TA-1887 (JNJ-39933673) 是一种高效的、选择性的、具有口服活性的SGLT2抑制剂 (IC50: 1.4 nM)，具有降血糖作用。TA-1887 可用于糖尿病研究。
| 生物活性 | TA-1887 (JNJ-39933673) is a highly potent, selective and orally activeSGLT2inhibitor (IC50: 1.4 nM) with antihyperglycemic effects. TA-1887 can be used in the research of diabetes[1][2]. |
| IC50& Target[1] | SGLT2 1.4 nM (IC50) | SGLT1 230 nM (IC50) |
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体内研究
(In Vivo) | TA-1887 (30 mg/kg, oral administration, rats) induces glucose excretion over a 24 h period of 2502 mg per 200 g body weight[1].
TA-1887 (3 mg/kg, oral administration) reduces blood glucose levels without influencing food intake in hyperglycemic high-fat diet-fed KK (HF-KK) mice[1].
TA-1887 (30 mg/kg/day, oral gavage for 2 weeks) significantly reduces GFR (glomerular filtration rate) in BSA-overloaded diabetic mice[2].
TA-1887 (0.01% w/w in chow, HF diets fed mice) antagonizes diabetic cachexia and decreases mortality in diabetic mice[3].
| Animal Model: | Sprague-Dawley rats[1] | | Dosage: | 30 mg/kg | | Administration: | Oral administration | | Result: | Induced extensive UGE (urinary glucose excretion) through continuous suppression of renal glucose reuptake. |
| Animal Model: | BSA-overloaded diabetic mice[2] | | Dosage: | 30 mg/kg | | Administration: | Oral gavage for 2 weeks | | Result: | Suppressed the induction of TGF‐β2 level in vehicle‐ reated BSA‐overloaded diabetic mice.
Suppressed COL3 gene levels. |
| Animal Model: | Male Sprague-Dawley rats (pharmacokinetic assay)[1] | | Dosage: | 3 mg/kg (i.v.), 10 mg/kg (p.o.) | | Administration: | Oral administration (p.o.), intravenous injection (i.v.) | | Result: | Pharmacokinetic (PK) parameters of TA-1887.
| Parameters | dose (mg/kg) | Cmax(ng/mL) | t1/2(h) | F (%) | |
| TA-18873 | (i.v.) | | 3.9 | | |
| TA-18873 | 10 (p.o.) | 2723 | 3.9 | 78 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
