| APC 366mast cell tryptase inhibitor,selective and competitive |
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.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 158921-85-8 | SDF | Download SDF |
| Chemical Name | (S)-1-((S)-5-guanidino-2-(1-hydroxy-2-naphthamido)pentanoyl)pyrrolidine-2-carboxamide | ||
| Canonical SMILES | O=C(C1=C(O)C2=CC=CC=C2C=C1)N[C@@H](CCCNC(N)=N)C(N3[C@H](C(N)=O)CCC3)=O | ||
| Formula | C22H28N6O4 | M.Wt | 440.5 |
| Solubility | Soluble to 5 mg/ml in 20% ethanol / H2O | Storage | Store at -20°C |
| Physical Appearance | White lyophilised 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. | ||
APC 366 is a selective and competitive inhibitor of tryptase [1, 2, 3]. After about 4 h of incubation with human tryptase, APC 366 showed an inhibitory potential with a Ki value of 530 nM and an IC50 value of 1400 ± 240 nM [3].
Tryptase is a mast cell serine protease. It had been implicated in the allergic asthma pathophysiology [2].
It seemed that actions of tryptase were dependent on an intact catalytic site. APC 366 inhibited DNA synthesis and the proliferation of the smooth muscle cell (SMC) induced by tryptase. In this study, thymidine incorporation was reduced by APC 366 by 79%. Heating to inactivate enzymatic activity also abolished the ability of tryptase to stimulate SMC proliferation and DNA synthesis [4].
In urine in the control pigs, the concentration of histamine was immediately elevated after allergen challenge. But treatment with APC 366 markedly decreased this release [5]. In vivo in a sheep model, administration with APC 366 decreased allergen-induced early and late-phase bronchoconstriction and hyperresponsiveness [4]. In allergic sheep, APC 366 was administered by aerosol in all experiments. In vehicle control trials, antigen challenge caused peak early and late increases in specific lung resistance with values of 259 ± 30% and 183 ± 27% over baseline, respectively. 0.5 h before, 4 h after and 24 h after antigen challenge, treatment with APC 366 at 9 mg/3 ml H2O slightly decreased the peak early response (194 ± 41%) and significantly inhibited the late response (38 ± 6%, p < 0.05)="">
References: [1]. Krishna MT, Chauhan A, Little L, et al. Inhibition of mast cell tryptase by inhaled APC 366 attenuates allergen-induced late-phase airway obstruction in asthma. Journal of Allergy and Clinical Immunology, 2001, 107(6): 1039-1045.[2]. Clark JM, Abraham WM, Fishman CE, et al. Tryptase inhibitors block allergen-induced airway and inflammatory responses in allergic sheep. American journal of respiratory and critical care medicine, 1995, 152(6): 2076-2083.[3]. Hallgren J, Estrada S, Karlson U, et al. Heparin antagonists are potent inhibitors of mast cell tryptase. Biochemistry, 2001, 40(24): 7342-7349.[4]. Berger P, Perng DW, Thabrew H, et al. Tryptase and agonists of PAR-2 induce the proliferation of human airway smooth muscle cells. Journal of Applied Physiology, 2001, 91(3): 1372-1379.[5]. Sylvin H, Dahlbck M, Van Der Ploeg I, et al. The tryptase inhibitor APC-366 reduces the acute airway response to allergen in pigs sensitized to Ascaris suum. Clinical & Experimental Allergy, 2002, 32(6): 967-971.
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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。
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。
英文名称：horseradish peroxidase;HRP
定义：一种糖蛋白，由于在辣根中该酶的含量很高，故名。它以铁卟啉为辅基，在过氧化氢存在时能催化苯酚、苯胺及其取代物聚合。
