2-((4-(环丙烷羰基)哌嗪-1-基)甲基)苯并[D]异噻唑-3(2H)-酮
|
|
|
- CAS号:
- 877963-94-5
- 英文名:
- LOC-14
- 英文别名:
- OC14;LOC-14;LOC14, ≥98%;LOC 14;LOC14;LOC 14,inhibit,LOC14,Inhibitor,LOC-14;2-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]methyl]-1,2-benzisothiazol-3(2H)-one;2-((4-(cyclopropanecarbonyl)piperazin-1-yl)methyl)benzo[d]isothiazol-3(2H)-one;1,2-Benzisothiazol-3(2H)-one, 2-[[4-(cyclopropylcarbonyl)-1-piperazinyl]methyl]-;2-[(4-cyclopropanecarbonylpiperazin-1-yl)methyl]-2,3-dihydro-1,2-benzothiazol-3-one
- 中文名:
- 2-((4-(环丙烷羰基)哌嗪-1-基)甲基)苯并[D]异噻唑-3(2H)-酮
- 中文别名:
- 化合物LOC14;LOC14,蛋白质二硫键异构酶(PDI)调节剂;2-((4-(环丙烷羰基)哌嗪-1-基)甲基)苯并[D]异噻唑-3(2H)-酮;2-[[[4-(环丙基羰基)-1-哌嗪基]甲基] -1,2-苯并异噻唑-3(2H) - 酮
- CBNumber:
- CB14668146
- 分子式:
- C16H19N3O2S
- 分子量:
- 317.41
- MOL File:
- 877963-94-5.mol
|
|
|
2-((4-(环丙烷羰基)哌嗪-1-基)甲基)苯并[D]异噻唑-3(2H)-酮化学性质
-
沸点:
-
528.5±60.0 °C(Predicted)
-
|
-
密度:
-
1.390±0.06 g/cm3(Predicted)
-
|
-
储存条件:
-
2-8°C
-
|
-
溶解度:
-
DMF: 10mg/mL; DMF:PBS (pH 7.2) (1:1): 0.5mg/mL; DMSO: 3mg/mL; Ethanol: 3mg/mL; Ethanol:PBS (pH 7.2) (1:6): 0.14mg/mL
-
|
-
形态:
-
A crystalline solid
-
|
-
酸度系数(pKa):
-
6.16±0.10(Predicted)
-
|
2-((4-(环丙烷羰基)哌嗪-1-基)甲基)苯并[D]异噻唑-3(2H)-酮性质、用途与生产工艺
LOC14 是一种有效的 protein disulfide isomerase (PDI) 的抑制剂，EC50值为500 nM和Kd值为62 nM。
LOC14 (0.01-100 μM; 24 hours) exhibits the capacity to inhibit recombinant (r)PDIA3 at an IC50 of approximately 5 μM.
Cell Viability Assay
|
Cell Line:
|
MTEC cells
|
|
Concentration:
|
0.01 μM; 0.1 μM; 0.5 μM; 1 μM; 5 μM; 10 μM; 100 μM
|
|
Incubation Time:
|
24 hours
|
|
Result:
|
Inhibited recombinant (r)PDIA3 activity.
|
LOC14 (orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks) significantly improves motor function, attenuated brain atrophy and extended survival in the N171–82Q HD mice.
|
Animal Model:
|
Male N171–82Q HD mice
|
|
Dosage:
|
20 mg/kg
|
|
Administration:
|
Orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks
|
|
Result:
|
Improved motor function in HD mice.
|
2-((4-(环丙烷羰基)哌嗪-1-基)甲基)苯并[D]异噻唑-3(2H)-酮
上下游产品信息
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-100432 | LOC14 | | 1 mg | 360元 |
| 2024/04/30 | HY-100432 | 2-((4-(环丙烷羰基)哌嗪-1-基)甲基)苯并[D]异噻唑-3(2H)-酮
LOC14 | 877963-94-5 | 5mg | 1000元 |
2-((4-(环丙烷羰基)哌嗪-1-基)甲基)苯并[D]异噻唑-3(2H)-酮
生产厂家
877963-94-5, 2-((4-(环丙烷羰基)哌嗪-1-基)甲基)苯并[D]异噻唑-3(2H)-酮 相关搜索:
- 药靶配体
- LOC14,蛋白质二硫键异构酶(PDI)调节剂
- 2-((4-(环丙烷羰基)哌嗪-1-基)甲基)苯并[D]异噻唑-3(2H)-酮
- 化合物LOC14
- 2-[[[4-(环丙基羰基)-1-哌嗪基]甲基] -1,2-苯并异噻唑-3(2H) - 酮
- 877963-94-5
- LOC 14,inhibit,LOC14,Inhibitor,LOC-14
- OC14
- LOC-14
- 2-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]methyl]-1,2-benzisothiazol-3(2H)-one
- LOC 14;LOC14
- LOC14, ≥98%
- 2-((4-(cyclopropanecarbonyl)piperazin-1-yl)methyl)benzo[d]isothiazol-3(2H)-one
- 1,2-Benzisothiazol-3(2H)-one, 2-[[4-(cyclopropylcarbonyl)-1-piperazinyl]methyl]-
- 2-[(4-cyclopropanecarbonylpiperazin-1-yl)methyl]-2,3-dihydro-1,2-benzothiazol-3-one