Navarixin [473727-83-2]
Référence HY-10198-5mg
Conditionnement : 5mg
Marque : MedChemExpress
Navarixine (SCH 527123) est un antagoniste des CXCR1 et CXCR2 qui est puissant, allostérique et oralement actif, avec Kd valeurs de 41 nM pour cynomolgus CXCR1 et 0,20 nM, 0,20 nM, 0,08 nM pour souris, rat et cynomolgus monkey CXCR2, respectivement.
Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
Navarixin Chemical Structure
CAS No. : 473727-83-2
This product is a controlled substance and not for sale in your territory.
Based on 19 publication(s) in Google Scholar
Description |
Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly[1][2]. |
||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target[1][2][3] |
|
||||||||||||
In Vitro |
Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly[1]. Navarixin (1 nM) reduces CXCL8 potency in stimulating Ba/F3-hCXCR2 chemotaxis. Navarixin (3 nM) significantly inhibits the potency and efficacy of CXCL1-induced neutrophils (PMN) chemotaxis. Navarixin (300 nM) significantly decreases chemokine potency and slightly decreases maximal cell movement for Ba/F3-CXCR1 cells[2]. Navarixin (25 μM) is sufficient to block IL-8-mediated CXCR2 activation in HCT116, E2, Caco2, and IIIe cells, in which phosphorylation of downstream kinases of CXCR2 is reduced in a concentration-dependent manner[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
In Vivo |
Navarixin (0.1-10 mg/kg, p.o.) blocks pulmonary neutrophilia (ED50=1.2 mg/kg) and goblet cell hyperplasia (32-38% inhibition at 1-3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. In rats, Navarixin (0.1-3 mg/kg p.o.) suppresses the pulmonary neutrophilia (ED MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
Essai clinique |
|
||||||||||||
Masse moléculaire |
397.42 |
||||||||||||
Formule |
C21H23N3O5 |
||||||||||||
CAS No. |
473727-83-2 |
||||||||||||
Appearance |
Solid |
||||||||||||
Color |
Light yellow to yellow |
||||||||||||
SMILES |
O=C1C(C(NC2=CC=CC(C(N(C)C)=O)=C2O)=C1N[C@H](CC)C3=CC=C(O3)C)=O |
||||||||||||
Livraison | Room temperature in continental US; may vary elsewhere. |
||||||||||||
Stockage |
|
||||||||||||
Solvant et solubilité |
In Vitro:
DMSO : ≥ 50 mg/mL (125.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) *"≥" means soluble, but saturation unknown. Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
|
||||||||||||
Pureté et documentation |
Purity: 98.00% |
||||||||||||
Références |
|
Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
---|
DMSO | 1 mM | 2.5162 mL | 12.5811 mL | 25.1623 mL | 62.9057 mL |
5 mM | 0.5032 mL | 2.5162 mL | 5.0325 mL | 12.5811 mL | |
10 mM | 0.2516 mL | 1.2581 mL | 2.5162 mL | 6.2906 mL | |
15 mM | 0.1677 mL | 0.8387 mL | 1.6775 mL | 4.1937 mL | |
20 mM | 0.1258 mL | 0.6291 mL | 1.2581 mL | 3.1453 mL | |
25 mM | 0.1006 mL | 0.5032 mL | 1.0065 mL | 2.5162 mL | |
30 mM | 0.0839 mL | 0.4194 mL | 0.8387 mL | 2.0969 mL | |
40 mM | 0.0629 mL | 0.3145 mL | 0.6291 mL | 1.5726 mL | |
50 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL | 1.2581 mL | |
60 mM | 0.0419 mL | 0.2097 mL | 0.4194 mL | 1.0484 mL | |
80 mM | 0.0315 mL | 0.1573 mL | 0.3145 mL | 0.7863 mL | |
100 mM | 0.0252 mL | 0.1258 mL | 0.2516 mL | 0.6291 mL |