BAY-X 1005 (Synonyms: BAY X 1005; DG-031) |
| Catalog No.GC12232 |
BAY-X 1005(BAY X 1005; DG-031)는 경구 활성 및 선택적 5-리폭시게나제 활성화 단백질(FLAP) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 128253-31-6
Sample solution is provided at 25 µL, 10mM.
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BAY-X 1005 is a selective inhibitor of 5-lipoxygenase-activating protein [1].
5-lipoxygenase-activating protein (FLAP) is an integral protein and plays an important role in the activation of 5-lipoxygenase (5-LOX) and the synthesis of leukotrienes, which regulating immune responses.
BAY-X 1005 is a selective inhibitor of leukotriene synthesis. BAY X 1005 binds to FLAP and inhibits 5-LOX translocation from the cytosol to membranes [1]. BAY-X1005 inhibited LTB4 synthesis with IC50 values of 0.22, 0.026 and 0.039 μM for isolated PMNL of human, rat and mouse respectively and inhibited LTC4 synthesis with IC50 value of 0.021 μM in mouse macrophages [2].
In the arachidonate-induced mouse ear inflammation test, BAY-X 1005 inhibited myeloperoxidase activity and edema formation with ED50 values of 7.9 and 48.7, respectively [2].
Also, BAY-X 1005 (100 mg/kg) reduced platelet-activating factor-induced death of mice by 51% in a dose-dependent way. In animal models, BAY-X 1005 inhibited the synthesis of LTB4 and LTC4, which reduced edema formation, the vascular phenomena of inflammation and leukocyte immigration [3].
References:
[1]. Hatzelmann A, Fruchtmann R, Mohrs KH, et al. Mode of action of the leukotriene synthesis (FLAP) inhibitor BAY X 1005: implications for biological regulation of 5-lipoxygenase. Agents Actions, 1994, 43(1-2): 64-68.
[2]. Müller-Peddinghaus R, Fruchtmann R, Ahr HJ, et al. BAY X1005, a new selective inhibitor of leukotriene synthesis: pharmacology and pharmacokinetics. J Lipid Mediat, 1993, 6(1-3): 245-248.
[3]. Müller-Peddinghaus R, Kohlsdorfer C, Theisen-Popp P, et al. BAY X1005, a new inhibitor of leukotriene synthesis: in vivo inflammation pharmacology and pharmacokinetics. J Pharmacol Exp Ther, 1993, 267(1): 51-57.
| Cas No. | 128253-31-6 | SDF | |
| Synonyms | BAY X 1005; DG-031 | ||
| Chemical Name | (S)-2-cyclopentyl-2-(4-(quinolin-2-ylmethoxy)phenyl)acetic acid | ||
| Canonical SMILES | OC([C@H](C(C=C1)=CC=C1OCC2=NC3=CC=CC=C3C=C2)C4CCCC4)=O | ||
| Formula | C23H23NO3 | M.Wt | 361.43 |
| Solubility | <36.14mg/ml in DMSO | Storage | Store at RT |
| 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 | 2.7668 mL | 13.8339 mL | 27.6679 mL |
| 5 mM | 0.5534 mL | 2.7668 mL | 5.5336 mL |
| 10 mM | 0.2767 mL | 1.3834 mL | 2.7668 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 ddH2O, 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
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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