.
规格 价格 是否有货 数量
1mg
In-stock
5mg
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10mg
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生物活性

Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.

分子式
C23H25ClD3N3O5S
分子量
497.02252
CAS号
1219803-02-7
中文名称
格列本脲-D3氘代内标
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro: 

DMSO: 100 mg/mL (201.20 mM; Need ultrasonic)

H2O: 0.1 mg/mL (0.20 mM; Need ultrasonic and warming)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 2.0120 mL 10.0600 mL 20.1199 mL
5 mM 0.4024 mL 2.0120 mL 4.0240 mL
10 mM 0.2012 mL 1.0060 mL 2.0120 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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计算结果:

工作液浓度 mg/ml;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。