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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1003005-29-5
- 分子式: C24H26FNO5
- 分子量:427.47
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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] |
体内実験
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
化学情報
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CAS 番号 1003005-29-5
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分子量 427.47
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分子式 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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別名
JNJ-39933673
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TA-1887 関連分類
HY-12608 関連分類
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