TA-1887
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.
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- No. CAS: 1003005-29-5
- Fòrmula: C24H26FNO5
- Peso molecular:427.47
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
SGLT2 1.4 nM (IC50) |
SGLT1 230 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | EC50 |
1.9 nM
Compound: 6
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Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as reduction in [14C]-alpha-methylglucopyranoside uptake after 2 hrs by liquid scintillation counting
Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as reduction in [14C]-alpha-methylglucopyranoside uptake after 2 hrs by liquid scintillation counting
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[PMID: 21090651] |
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats[1]
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Dosage:30 mg/kg
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Administration:Oral administration
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Result:Induced extensive UGE (urinary glucose excretion) through continuous suppression of renal glucose reuptake.
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Animal Model:BSA-overloaded diabetic mice[2]
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Dosage:30 mg/kg
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Administration:Oral gavage for 2 weeks
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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]
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Dosage:3 mg/kg (i.v.), 10 mg/kg (p.o.)
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Administration:Oral administration (p.o.), intravenous injection (i.v.)
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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
Chemical Information
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No. CAS 1003005-29-5
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Peso molecular 427.47
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Fòrmula C24H26FNO5
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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
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Synonyms
JNJ-39933673
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TA-1887 Related Classifications
HY-12608 Related Classifications
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