| 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.
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
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
APC 366 Dilution Calculator
calculate
APC 366 Molarity Calculator
calculate
| 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.
