JNJ-39933673

• 常用名: JNJ-39933673
• 英文名: JNJ-39933673
• CAS号: 1003005-29-5
• 分子量: 427.46500
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₂₆FNO₅
• 熔点: N/A
• 闪点: N/A

JNJ-39933673用途

TA-1887(JNJ-39933673)是一种高效、选择性和口服活性SGLT2抑制剂(IC50:1.4nM),具有降血糖作用。TA-1887可用于糖尿病研究[1][2]。

JNJ-39933673名称

• 英文名: (2R,3R,4S,5S,6R)-2-[3-[(4-cyclopropylphenyl)methyl]-4-fluoroindol-1-yl]-6-(hydroxymethyl)oxane-3,4,5-triol

JNJ-39933673生物活性

• 描述: TA-1887(JNJ-39933673)是一种高效、选择性和口服活性SGLT2抑制剂(IC50:1.4nM),具有降血糖作用。TA-1887可用于糖尿病研究[1][2]。
• 相关类别:
  研究领域 >> 代谢疾病
  信号通路 >> 跨膜转运 >> SGLT
• 靶点实验:

  SGLT2:1.4 nM (IC50)

  SGLT1:230 nM (IC50)

• 体内研究: TA-1887(30 mg/kg,口服,大鼠)在每200 g体重2502 mg的24小时内诱导葡萄糖排泄[1]。TA-1887(3 mg/kg,口服)在不影响高血糖高脂肪饮食喂养的KK(HF-KK)小鼠的食物摄入量的情况下降低血糖水平[1]。TA-1887(30 mg/kg/天,口服灌胃2周)显著降低BSA负荷过重糖尿病小鼠的肾小球滤过率[2]。TA-1887(0.01%w/w,喂食含HF食物的小鼠)对抗糖尿病恶病质,并降低糖尿病小鼠的死亡率[3]。动物模型：Sprague-Dawley大鼠[1]剂量：30mg/kg给药：口服结果：通过持续抑制肾葡萄糖再摄取,诱导大范围UGE(尿糖排泄)。动物模型：BSA超载糖尿病小鼠[2]剂量：30 mg/kg给药：口服灌胃2周结果：抑制载体治疗的BSA超限糖尿病小鼠TGF-β2水平的诱导。抑制COL3基因水平。动物模型：雄性Sprague-Dawley大鼠(药代动力学分析)[1]剂量：3 mg/kg(静脉注射),10 mg/kg(口服)给药：口服(口服),静脉注射
• 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.

  [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.

JNJ-39933673物理化学性质

• 分子式: C₂₄H₂₆FNO₅
• 分子量: 427.46500
• 精确质量: 427.18000
• PSA: 95.08000
• LogP: 2.22100
• InChIKey: PXRGAWZIQZMHTH-PFKOEMKTSA-N
• SMILES: OCC1OC(n2cc(Cc3ccc(C4CC4)cc3)c3c(F)cccc32)C(O)C(O)C1O

JNJ-39933673靶点实验

查看更多实验

实验名称：Toxicity in high-fat diet-fed KK/Ta Jcl mouse assessed as effect on food intake at 3 ... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL3110556

实验名称：Antihyperglycemic activity in high-fat diet-fed KK/Ta Jcl mouse assessed as reduction... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL3110557

实验名称：Metabolic stability in monkey intestinal microsomes assessed as compound hydrolysis b... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3110558

实验名称：Metabolic stability in dog intestinal microsomes assessed as compound hydrolysis by H... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3110559

实验名称：Metabolic stability in rat intestinal microsomes assessed as compound hydrolysis by H... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3110560

实验名称：Metabolic stability in human intestinal microsomes assessed as compound hydrolysis by... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3110561

实验名称：Intrinsic clearance in monkey intestinal microsomes after 30 mins 来源：ChEMBL 靶标：N/A External Id：CHEMBL3110562

实验名称：Intrinsic clearance in rat intestinal microsomes after 30 mins 来源：ChEMBL 靶标：N/A External Id：CHEMBL3110563

实验名称：Intrinsic clearance in dog intestinal microsomes after 30 mins 来源：ChEMBL 靶标：N/A External Id：CHEMBL3110564

实验名称：Intrinsic clearance in human intestinal microsomes after 30 mins 来源：ChEMBL 靶标：N/A External Id：CHEMBL3110565

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JNJ-39933673英文别名

• unii-q8bx693uk2
• ta-1887
• JNJ-39933673