BayCysLT2 (Synonyms: CAY10633) |
| Katalog-Nr.GC13020 |
CysLT2 receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 712313-33-2
Sample solution is provided at 25 µL, 10mM.
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BayCysLT2, an isophthalic acid derivative, is a selective and potent CysLT2 receptor antagonist [1].
Cysteinyl leukotrienes (CysLTs) belong to a family of G protein-coupled receptors (GPCRs). The cysteinyl leukotrienes (CysLTs) are inflammatory mediators associated with neuronal injury after brain ischemia through the activation of their receptors, CysLT1R and CysLT2R [2].
In vitro: BayCysLT2 inhibited radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 35 and >10,000 nM, respectively [1]. BayCysLT2 reversed LTC4-stimulated perfusion pressure increase and contractility decrease in isolated Langendorff-perfused guinea pig hearts in a concentration-dependent manner [1]. BayCysLT2 protected astrocytes from ischemic injury [3].
In vivo: BayCysLT2 attenuated myocardial infarction damage but also inhibited LTD4-induced Evans blue dye leakage in the mouse ear vasculature [4].
References:
[1] M. Harter, J. Erguden, F. Wunder, et al. Isophtalic acid derivatives. 10/537,623, 1-104 (2006).
[2] Takasaki J, Kamohara M, Matsumoto M, et al. The molecular characterization and tissue distribution of the human cysteinyl leukotriene CysLT 2 receptor[J]. Biochemical and biophysical research communications, 2000, 274(2): 316-322.
[3] X. J. Huang, W.P. Zhang, C.T. Li, W.Z. Shi, S.H. Fang, Y.B. Lu, Z. Chen, E.Q. Wei. Activation of CysLT receptors induces astrocyte proliferation and death after oxygen–glucose deprivation. Glia, 56 (2008), pp. 27–37
[4] N. C. Ni, D. Yan, L.L. Ballantyne, A. Barajas-Espinosa St, T. Amand, D.A. Pratt, C.D. Funk. A selective cysteinyl leukotriene receptor 2 antagonist blocks myocardial ischemia/reperfusion injury and vascular permeability in mice. J. Pharmacol. Exp. Ther., 339 (2011), pp. 768–778
| Cas No. | 712313-33-2 | SDF | |
| Überlieferungen | CAY10633 | ||
| Chemical Name | 3-[[(3-carboxycyclohexyl)amino]carbonyl]-4-[3-[4-(4-phenoxybutoxy)phenyl]propoxy]-benzoic acid | ||
| Canonical SMILES | O=C(NC1CCCC(C(O)=O)C1)C2=CC(C(O)=O)=CC=C2OCCCC(C=C3)=CC=C3OCCCCOC4=CC=CC=C4 | ||
| Formula | C34H39NO8 | M.Wt | 589.7 |
| Löslichkeit | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6958 mL | 8.4789 mL | 16.9578 mL |
| 5 mM | 0.3392 mL | 1.6958 mL | 3.3916 mL |
| 10 mM | 0.1696 mL | 0.8479 mL | 1.6958 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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