Teijin compound 1 (Synonyms: Teijin compound 1 hydrochloride) |
| Catalog No.GC17834 |
Le composé Teijin 1 (chlorhydrate du composé Teijin 1) est un antagoniste puissant et spécifique de CCR2, avec des IC50 de 180 nM pour CCR2b.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1313730-14-1
Sample solution is provided at 25 µL, 10mM.
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Teijin compound 1 is a specific CCR 2 antagonist with IC50s of 24 and 180 nM in chemotaxis and binding assay, respectively.
Ile263 and Thr292 in CCR2 contribute significantly to binding of Teijin compound 1 in CCR2. Residue Glu291 in TM7, a highly conserved residue in many CC chemokine receptors, contributes substantially to binding of the protonated Teijin compound 1, and CCL2. His121 on TM3 and Ile263 on TM6 also strongly interact with Teijin compound 1[2].
In ApoE-deficient mice, Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and Teijin compound 1 reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta[3].
References:
[1]. Moree WJ, et al. Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1869-73.
[2]. Hall SE, et al. Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5. Mol Pharmacol. 2009 Jun;75(6):1325-36.
[3]. Calin M, et al. VCAM-1 directed target-sensitive liposomes carrying CCR2 antagonists bind to activated endothelium and reduce adhesion and transmigration of monocytes. Eur J Pharm Biopharm. 2015 Jan;89:18-29.
| Cas No. | 1313730-14-1 | SDF | |
| Synonymes | Teijin compound 1 hydrochloride | ||
| Chemical Name | (S)-N-(2-((1-(4-chlorobenzyl)pyrrolidin-3-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide hydrochloride | ||
| Canonical SMILES | ClC1=CC=C(C=C1)CN2C[C@H](CC2)NC(CNC(C3=CC=CC(C(F)(F)F)=C3)=O)=O.Cl | ||
| Formula | C21H21ClF3N3O2.HCl | M.Wt | 476.32 |
| Solubility | DMSO: 100 mM,Water: 10 mM | 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. |
||
| 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 | 2.0994 mL | 10.4971 mL | 20.9943 mL |
| 5 mM | 419.9 μL | 2.0994 mL | 4.1989 mL |
| 10 mM | 209.9 μL | 1.0497 mL | 2.0994 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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