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抑制剂/激活剂

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凋亡与自噬

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Canagliflozin 卡格列净; JNJ 28431754

Canagliflozin (TA 7284, JNJ 28431754)是一种高效的，选择性SGLT2抑制剂，作用于hSGLT2，无细胞试验中IC50为2.2 nM，比作用于hSGLT1选择性高413倍

货号：
TK0217
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	842133-18-0
生物活性	Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.
分子式	C24H25FO5S
分子量	444.52
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : ≥ 50 mg/mL (112.48 mM)
体内研究	Canagliflozin (30 mg/kg treatment for 4 weeks) reduces blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice. Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats.
体外研究	Canagliflozin inhibits Na-dependent C-AMG uptake in CHO-hSGLT2 cells, with an IC50 of 4.4±1.2 nM. Similar IC50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 684±159 nM and >1,000 nM, respectively.
文献	•Nature. 2018 Aug;560(7719):499-503. •Mol Cell. 2020 Oct 1;80(1):87-101.e5. •Cardiovasc Res. 02 November 2020. •Mol Metab. 2019 Jan;19:1-12. •Biomed Pharmacother. 2020 Dec;132:110821. •Biochem Pharmacol. 2020 May;175:113856. •Biochem Pharmacol. 2018 Jun;152:45-59. •Vascul Pharmacol. 2018 Oct;109:56-71. •Int J Oncol. 2020 Nov;57(5):1223-1233. •Int Immunopharmacol. 2020 Nov;88:106969. •Sci Rep. 2021 Jul 1;11(1):13700. •Int J Med Sci. 2018 Jun 13;15(9):937-943. •Mol Med Rep. 2021 Oct;24(4):703. •Biomed Chromatogr. 2019 Nov;33(11):e4663. •Biomed Chromatogr. 2016 Oct;30(10):1549-55.
纯度及产品资料	98%

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