ND-336
目录号 : GC44341A selective inhibitor of MMP-2, -9, and -14
Cas No.:1807453-83-3
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
ND-336 is a selective inhibitor of the gelatinases matrix metalloproteinase-2 (MMP-2) and MMP-9, as well as MMP-14 (Kis = 85, 150, and 120 nM, respectively). It has minimal effect on other MMPs. ND-336 accelerates diabetic wound healing in mice by lowering inflammation and by enhancing angiogenesis and re-epithelialization of the wound.
| Cas No. | 1807453-83-3 | SDF | |
| Canonical SMILES | NCC(C=C1)=CC=C1OC2=CC=C(S(CC3SC3)(=O)=O)C=C2.Cl | ||
| 分子式 | C16H17NO3S2•HCl | 分子量 | 371.9 |
| 溶解度 | DMF: 5 mg/mL,DMSO: 30 mg/mL,DMSO:PBS (pH 7.2)(1:5): 0.16 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 | 2.6889 mL | 13.4445 mL | 26.8889 mL |
| 5 mM | 0.5378 mL | 2.6889 mL | 5.3778 mL |
| 10 mM | 0.2689 mL | 1.3444 mL | 2.6889 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。
Restructuring of the extracellular matrix in diabetic wounds and healing: A perspective
Pharmacol Res 2016 May;107:243-248.PMID:27033051DOI:10.1016/j.phrs.2016.03.008.
Diabetic foot ulcers are a complication of diabetes for which treatment options are limited and not effective, resulting in 73,000 lower-limb amputations in the United States every year. Wound healing is a complex process with a highly orchestrated cascade of events, in which the extracellular matrix (ECM) interacts with growth factors and cells. Matrix metalloproteinases (MMPs) are involved in all wound healing events, in particular MMP-8 and MMP-9, whose physiological functions are to degrade damaged collagen type I and to facilitate keratinocyte migration and re-epithelialization, respectively. MMP substrate redundancy permits another MMP to substitute for MMP-9 during normal wound healing. Under the hypoxic and inflammatory environment of diabetic wounds, increased reactive oxygen species (ROS) and upregulation of MMP-9 results in wounds that are recalcitrant to healing. We have determined that MMP-8 plays a role in the body's response to wound healing and that MMP-9 is the pathological consequence of the disease with detrimental effects. Thus, selective inhibition of MMP-9, while leaving MMP-8 activity unaffected, is desirable. ND-336 has such inhibitory profile and is a promising strategy for treatment of diabetic foot ulcers.
Acceleration of diabetic wound healing using a novel protease-anti-protease combination therapy
Proc Natl Acad Sci U S A 2015 Dec 8;112(49):15226-31.PMID:26598687DOI:10.1073/pnas.1517847112.
Nonhealing chronic wounds are major complications of diabetes resulting in >70,000 annual lower-limb amputations in the United States alone. The reasons the diabetic wound is recalcitrant to healing are not fully understood, and there are limited therapeutic agents that could accelerate or facilitate its repair. We previously identified two active forms of matrix metalloproteinases (MMPs), MMP-8 and MMP-9, in the wounds of db/db mice. We argued that the former might play a role in the body's response to wound healing and that the latter is the pathological consequence of the disease with detrimental effects. Here we demonstrate that the use of compound ND-336, a novel highly selective inhibitor of gelatinases (MMP-2 and MMP-9) and MMP-14, accelerates diabetic wound healing by lowering inflammation and by enhancing angiogenesis and re-epithelialization of the wound, thereby reversing the pathological condition. The detrimental role of MMP-9 in the pathology of diabetic wounds was confirmed further by the study of diabetic MMP-9-knockout mice, which exhibited wounds more prone to healing. Furthermore, topical administration of active recombinant MMP-8 also accelerated diabetic wound healing as a consequence of complete re-epithelialization, diminished inflammation, and enhanced angiogenesis. The combined topical application of ND-336 (a small molecule) and the active recombinant MMP-8 (an enzyme) enhanced healing even more, in a strategy that holds considerable promise in healing of diabetic wounds.
[Variation Characteristics and Sources of Polycyclic Aromatic Hydrocarbons in Karst Subterranean River During Rainfall Events]
Huan Jing Ke Xue 2015 Nov;36(11):4088-94.PMID:26910994doi
The water samples were continuously collected at the outlet of Nanshan Laolongdong subterranean river basin, which is located in Chongqing, during the rainfall event in June 2014. Sixteen priority polycyclic aromatic hydrocarbons (PAHs) in water were quantitatively analyzed by gas chromatography-mass spectrometry (GC-MS). The objectives of this study were to reveal the variation characteristics and sources of PAH16 in karst subterranean river during the rainfall event. The results showed that the subterranean river responded promptly to the rainfall, and there were four peaks of the total concentrations of PAH16, two peaks occurred during the flow rise stage, the others were in the maximum flow and flow decline stages. The total concentrations of PAH16 ranged 101-3 624 ng x L(-1), with a mean of 578 ng x L(-1), the total concentrations of 7 carcinogenic PAHs ranged ND-336 ng x L(-1), with a mean of 31.1 ng x L(-1). The PAH compositional profiles were dominated by 2,3-ring compounds, which accounted for 86.17% of the total concentrations of PAH16. The total concentrations of PAH16 were most influenced by the rainfall, through the cleaning of atmospheric pollutants by the rain and the scouring of the surface contaminants by the rainfall runoff. The PAHs in water mainly originated from the incomplete combustion of petroleum products and fossil fuels such as coal, as well as natural digenetic process. Compared to other areas in the world, the concentrations of PAH16 were generally at moderately polluted and heavily polluted levels.