Cathepsin G Inhibitor I
目录号 : GC10376Cathepsin G Inhibitor I 是一种有效的、选择性的、可逆的、竞争性的、非肽的组织蛋白酶 G 抑制剂。
Cas No.:429676-93-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 53 nM
Cathepsin G (EC 3.4.21.20, chymotrypsin-like proteinase, neutral proteinase) is an enzymatic protein belonging to the peptidase or protease families. In humans, it is coded by the CTSG gene. Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G.
In vitro: Cathepsin G Inhibitor I shows reversible, competitive inhibition with IC50 and Ki values of 53 ± 12 (N = 10) and 63 ± 14 nM (N = 5), respectively. Another attribute of Cathepsin G Inhibitor I relates to its selectivity vs other serine proteases. It weakly inhibits chymotrypsin (Ki = 1.5 ± 0.2 μM), and poorly inhibits (
In vivo: Cathepsin G Inhibitor I is currently in in-vitro investigation and no animal in vivo study is ongoing [1].
Clinical trial: Cathepsin G Inhibitor I is currently in the preclinical development and no clinical trial is ongoing.
Reference:
[1] Greco MN, Hawkins MJ, Powell ET, Almond HR Jr, Corcoran TW, de Garavilla L, Kauffman JA, Recacha R, Chattopadhyay D, Andrade-Gordon P, Maryanoff BE. Nonpeptide inhibitors of cathepsin G: optimization of a novel beta-ketophosphonic acid lead by structure-based drug design. J Am Chem Soc. 2002;124(15):3810-1.
| Cas No. | 429676-93-7 | SDF | |
| 化学名 | [2-[3-[(1-benzoylpiperidin-4-yl)-methylcarbamoyl]naphthalen-2-yl]-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid | ||
| Canonical SMILES | CN(C1CCN(CC1)C(=O)C2=CC=CC=C2)C(=O)C3=CC4=CC=CC=C4C=C3C(=O)C(C5=CC=CC6=CC=CC=C65)P(=O)(O)O | ||
| 分子式 | C36H33N2O6P | 分子量 | 620.64 |
| 溶解度 | DMF: 5 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6112 mL | 8.0562 mL | 16.1124 mL |
| 5 mM | 0.3222 mL | 1.6112 mL | 3.2225 mL |
| 10 mM | 0.1611 mL | 0.8056 mL | 1.6112 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。