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- 详细信息
- 技术资料
- 库存：
36
- 英文名：
Tofogliflozin (CSG452)
- CAS号：
903565-83-3
- 供应商：
上海莼试
- 保存条件：
Store at -20°C
- 规格：
2mg 5mg 10mg 50mg
使用方法：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
商品属性：
产品描述：
分子式:C22H26O6
分子量:386.44
溶解度:Soluble in DMSO
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.IC50 value: 2.9/14.9/6.4 nM(human/rat/mouse SGLT2) [1]Target: SGLT2 inhibitorin vitro: Tofogliflozin competitively inhibited SGLT2 in cells overexpressing SGLT2, and K(i) values for human, rat, and mouse SGLT2 inhibition were 2.9, 14.9, and 6.4 nM, respectively. The selectivity of tofogliflozin toward human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1 was the highest among the tested SGLT2 inhibitors under clinical development [1]. tofogliflozin was catalyzed to the primary hydroxylated derivative (M4) by CYP2C18, CYP4A11 and CYP4F3B, then M4 was oxidized to M1. 3. Tofogliflozin had no induction potential on CYP1A2 and CYP3A4 [4].in vivo: A single oral gavage of tofogliflozin increased renal glucose clearance and lowered the blood glucose level in Zucker diabetic fatty rats. Tofogliflozin also improved postprandial glucose excursion in a meal tolerance test with GK rats. In db/db mice, 4-week tofogliflozin treatment reduced glycated hemoglobin and improved glucose tolerance in the oral glucose tolerance test 4 days after the final administration [1]. Tofogliflozin (400 ng/ml) induced UGE of about 2 mg.kg?1.min?1 and increased EGP by 1-2 mg.kg?1.min?1, resulting in PG in the normal range [2]. Tofogliflozin suppressed plasma glucose and glycated Hb and preserved pancreatic beta-cell mass and plasma insulin levels. No improvement of glycaemic conditions or insulin level was orved with losartan treatment [3].[1]. Nagata T, et al. Tofogliflozin, a novel sodium-glucose co-transporter 2 inhibitor, improves renal and pancreatic function in db/db mice. Br J Pharmacol. 2013 Oct;170(3):519-31. [2]. Yamane M, et al. In vitro profiling of the metabolism and drug-drug interaction of tofogliflozin, a potent and highly specific sodium-glucose co-transporter 2 inhibitor, using human liver microsomes, human hepatocytes, and recombinant human CYP. Xenobioti [3]. Suzuki M, et al. Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice. J Pharmacol Exp Ther. 2012 Jun;341(3):692-701. [4]. Nagata T, et al. Selective SGLT2 inhibition by tofogliflozin reduces renal glucose reabsorption under hyperglycemic but not under hypo- or euglycemic conditions in rats. Am J Physiol Endocrinol Metab. 2013 Feb 15;304(4):E414-23.
