6-(3-氟苯基)-N-[1-(2,2,2-三氟乙基)-4-哌啶基]-3-吡啶羧酰胺
- CAS号:1033836-12-2
- 英文名:3-PYRIDINECARBOXAMIDE, 6-(3-FLUOROPHENYL)-N-[1-(2,2,2-TRIFLUOROETHYL)-4-PIPERIDINYL]-
- 中文名:6-(3-氟苯基)-N-[1-(2,2,2-三氟乙基)-4-哌啶基]-3-吡啶羧酰胺
- CBNumber:CB22599009
- 分子式:C19H19F4N3O
- 分子量:381.37
- MOL File:1033836-12-2.mol
- 沸点 :487.2±45.0 °C(Predicted)
- 密度 :1.33±0.1 g/cm3(Predicted)
- 储存条件 :2-8°C
- 溶解度 :Soluble in DMSO
- 形态 :crystalline solid
- 酸度系数(pKa) :9.55±0.20(Predicted)
- 颜色 :White to off-white
6-(3-氟苯基)-N-[1-(2,2,2-三氟乙基)-4-哌啶基]-3-吡啶羧酰胺性质、用途与生产工艺
- 生物活性 HPGDS inhibitor 1 是一种有效的,选择性的和具有口服活性的 HPGDS 抑制剂,在酶和细胞分析中的 IC50 值分别为 0.6 nM 和 32 nM。HPGDS inhibitor 1 不抑制人 L-PGDS,mPGES,COX-1,COX-2 或 5-LOX。
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靶点
IC50: 0.6 nM (HPGDS in enzyme assays) and 32 nM (HPGDS in cellular assays)
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体外研究
HPGDS inhibitor 1 has equal potency against purified HPGDS from human, rat, dog, and sheep (IC 50 , 0.5-2.3 nM).
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体内研究
HPGDS inhibitor 1 (compound 8; 1 mg/kg) has excellent PK characteristics with 76% bioavailability, and the T 1/2 is 4.1 hours in rats.
Rats dosed orally with 1 mg/kg and 10 mg/kg HPGDS inhibitor 1 (compound 8) are sacrificed at various times. Oral administration of HPGDS inhibitor 1 blocks PGD2 production in the rat spleen; inhibition of PGD2 is inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time- and dose-dependent manner.
HPGDS inhibitor 1 (compound 8; 1 mg/mL) illustrates efficacy in an in vivo sheep model of asthma.
- 更新日期:2025/02/08
- 产品编号:HY-10439
- 产品名称:6-(3-氟苯基)-N-[1-(2,2,2-三氟乙基)-4-哌啶基]-3-吡啶羧酰胺 HPGDS inhibitor 1
- CAS编号:1033836-12-2
- 包装:1 mg
- 价格:359元
- 更新日期:2025/02/08
- 产品编号:HY-10439
- 产品名称:6-(3-氟苯基)-N-[1-(2,2,2-三氟乙基)-4-哌啶基]-3-吡啶羧酰胺 HPGDS inhibitor 1
- CAS编号:1033836-12-2
- 包装:10mM * 1mLin DMSO
- 价格:963元
- 公司名称:A.J Chemicals
- 联系电话:--
- 电子邮件:sales@ajchem.in
- 国家:印度
- 产品数:6100
- 优势度:58