[CAS NO. 1003005-29-5] TA-1887
PRODUCTS SPECIFICATIONS [1003005-29-5]
DESCRIPTION [1003005-29-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 427.47 |
| Molecular Formula | C24H26FNO5 |
| SMILES | FC1=C2C(N([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)C=C2CC4=CC=C(C5CC5)C=C4)=CC=C1 |
Summary
IC50 & Target
|
SGLT2 1.4 nM (IC 50 ) |
SGLT1 230 nM (IC 50 ) |
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
| 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.
|
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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.
- [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.
- [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.