Mavatrep

• 常用名: Mavatrep
• 英文名: Mavatrep
• CAS号: 956274-94-5
• 分子量: 422.44200
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₅H₂₁F₃N₂O
• 熔点: N/A
• 闪点: N/A

Mavatrep用途

Mavatrep是一种口服生物有效的TRPV1拮抗剂, 对hTRPV1通道具有高亲和力, 抑制TRPV1激动剂与[3H]-Resiniferatoxin结合(Ki=6.5 nM), 对CYP亚型 3A4, 1A2, 和 2D6的酶活性作用效果较低。

Mavatrep名称

• 中文名: Mavatrep
• 英文名: 2-[2-[2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-3H-benzimidazol-5-yl]phenyl]propan-2-ol

Mavatrep生物活性

• 描述: Mavatrep是一种口服生物有效的TRPV1拮抗剂, 对hTRPV1通道具有高亲和力, 抑制TRPV1激动剂与[3H]-Resiniferatoxin结合(Ki=6.5 nM), 对CYP亚型 3A4, 1A2, 和 2D6的酶活性作用效果较低。
• 相关类别:
  信号通路 >> 跨膜转运 >> TRP频道
  研究领域 >> 其他
• 参考文献:

  [1]. Parsons WH, et al. Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep). J Med Chem. 2015 May

Mavatrep物理化学性质

• 分子式: C₂₅H₂₁F₃N₂O
• 分子量: 422.44200
• 精确质量: 422.16100
• PSA: 48.91000
• LogP: 6.64650
• InChIKey: ORDHXXHTBUZRCN-NTEUORMPSA-N
• SMILES: CC(C)(O)c1ccccc1-c1ccc2nc(C=Cc3ccc(C(F)(F)F)cc3)[nH]c2c1
• 储存条件: 2-8℃

Mavatrep靶点实验

查看更多实验

实验名称：Toxicity in Sprague-Dawley rat assessed as increase in core body temperature at 100 m... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL3430260

实验名称：Toxicity in guinea pig assessed as induction of hemodynamic/electrocardiographic effe... 来源：ChEMBL 靶标：Cavia porcellus External Id：CHEMBL3430261

实验名称：Displacement of [3H]-astemizole from recombinant human ERG at 10 uM 来源：ChEMBL 靶标：Potassium voltage-gated channel subfamily H member 2 External Id：CHEMBL3430259

实验名称：Toxicity in Sprague-Dawley rat assessed as increase in core body temperature at 10 mg... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL3430264

实验名称：Antagonist activity at recombinant human TRPV1 expressed in HEK293 cells assessed as ... 来源：ChEMBL 靶标：Transient receptor potential cation channel subfamily V member 1 External Id：CHEMBL3429301

实验名称：Toxicity in Sprague-Dawley rat assessed as increase in core body temperature at 100 m... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL3430262

实验名称：Toxicity in Sprague-Dawley rat assessed as increase in core body temperature at 0.1 t... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL3430263

实验名称：Oral bioavailability in rat at 10 mg/kg 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL3429305

实验名称：Clearance in rat at 2 mg/kg, iv 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL3429306

实验名称：Metabolic stability in rat liver microsomes assessed as compound remaining after 10 m... 来源：ChEMBL 靶标：Liver microsome External Id：CHEMBL3429303

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Mavatrep英文别名

• Mavatrep