规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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10mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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体外研究 (In Vitro) |
在 CHO-hSGLT2 细胞中,canagliflozin 抑制 Na+ 依赖性 14C-AMG 摄取,IC50 为 4.4±1.2 nM。在 CHO-mSGLT2 和 CHO-rSGLT2 细胞中,大鼠和小鼠 SGLT2 的 IC50 值分别为 2.0 nM 和 3.7 nM。 Canagliflozin 抑制 CHO-hSGLT1 和 mSGLT1 细胞中 14C-AMG 的吸收,IC50 分别为 684±159 nM 和 >1,000 nM[1]。
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体内研究 (In Vivo) |
在 DIO 小鼠中,卡格列净 (30 mg/kg) 治疗 4 周可降低体重增加、呼吸交换率和血糖 (BG) 水平[1]。给予卡格列净(3 mg/kg)三周后,与媒介物治疗的大鼠相比,用 ZF 治疗的大鼠由于尿葡萄糖排泄(UGE)增加而出现体重减轻,但总食物消耗量没有显着变化[1]。
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动物实验 |
Animal/Disease Models: Diet-induced obese, insulin resistantmice (DIO) Mice[1]
Doses: 30 mg/kg Route of Administration: po (oral gavage); daily; 4 weeks Experimental Results: decreased BG levels, respiratory exchange ratio, and body weight gain. Animal/Disease Models: Male Zucker fatty (ZF) obese, insulin resistant rats[1] Doses: 3 mg /kg Route of Administration: po (oral gavage); daily; 3 weeks Experimental Results: UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight. |
参考文献 |
[1]. Liang Y, et al. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS One. 2012;7(2):e30555.
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分子式 |
C48H52F2O11S2
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分子量 |
907.05
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CAS号 |
928672-86-0
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相关CAS号 |
Canagliflozin;842133-18-0
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SMILES |
S1C(C2C([H])=C([H])C(=C([H])C=2[H])F)=C([H])C([H])=C1C([H])([H])C1=C(C([H])([H])[H])C([H])=C([H])C(=C1[H])[C@@]1([H])[C@@]([H])([C@]([H])([C@@]([H])([C@@]([H])(C([H])([H])O[H])O1)O[H])O[H])O[H]
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别名 |
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% CMC+0.25% Tween 80 :18 mg/mL 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 1.1025 mL | 5.5124 mL | 11.0248 mL | |
5 mM | 0.2205 mL | 1.1025 mL | 2.2050 mL | |
10 mM | 0.1102 mL | 0.5512 mL | 1.1025 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 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。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。