| N6022GSNOR inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.52%
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Chemical structure
| Kinase experiment [1]： | |
Alcohol dehydrogenase (ADH) Enzyme Assays | For ADH IB, ADH II, and ADH IV assays, enzyme activity was determined by measuring the increase in A340 due to reduction of NAD+ to NADH using conditions similar to those described by Sanghani et al. N6022 was dissolved and diluted in a PBS solution containing 1 N NaOH (1%). The IC50 values for N6022 versus ADH IB and ADH II were determined with ethanol as the substrate. The final assay conditions for ADH IB were 50 mM sodium phosphate (pH 7.4), 20 μg/mL ADH IB, 2 mM NAD+, and 2 mM ethanol, and the final assay conditions for ADH II were 90 mM sodium pyrophosphate (pH 8.9), 4.4 μg/mL ADH II, 23.6 mM NAD+, and 14.4 mM ethanol. The IC50 value of N6022 against ADH IV was determined using hexanol as a substrate. The hexanol was first dissolved in DMSO so that it could be dissolved in assay buffer. The final assay conditions were 50 mM sodium phosphate (pH 7.4), 1.25 μg/mL ADH IV, 2 mM NAD+, 400 μM hexanol, and 1% DMSO. |
| Animal experiment [2]: | |
Animal models | Female BALB/c mice model |
Dosage form | 0.1 mg/kg to 10 mg/kg, i.v. for 1-48 h |
Applications | N6022 dose-dependently decreased enhanced pause (Penh) and Bronchoalveolar lavage fluid (BALF) eosinophils, increased bronchoalveolar lavage fluid (BALF) nitrite and plasma cyclic guanosine monophosphate (cGMP) in ovalbumin (OVA)-sensitized mice. Moreover, N6022 attenuated the OVA-induced increase in nuclear factor kappa B (NFκB) activation and decreased methacholine (MCh)-induced contraction in isolated rat tracheal rings. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: 1. Green, L. S., Chun, L. E., Patton, A. K., Sun, X., Rosenthal, G. J. and Richards, J. P. (2012) Mechanism of inhibition for N6022, a first-in-class drug targeting S-nitrosoglutathione reductase. Biochemistry. 51, 2157-21682 2. Blonder, J. P., Mutka, S. C., Sun, X., Qiu, J., Green, L. H., Mehra, N. K., Boyanapalli, R., Suniga, M., Look, K., Delany, C., Richards, J. P., Looker, D., Scoggin, C. and Rosenthal, G. J. (2014) Pharmacologic inhibition of S-nitrosoglutathione reductase protects against experimental asthma in BALB/c mice through attenuation of both bronchoconstriction and inflammation. BMC Pulm Med. 14, 3 | |
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| Cas No. | 1208315-24-5 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 3-[1-(4-carbamoyl-2-methylphenyl)-5-(4-imidazol-1-ylphenyl)pyrrol-2-yl]propanoic acid | ||
| Canonical SMILES | CC1=C(C=CC(=C1)C(=O)N)N2C(=CC=C2C3=CC=C(C=C3)N4C=CN=C4)CCC(=O)O | ||
| Formula | C24H22N4O3 | M.Wt | 414.46 |
| Solubility | ≥20.7mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
N6022 is a specific and fully reversible inhibitor of S-nitrosoglutathione reductase (GSNOR) with IC50 value of 8nM [1].
N6022 is a first-in-class inhibitor of GSNOR. Inhibition of GSNOR causes the accumulation of GSNO which acts as a vasodilator and anti-inflammatory factor. N6022 presents an IC50 value of 8nM in the GSNO reduction assay and 32nM in the HMGSH oxidation assay. The Ki values are 2.5nM and 3.1nM, respectively. N6022 is selective against GSNOR over other human ADH enzymes. The IC50 values are 21μM, 67μM and 0.5μM for ADH IB, ADH II and ADH IV, respectively. N6022 also shows no effect on the NADPH-dependent enzyme, human carbonyl reductase, with IC50 value of 221μM. Currently, N6022 is under clinical studies for the treatment of inflammatory lung diseases [1].
References:[1] Green L S, Chun L E, Patton A K, et al. Mechanism of inhibition for N6022, a first-in-class drug targeting S-nitrosoglutathione reductase. Biochemistry, 2012, 51(10): 2157-2168.
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BAS-ELISA是在常规ELISA原理的基础上，结合生物素(B)与亲和素(A)间的高度放大作用，而建立的一种检测系统。生物素很易与蛋白质(如抗体等)以共价键结合。这样，结合了酶的亲和素分子与结合有特异性抗体的生物素分子产生反应，既起到了多级放大作用，又由于酶在遇到相应底物时的催化作用而呈色，达到检测未知抗原(或抗体)分子的目的。
辣根过氧化物酶（Horseradish Peroxidase,HRP）比活性高，稳定，分子量小，纯酶容易制备，所以最常用。HRP广泛分布于植物界，辣根中含量高，它是由无色的酶蛋白和棕色的铁卟啉结合而成的糖蛋白，糖含量18%。HRP由多个同功酶组成，分子量为40,000，等电点为PH3～9，酶催化的最适PH因供氢体不同而稍有差异，但多在PH5左右。酶溶于水和58%以下饱和度硫酸铵溶液。HRP的辅基和酶蛋白最大吸收光谱分别为403nm和275nm，一般以OD403nm /OD275nm的比值RZ（德文Reinheit Zahl）表示酶的纯度。高纯度的酶RZ值应在3.0左右（最高可达3.4）。RZ值越小，非酶蛋白就越多。 1） RZ>3 活性 >250u/mg， 主要应用于免疫学，是高纯度的过氧化酶。采用特殊色谱纯化技术以除去会影响免疫学反应的同工酶B .
2） RZ>2 活性 >180u/mg ，主要应用于临床化学，我们的客户也有将这个规格的产品应用于免疫学研究的。此时，一个标准化的分析方法就变得尤为重要。
3） RZ>1 活性 >100u/mg，主要应用于血糖试纸和尿液分析试纸。
4） RZ>0.6 活性 >60u/mg ，主要应用于尿液分析试纸。向左转|向右转
1.若都为正常，那么并未有太大问题，只要定期复查就可以了。
2.如果TGAb、TMAb、甲状腺功能均高，那么就是桥本氏甲状腺炎并甲亢，需要抗甲亢治疗。
3.如果TGAb、TMAb高，甲状腺功能下降，那么就是桥本氏甲状腺炎并甲减，需要进行甲减治疗。
4.如果TGAb、TMAb高，甲状腺功能正常，那么就是桥本氏甲状腺炎，无需特殊治疗，只要定期复查甲状腺功能就可能以了，不过这种情况有可能以后演变成甲减或者甲亢。