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
公司正在出售的产品：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
商品属性：
| 货号 | CS-01Y68712 | 规格 | 2mg 5mg 10mg 50mg |
| CAS号 | 903565-83-3 | 分子量 | 386.44 |
| 含量 | >98.00% | 别名 | N/A |
| 分子式 | C22H26O6 | 化学名 | N/A |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C22H26O6
分子量:386.44
溶解度:Soluble in DMSO
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.IC50 value: 2.9/14.9/6.4 nM(human/rat/mouse SGLT2) [1]Target: SGLT2 inhibitorin vitro: Tofogliflozin competitively inhibited SGLT2 in cells overexpressing SGLT2, and K(i) values for human, rat, and mouse SGLT2 inhibition were 2.9, 14.9, and 6.4 nM, respectively. The selectivity of tofogliflozin toward human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1 was the highest among the tested SGLT2 inhibitors under clinical development [1]. tofogliflozin was catalyzed to the primary hydroxylated derivative (M4) by CYP2C18, CYP4A11 and CYP4F3B, then M4 was oxidized to M1. 3. Tofogliflozin had no induction potential on CYP1A2 and CYP3A4 [4].in vivo: A single oral gavage of tofogliflozin increased renal glucose clearance and lowered the blood glucose level in Zucker diabetic fatty rats. Tofogliflozin also improved postprandial glucose excursion in a meal tolerance test with GK rats. In db/db mice, 4-week tofogliflozin treatment reduced glycated hemoglobin and improved glucose tolerance in the oral glucose tolerance test 4 days after the final administration [1]. Tofogliflozin (400 ng/ml) induced UGE of about 2 mg.kg?1.min?1 and increased EGP by 1-2 mg.kg?1.min?1, resulting in PG in the normal range [2]. Tofogliflozin suppressed plasma glucose and glycated Hb and preserved pancreatic beta-cell mass and plasma insulin levels. No improvement of glycaemic conditions or insulin level was orved with losartan treatment [3].[1]. Nagata T, et al. Tofogliflozin, a novel sodium-glucose co-transporter 2 inhibitor, improves renal and pancreatic function in db/db mice. Br J Pharmacol. 2013 Oct;170(3):519-31. [2]. Yamane M, et al. In vitro profiling of the metabolism and drug-drug interaction of tofogliflozin, a potent and highly specific sodium-glucose co-transporter 2 inhibitor, using human liver microsomes, human hepatocytes, and recombinant human CYP. Xenobioti [3]. Suzuki M, et al. Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice. J Pharmacol Exp Ther. 2012 Jun;341(3):692-701. [4]. Nagata T, et al. Selective SGLT2 inhibition by tofogliflozin reduces renal glucose reabsorption under hyperglycemic but not under hypo- or euglycemic conditions in rats. Am J Physiol Endocrinol Metab. 2013 Feb 15;304(4):E414-23.
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
公司正在出售的产品：
| Recombnant Human PROK2, N-GT | Recombnant Lyophophatdylcholne Acyltranferae 1 (LPCAT1) |
| Recombnant Lyophophatdylcholne Acyltranferae 2 (LPCAT2) | 细胞膜钙ATP酶1封闭多肽 |
| Recombnant Lyophophatdylcholne Acyltranferae 3 (LPCAT3) | 溴区结构域相邻锌指蛋白1A封闭多肽 |
| Recombnant Galactoylceramdae (GALC) | 硫代硫酸硫转移酶封闭多肽 |
| Recombnant Arylulfatae B (ARB) | 磷酸化血小板源性生长因子受体-B封闭多肽 |
| Recombnant Glycne-N-Methyltranferae (GNMT) | 配对盒基因5封闭多肽 |
| Recombnant Myo notol Oxygenae (MOX) | 磷酸化原癌基因c-Raf封闭多肽 |
| Recombnant Trehalae (TREH) | Bcl-2封闭多肽 |
| Recombnant Uracl DNA Glycoylae (UNG) | 细胞表面趋化因子受体4相关蛋白4封闭多肽 |
| Recombnant UDP Glycoyltranferae 8 (UGT8) | 低密度脂蛋白受体结构域蛋白1封闭多肽 |
| Recombnant Ubqutn Carboxyl Termnal Hydrolae L1 (UCHL1) | 生长休止特定蛋白1封闭多肽 |
| Recombnant Ubquln 2 (UBQLN2) | TWK相关酸敏感钾离子通道蛋白9封闭多肽 |
| Recombnant Thymdylate ynthetae (TYM) | Tofogliflozin (CSG452)6号染色体开放阅读框223封闭多肽 |
| Recombnant Glutaredoxn 3 (GLRX3) | 睾丸特异激酶底物蛋白封闭多肽 |
| PERQ1蛋白封闭多肽 | 肾脏和脑蛋白封闭多肽 |
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Tofogliflozin (CSG452)
￥600 - 3200
