2-Aminopurine (hydrochloride)
(Synonyms: 2-AP) 目录号 : GC42123A fluorescent analog of guanosine and adenosine
Cas No.:1428126-74-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
2-Aminopurine is a fluorescent analog of guanosine and adenosine that is used as a site-specific probe of nucleic acid structure and dynamics. It base pairs with cytosine in a wobble configuration or with thymine in a Watson-Crick geometry. [1] In addition to its usefulness in studies of base stacking interactions, 2-aminopurine has been used as a probe for DNA base flipping by methyl transferases. [2] 2-Aminopurine exhibits an excitation/emission of 320/381 nm, respectively, when adjusted to reduce interference with DNA base absorption as well as tryptophan fluorescence. 2-Aminopurine inhibits the double-stranded RNA-dependent protein kinase, protein kinase R, whose activity mediates antiviral defense and participates in toll-like receptor signaling.[3]
Reference:
[1]. Jean, J.M., and Hall, K.B. 2-Aminopurine fluorescence quenching and lifetimes: Role of base stacking. Proc.Nat.Acad.Sci.USA 98(1), 37-41 (2001).
[2]. Holz, B., Klimasauskas, S., Serva, S., et al. 2-Aminopurine as a fluorescent probe for DNA base flipping by methyltransferases. Nucleic Acids Res. 26(4), 1076-1083 (1998).
[3]. Endoh, Y., Chung, Y.M., Clark, I.A., et al. IL-10-dependent S100A8 gene induction in monocytes/macrophages by double-stranded RNA. J. Immunol. 182(4), 2258-2268 (2009).
Cas No. | 1428126-74-2 | SDF | |
别名 | 2-AP | ||
化学名 | 9H-purin-2-amine, dihydrochloride | ||
Canonical SMILES | NC1=NC2=NC=NC2=CN1.Cl.Cl | ||
分子式 | C5H5N5•2HCl | 分子量 | 208.1 |
溶解度 | PBS (pH 7.2): 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。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 4.8054 mL | 24.0269 mL | 48.0538 mL |
5 mM | 0.9611 mL | 4.8054 mL | 9.6108 mL |
10 mM | 0.4805 mL | 2.4027 mL | 4.8054 mL |
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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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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,
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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。
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The treatment of herpes simplex infections: an evidence-based review
Arch Intern Med 2008 Jun 9;168(11):1137-44.PMID:18541820DOI:10.1001/archinte.168.11.1137.
Genital and labial herpes simplex virus infections are frequently encountered by primary care physicians in the United States. Whereas the diagnosis of this condition is often straightforward, choosing an appropriate drug (eg, acyclovir, valacyclovir hydrochloride, or famciclovir) and dosing regimen can be confusing in view of (1) competing clinical approaches to therapy; (2) evolving dosing schedules based on new research; (3) approved regimens of the Food and Drug Administration that may not match recommendations of the Centers for Disease Control and Prevention or of other experts; and (4) dissimilar regimens for oral and genital infections. The physician must first choose an approach to treatment (ie, intermittent episodic therapy, intermittent suppressive therapy, or chronic suppressive therapy) based on defined clinical characteristics and patient preference. Then, an evidence-based dosing regimen must be selected. In this review, data from all sources are tabulated to provide a handy clinical reference.
Management of herpes simplex and varicella-zoster virus infections
West J Med 1997 Mar;166(3):211-5.PMID:9143202doi
Herpes simplex virus and varicella-zoster virus are common infections and are seen frequently in clinical practice. Infection with these viruses results in cutaneous lesions that may be diagnosed clinically, but widely available laboratory testing is useful for confirmation. Asymptomatic herpes simplex virus shedding, or "subclinical reactivation," likely occurs in all persons infected with herpes simplex virus and results in the transmission of virus despite the absence of signs or symptoms that suggest active infection. Oral and intravenous acyclovir are effective in treating initial and recurrent herpes simplex and varicella-zoster virus infections. The daily administration of oral acyclovir as suppressive therapy is effective in patients with frequently recurring genital infection with herpes simplex virus by reducing the number of symptomatic recurrences and the frequency of asymptomatic virus shedding. Two new antiviral agents, famciclovir and valacyclovir hydrochloride, have been approved for the short-term treatment of recurrent genital herpes simplex virus and recurrent zoster in nonimmunocompromised hosts. Famciclovir and valacyclovir demonstrate superior pharmacokinetics compared with acyclovir and allow for less frequent daily dosing with higher achievable serum drug concentrations. The attenuated live varicella virus vaccine is now available in the United States and prevents primary varicella-zoster virus infection in susceptible children and adults.
