cis-ACCP
目录号 : GC10149
A matrix metalloproteinase inhibitor
Cas No.:777075-44-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 4 and 20 μM for MMP-2 and MMP-9, respectively
cis-ACCP is a type IV collagen-specific MMP-2 and MMP-9 inhibitor.
Matrix metalloproteinases (MMPs) belong to a family of proteases that play a keyrole in tissue remodeling and repair via degrading extracellular matrix proteins, therefore enabling cell migration.
In vitro: cis-ACCP could preferentially inhibit MMP-2 and MMP-9 with a preference for MMP-2. The trans-ACCP did not inhibit the gelatinases but had moderate activity against MMP-3 and MMP-13. These findings indicated specificity of the compounds regarding binding to the enzymes. Furthermore, addition of cis-ACCP to tumor cells was able to prevent their traversion dose-dependently, about 90% at the highest concentration tested [1].
In vivo: Aninmal study showd that cis-ACCP could reduce metastasis formation in mice by approximately 90% when administered by a repetitive once daily dosing regimen at 50 mg/kg via oral or i.p. routes and was nontoxic up to 500 mg/kg, following i.p. administration daily for two weeks. In addition, the pharmacokinetic investigation in rats revealed distribution restricted into the extracellular fluid, the site of action for the antimetastatic activity and rapid elimination from blood [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Hoffman, A. ,Qadri, B.,Frant, J., et al. Carbamoylphosphonate matrix metalloproteinase inhibitors 6: Cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor-synthesis and pharmacodynamic and pharmacokinetic analysis. Journal of Medicinal Chemistry 51, 1406-1414 (2008).
| Cas No. | 777075-44-2 | SDF | |
| 化学名 | P-[[[(1R,2S)-2-aminocyclohexyl]amino]carbonyl]-phosphonic acid | ||
| Canonical SMILES | N[C@H]1CCCC[C@H]1NC(P(O)(O)=O)=O | ||
| 分子式 | C7H15N2O4P | 分子量 | 222.2 |
| 溶解度 | ≤0.15mg/ml in ethanol;0.3mg/ml in PBS, pH 7.2, | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.5005 mL | 22.5023 mL | 45.0045 mL |
| 5 mM | 0.9001 mL | 4.5005 mL | 9.0009 mL |
| 10 mM | 0.45 mL | 2.2502 mL | 4.5005 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。