GNF362
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- CAS号:
- 1003019-41-7
- 英文名:
- GNF362
- 英文别名:
- GNF362;GNF362,GNF-362;Benzonitrile, 4-[4-[[(3R)-3-methyl-4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]methyl]-1H-pyrazol-3-yl]-
- 中文名:
- GNF362
- 中文别名:
- 化合物 T11446
- CBNumber:
- CB35821465
- 分子式:
- C22H21F3N6
- 分子量:
- 426.44
- MOL File:
- 1003019-41-7.mol
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GNF362化学性质
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沸点:
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623.9±55.0 °C(Predicted)
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密度:
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1.38±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 125 mg/mL (293.12 mM)
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酸度系数(pKa):
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13.04±0.50(Predicted)
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GNF362性质、用途与生产工艺
GNF362 是肌醇三磷酸3'激酶 B (Itpkb) 的选择性，有效且可口服生物利用的抑制剂，IC50为 9 nM。 GNF362 还抑制 Itpka 和 Itpkc，IC50 值分别为 20 nM 和 19 nM。 肌醇三磷酸3'激酶 B (Itpkb) 是一种 Ca2+ 依赖性激酶，其磷酸化 Ins (1,4,5) P3 的 3' 位置，生成肌醇 1,3,4,5-四磷酸 [Ins (1,3,4,5) P4]。
GNF362 (0-10 mM) blocks Ins (1,3,4,5) P4 production, enhances antigen receptor-driven Ca
2+
responses and lead to apoptosis of activated T cells in an Itpkb-dependent manner in lymphocytes.
GNF362 augments SOC responses following antigen receptor cross-linking, with an EC
50
of 12 nM in primary B or T lymphocytes.
GNF362 (orally administration; 6 or 20 mg/kg; twice daily; 21 days) shows minimal block in antibody production but shows significant inhibition of joint swelling at 6 mg/kg, reduces inflammatory cell infiltrate, joint damage, and proteoglycan loss at 20 mg/kg.
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Animal Model:
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A Lewis rat antigen-induced arthritis (rAIA) model
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Dosage:
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6 or 20 mg/kg
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Administration:
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Orally administration; 6 or 20 mg/kg; twice daily; 21 days
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Result:
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Reduced knee swelling in both the 20mg/kg and 6mg/kg treatment groups of GNF362 by 47% and 34%, respectively.
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GNF362
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上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-126750 | GNF362 | | 1 mg | 1590元 |
| 2024/04/30 | HY-126750 | GNF362
GNF362 | 1003019-41-7 | 10mM * 1mLin DMSO | 3280元 |
1003019-41-7, GNF362 相关搜索:
- 化合物 T11446
- 1003019-41-7
- Benzonitrile, 4-[4-[[(3R)-3-methyl-4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]methyl]-1H-pyrazol-3-yl]-
- GNF362,GNF-362
- GNF362