(+-)-carbocyclic 5'-nor-2'-deoxyguanosine and related purine derivatives: synthesis and antiviral properties
J Med Chem 1992 Jun 12;35(12):2191-5.PMID:1319491DOI:10.1021/jm00090a007.
Beginning with 3-cyclopenten-1-ylamine hydrochloride, the 5'-nor derivatives of carbocyclic 2'-deoxyguanosine (2), 2'-deoxyadenosine (3), and 2,6-diaminopurine 2'-deoxyribofuranoside (4) have been prepared. These compounds were evaluated for antiviral potential versus herpes simplex virus, varicella-zoster virus, cytomegalovirus, vaccinia virus, vesicular stomatitis virus, and human immunodeficiency virus and found to lack activity. Also, compounds 2-4 were virtually nontoxic toward the host (human diploid fibroblast ESM and HEL) cells. These biological properties may be due to the inability of 2-4 to be phosphorylated to the requisite nucleotide level that is likely to be necessary for biological activity by correlation to carbocyclic 2'-deoxyguanosine (1), which possesses significant antiviral properties as a result of conversion to its 5'-triphosphate derivative.
Phosphorylation and dephosphorylation events play critical roles in Sindbis virus maturation
Virology 1993 Oct;196(2):703-11.PMID:8396806DOI:10.1006/viro.1993.1527.
We have examined the effects of various inhibitors of protein kinases and phosphatases on Sindbis virus maturation in BHK cells. 2-Aminopurine, a nonspecific protein kinase inhibitor, N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide hydrochloride (W-7), a specific inhibitor of calmodulin/Ca(2+)-dependent protein kinase, and okadaic acid (OKA), a protein phosphatase inhibitor, dose-dependently inhibited Sindbis virus maturation. Although virus production was inhibited, the membrane glycoprotein precursors PE2/E1 were exported from the endoplasmic reticulum and PE2 was converted to E2 at normal kinetic rates. The glycoproteins were delivered to the plasma membrane in conformations which rendered them competent for low pH-mediated cell-cell fusion from within. Electron microscopy showed that in the presence of W-7, virus nucleocapsids were free in the cell cytoplasm, while in the presence of OKA, the nucleocapsids were associated with cell membranes. Metabolic labeling of Sindbis virus-infected cells with [32P]orthophosphate in the presence of OKA resulted in the specific labeling of the PE2/E2 glycoprotein. We have previously shown that the carboxyl terminus of the PE2 glycoprotein is initially buried in cell membranes and is then exposed to the cytoplasm at some later stage in virus maturation. The data shown are consistent with the hypothesis that phosphorylation and dephosphorylation play a critical role in a late stage in Sindbis virus maturation, possibly in releasing of the E2 tail from cell membranes.
Combination analyses of anti-cancer drugs on human neuroendocrine tumor cell lines
Cancer Chemother Pharmacol 2009 Dec;65(1):5-12.PMID:19381631DOI:10.1007/s00280-009-0997-6.
Purpose: There is a large need for better pharmacological treatment of neuroendocrine tumors. The aim of this study was to investigate and quantify the cytotoxic potentiating effects resulting from a combination of five substances, NSC 95397, emetine, CGP-74514A hydrochloride, Brefeldin A and sanguinarine chloride, chosen from a previous screening of 1,280 pharmacologically active agents on neuroendocrine tumor cells, with standard cytotoxic agents currently used in the treatment of neuroendocrine tumors. Method: The human pancreatic carcinoid cell line BON-1, human typical bronchial carcinoid cell line NCI-H727 and the human atypical bronchial carcinoid cell line NCI-H720 were used. Combinations between doxorubicin, etoposide, oxaliplatin, docetaxel, and each one of the five agents were studied and simultaneous exposures were explored using the median-effect method. Results: Most of the combinations of NSC-95397 and emetine with doxorubicin, etoposide, docetaxel, and oxaliplatin showed synergism, and their remaining combinations were additive. Almost all of the CGP-74514A hydrochloride interactions were additive, while brefeldin A and sanguinarine displayed less synergy but more additive and antagonistic interactions in combination with the standard drugs. Conclusion: The synergistic and additive interactions make NSC-95397, emetine, and CGP-74514A hydrochloride potential candidates for incorporation into combination chemotherapy regimens and these drugs might be the suitable candidates for further clinical studies in patients with bronchial carcinoids and pancreatic endocrine tumors.