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- 2025年12月05日
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- 文献和实验
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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1700693-08-8
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1100.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥534.0 |
| 规格： | 5 mg | 产品价格： | ￥1000.0 |
| 规格： | 10 mg | 产品价格： | ￥1570.0 |
| 规格： | 25 mg | 产品价格： | ￥2830.0 |
| 规格： | 50 mg | 产品价格： | ￥4240.0 |
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JH-II-127
CAS No. : 1700693-08-8
MCE 国际站：JH-II-127
产品活性：JH-II-127一种口服有效的，具有高效力、选择性和脑渗透性的 LRRK2 抑制剂，其对野生型的 LRRK2 和LRRK2-G2019S 以及突变型的 LRRK2-A2016T 的 IC50 值分别为6、2 和 48 nM。JH-II-127 能够抑制小鼠包括大脑在内的所有组织中的 Ser935 磷酸化。JH-II-127 可用于帕金森综合征的研究。
研究领域：Autophagy
作用靶点：LRRK2
In Vitro: JH-II-127 (0.03, 0.1, 0.3, 1, 3 µM; 90 min) inhibits LRRK2 in HEK293 cells.
JH-II-127 (0.3, 1, 3 µM; 90 min) inhibits endogenously expressed LRRK2 in mouse Swiss 3T3 cells.
In Vivo: JH-II-127 (100 mg/kg; i.p.; single) results in near complete dephosphorylation of Ser935 of LRRK2 in all tissues including brain.
1.19
Pharmacokinetic Parameters of JH-II-127 in Wild type male C57BL/6 mice.| matrix | route | Tmax (h) | C0/Cmax (ng/mL) | AUCLast (h•ng/mL) | AUGINF (h•ng/mL) | T1/2 (h) | CL (mL/min/kg) | Vss (L/kg) |
| plasma | IV (2 mg/kg) | - | 1604.47 | 532.67 | 535.57 | 0.66 | 62.24 | 1.73 |
| plasma | PO (10 mg/kg) | 1 | 802.72 | 3094.58 | 3867.07 | - | - | - |
| brain | IV (2 mg/kg) | - | 1343.6 | 239.31 | 246.47 | 0.23 | 135.24 | 1.7 |
| brain | PO (10 mg/kg) | 1 | 247.35 | 688.21 | 762.38 | - | - | - |
相关产品：Bioactive Compound Library Plus | Kinase Inhibitor Library | CNS-Penetrant Compound Library | Autophagy Compound Library | Orally Active Compound Library | Anti-Parkinson's Disease Compound Library | Neurodegenerative Disease-related Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | Serine/Threonine Kinase Inhibitor Library | MLi-2 | IKK 16 | LRRK2-IN-1 | PF-06447475 | GNE0877 | GNE-7915 | GSK2578215A | HG-10-102-01 | XL01126 | PFE-360 | CZC-25146 | GNE-9605 | CZC-54252 | PF-06454589 | GSK2646264 | EB-42486 | LRRK2 inhibitor 1 | (R,R)-LRRK2-IN-7 | Indazole | JH-XII-03-02 | LRRK2-IN-10 | LRRK2-IN-2 | LRRK2-IN-3 | LRRK2-IN-4 | LRRK2-IN-5 | LRRK2-IN-6
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文献和实验were significantly decreased. High expressions of Bcl-2 and Bax were detected in 1 and 2μmol/L arseni c trioxide-treated cells, these were 46%, 87.33% and 83.08%, 95.83% respecti vely, among which that of Bax was more significant. Arsenic trioxide treatment at 0.5μ
Crystallization of Kinesin Family Motor Proteins
and phases of three heavy atom derivatives Eg5PDB: 1II6P21a=53.08 Åb=78.59 Åc=94.15 Åß=93.84°2.1 ÅMolecular replacement KIF1A-ADPPDB: 1I5SP212121a=41.67 Åb=51.92 Åc=157.06 Å2.2 ÅMolecular replacement KIF1A-AMPPCP(soaked)PDB: 1I6IP212121a=41.99 Åb=56.40 Åc=156
4CUygfRAQAXqGqESh8rfv9KslVRJo/B3/moaZLcgijKy6hdD6b+Xw/4oZ9VHsUgXlVQ1wo0yVUkDkZIlW7ZsWLliJfoPGAgj+uEydtwEZCdbjehFT08fQgPSuUtXPHxwn45rIrQl0etKr389wPZFc3FOfLuFBMDL5QFsr3ii+sSdGGgadU2/HlhhyZxzEFVlgb/gcv8crv6sjvE7B8IkStVPuLBmDtxzRj5jUYV+8xEYWDP3X8YxzoYvxkKAhY9YwGSmy9u
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