APC 366 |
カタログ番号GC16688
One-Click Copy Product Info
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APC 366 はマスト細胞トリプターゼの選択的阻害剤です (Ki = 7.1 μM)。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 158921-85-8
Sample solution is provided at 25 µL, 10mM.
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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) [2].
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.
| Cas No. | 158921-85-8 | 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 |
| 溶解度 | Soluble to 5 mg/ml in 20% ethanol / Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2701 mL | 11.3507 mL | 22.7015 mL |
| 5 mM | 454 μL | 2.2701 mL | 4.5403 mL |
| 10 mM | 227 μL | 1.1351 mL | 2.2701 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)