PMPA (NAALADase inhibitor)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PMPA是一种选择性的N-乙酰基化-α-连接的酸性二肽酶(NAALADase)抑制剂,Ki值为275 pM[1].
NAALADase(也称GCPII)是一种存在于膜中的锌金属酶,参与将神经肽N-乙酰天冬氨酰谷氨酸(NAAG)催化成萘乙酸(NAA)和谷氨酸的过程.研究表明,在神经/前列腺组织及癌症中,NAALADase具有最高表达,且NAALADase的抑制对前列腺癌的神经保护作用\检测\成像及治疗方面产生了各种效应[2] [3].
PMPA是一种强效的NAALADase抑制剂,具有比报道过的NAALADase抑制剂ZJ43更高的活性.在雄性C57/BL小鼠模型中,高剂量的PMPA抑制吗啡耐受的发展(类似于7.5 mg/kg的NMDA受体拮抗剂美金刚的效用),然而其对戒断的严重程度没有效用.浓度为100 mg/kg的PMPA也显著增强吗啡戒断,但是抑制吗啡诱发的条件性位置偏爱的获得与表达,这表明NAALADase参与阿片类药物成瘾现象[4].在训练期间,PMPA增加小鼠进入暗箱的潜伏期,且150 mg/kg剂量的PMPA损害自发交换,减少Y-迷宫任务中的运动,这表明,PMPA通过NAALADase的抑制作用影响小鼠学习记忆任务[5].
参考文献:
[1]. Tiffany, C.W., et al., Binding of the glutamate carboxypeptidase II (NAALADase) inhibitor 2-PMPA to rat brain membranes. Eur J Pharmacol, 2001. 427(2): p. 91-6.
[2]. Barinka, C., et al., Glutamate carboxypeptidase II in diagnosis and treatment of neurologic disorders and prostate cancer. Curr Med Chem, 2012. 19(6): p. 856-70.
[3]. Slusher, B.S., et al., Selective inhibition of NAALADase, which converts NAAG to glutamate, reduces ischemic brain injury. Nat Med, 1999. 5(12): p. 1396-402.
[4]. Popik, P., et al., Morphine tolerance and reward but not expression of morphine dependence are inhibited by the selective glutamate carboxypeptidase II (GCP II, NAALADase) inhibitor, 2-PMPA. Neuropsychopharmacology, 2003. 28(3): p. 457-67.
[5]. Lukawski, K., R.M. Kaminski, and S.J. Czuczwar, Effects of selective inhibition of N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) on mice in learning and memory tasks. Eur J Pharmacol, 2008. 579(1-3): p. 202-7.
Physical Appearance | White solid |
Storage | Desiccate at RT |
M.Wt | 226.12 |
Cas No. | 173039-10-6 |
Formula | C6H11O7P |
Solubility | Soluble to 100 mM in sterile water |
Chemical Name | 2-(phosphonomethyl)pentanedioic acid |
SDF | Download SDF |
Canonical SMILES | C(CC(=O)O)C(CP(=O)(O)O)C(=O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |