| Identification | Back Directory | [Name]
(2R,3R,4S,5S,6R)-2-[3-[(4-cyclopropylphenyl)methyl]-4-fluoroindol-1-yl]-6-(hydroxymethyl)oxane-3,4,5-triol | [CAS]
1003005-29-5 | [Synonyms]
(2R,3R,4S,5S,6R)-2-[3-[(4-cyclopropylphenyl)methyl]-4-fluoroindol-1-yl]-6-(hydroxymethyl)oxane-3,4,5-triol | [Molecular Formula]
C24H26FNO5 | [MDL Number]
MFCD27953017 | [MOL File]
1003005-29-5.mol | [Molecular Weight]
427.465 |
| Hazard Information | Back Directory | [Uses]
TA-1887 (JNJ-39933673) is a highly potent, selective and orally active SGLT2 inhibitor (IC50: 1.4 nM) with antihyperglycemic effects. TA-1887 can be used in the research of diabetes[1][2]. | [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‐treated BSA‐overloaded diabetic mice.
Suppressed COL3 gene levels.
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| 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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| [IC 50]
SGLT2: 1.4 nM (IC50); SGLT1: 230 nM (IC50) | [References]
[1] Sumihiro Nomura, et al. Novel Indole-N-glucoside, TA-1887 As a Sodium Glucose Cotransporter 2 Inhibitor for Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2013 Nov 13;5(1):51-5. DOI:10.1021/ml400339b
[2] Keiji Shimada, et al. Adenosine/adenosine type 1 receptor signaling pathway did not play dominant roles on the influence of sodium-glucose cotransporter 2 inhibitor in the kidney of bovine serum albumin-overloaded streptozotocin-induced diabetic mice. J Diabetes Investig. 2022 Jun;13(6):955-964. DOI:10.1111/jdi.13760
[3] Taichi Sugizaki, et al. Treatment of diabetic mice with the SGLT2 inhibitor TA-1887 antagonizes diabetic cachexia and decreases mortality. NPJ Aging Mech Dis. 2017 Sep 8;3:12. DOI:10.1038/s41514-017-0012-0 |
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