| fluoro-Dapagliflozinselective sodium-glucose cotransporter (SGLT) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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Chemical structure
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| Cas No. | 1181681-43-5 | SDF | Download SDF |
| Synonyms | flouro-DAPA | ||
| Chemical Name | (1S)-1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-4-deoxy-4-fluoro-D-glucitol | ||
| Canonical SMILES | ClC(C=CC([C@H]1[C@H](O)[C@@H](O)[C@H](F)[C@@H](CO)O1)=C2)=C2CC3=CC=C(OCC)C=C3 | ||
| Formula | C21H24ClFO5 | M.Wt | 410.9 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Ki: 5.3 and 330 nM for SGLT2 and SGLT1, respectively
fluoro-Dapagliflozin is a selective sodium-glucose cotransporter (SGLT) inhibitor.
Human Na(+)-D-glucose cotransporter (hSGLT) inhibitors constitute the newest class of diabetes drugs, blocking up to in-vivo 50% of renal glucose reabsorption.
In vitro: Dapagliflozin and fluoro-dapagliflozin could block glucose transport and glucose-coupled currents with around 100-fold specificity for hSGLT2 over hSGLT1. It was found that phlorizin and galacto-dapagliflozin rapidly dissociated from SGLT2, while fluoro-dapagliflozin dissociated from hSGLT2 at a rate 10-fold slower. In contrast, fluoro-dapagliflozin could quickly dissociate from hSGLT1 [1].
In vivo: Dapagliflozin, the close analog of fluoro-dapagliflozin, could acutely induce renal glucose excretion in normal and diabetic rats, improve glucose tolerance in normal rats, and reduce hyperglycemia in Zucker diabetic fatty at doses ranging from 0.1 to 1.0 mg/kg. Moreover, the once-daily dapagliflozin treatment was able to significantly lower fasting and fed glucose levels and led to a significant increase in glucose utilization rate [2].
Clinical trial: Clinical study found that dapagliflozin could lower hyperglycemia in treatment-naive patients with newly diagnosed type 2 diabetes, which made dapagliflozin a unique addition to existing treatment options for type 2 diabetes [3].
References:[1] Hummel, C. S.,Lu, C.,Liu, J., et al. Structural selectivity of human SGLT inhibitors. American Journal of Physiology.Cell Physiology 302(2), C373-C382 (2012).[2] Han, S. ,Hagan, D.L.,Taylor, J.R., et al. Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes 57, 1723-1729 (2008).[3] Ferrannini E, Ramos SJ, Salsali A, Tang W, List JF. Dapagliflozin monotherapy in type 2 diabetic patients with inadequate glycemic control by diet and exercise: a randomized, double-blind, placebo-controlled, phase 3 trial. Diabetes Care. 2010 Oct;33(10):2217-24.
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请问各位大神，做注射液中试时所用到磁力搅拌器需要资质吗？
加入溶液把搅拌子放在烧杯溶液中，将控温探头固定在橡胶夹头上，加热头插入至溶液中，不能影响到搅拌子，然后先插上仪器接插的电源插头，再接通电源打开电源调速开关，指标灯亮，即开始工作。
调速是由低速逐步调至高速，不允许高速档直接起动，以免搅拌子不同步，引起跳动。加热有开关控制，打开加热源开关，选择所需的温度，绿灯亮表明加热盘工作，红灯亮表明停止加热盘工作，此时进入恒温状态，不工作时应切断电源，为确保安全，使用时请接上地线．仪器应保持清洁干燥，严禁溶液进入机内，以免损坏机件防止剧烈震动．向左转|向右转
裂解液配方：
尿素7M
硫脲2M
CHAPS4%
二次水至20ml
使用前加DTT至65mM，tris至40mM，PMSF至1mM
上样液配方：
尿素8M
CHAPS2%
1%溴酚蓝0.002%
二次水至10ml
使用前加DTT至18mM，IPGbuffer至0.5%
由于都含有尿素，特别难溶解，好像含有尿素的温度不能超过37度，就在磁力搅拌器上一直搅着，发现过了一两个小时还没溶解，怎么回事么？中间还在34度左右水浴锅里水浴过，还是没溶解，溅在烧杯壁上的液体都已经结晶了。
有人碰到这样的问题么，很着急，急求帮助。
1.裂解液和上样液配方有无问题？
2.尿素怎么老不容，有没有什么方法加速其溶解？
本人想买一台制备胶体金的加热磁力搅拌器，大家帮忙推荐下什么品牌的较好，谢谢
鸣谢！
