T-1095

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

T-1095 是肾葡萄糖重吸收以及 Na+-葡萄糖协同转运蛋白 (SGLT) 和易化葡萄糖转运蛋白 2 (GLUT2) 表达的抑制剂。

T-1095 is an inhibitor of renal glucose reabsorption and the expression of Na+-glucose cotransporters (SGLTs) and facilitative glucose transporter 2 (GLUT2).(In Vivo):Administration of 0.03% and 0.1% (wt/wt diet) T-1095 to STZ rats for 4 weeks improved the hyperglycemia and dose-dependently decreased HbA1c. Moreover, treatment with 0.1% (wt/wt diet) T-1095 in STZ rats for 8 weeks not only reduced blood glucose and HbA1c, levels but also prevented the elevation of urinary albumin levels and kidney weight and the development of epithelial vacuolation. The expression of renal SGLT2, a major glucose transporter in the kidney, was not different in normal, STZ, and T-1095-treated STZ rats. In contrast, the elevated renal GLUT2 level in STZ rats was suppressed by T-1095.

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T-1095 is absorbed into the circulation via oral administration, is metabolized to the active form, T-1095A, and suppresses the activity of SGLTs in the kidney. Orally administered T-1095 (3-30 mg/kg) increases urinary glucose excretion in diabetic animals, thereby decreasing blood glucose levels.With long-term T-1095 (0.01% or 0.1% T-1095 mixed diet; for 28 days) treatment, both blood glucose and HbA1c levels were reduced in streptozotocin (STZ)-induced diabetic rats and yellow KK mice. In addition, there was amelioration of abnormal carbohydrate metabolism, i.e., hyperinsulinemia and hypertriglyceridemia, and of the development of microalbuminuria, in yellow KK mice.

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GPCR/G Protein

SGLT

SMS2

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209746-59-8

516.499

C26H28O11

>98% (HPLC)

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COC(=O)OC[C@H]1O[C@@H](Oc2cc(C)cc(O)c2C(=O)CCc2ccc3occc3c2)[C@H](O)[C@@H](O)[C@@H]1O

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(-20℃)

With Ice Pack

≥ 2 years