W 54011 |
| カタログ番号GC17129 |
W 54011 は、強力な経口活性非ペプチド C5a 受容体アンタゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 405098-33-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
W 54011 is a potent and orally active non-peptide C5a receptor antagonist with Ki value of 2.2 nM [1].
The complement C5a is a 74-amino acid peptide produced during complement activation processes. C5a plays an important role in mast cell degranulation, smooth muscle contraction, monocyte migration, blood vessel dilatation, increased vascular permeability at in?ammatory sites , and recruitment of immune cells [1][2].
W 54011 is a potent and orally active C5a receptor antagonist. W 54011 inhibited the binding of 125I-labeled C5a to human neutrophils with Ki value of 2.2 nM. In human neutrophils, W 54011 inhibited C5a-induced chemotaxis, intracellular Ca2+ mobilization, and generation of reactive super oxide species with IC50 values of 2.7, 3.1, and 1.6 nM, respectively. W 54011 was species specific and was able to inhibit C5a-induced intracellular Ca2+ mobilization in neutrophils of cynomolgus monkeys and gerbils but not mice, rats, guinea pigs, rabbits, and dogs [1]. In HMEC-1 endothelial cell line, W 54011 signi?cantly inhibited C5a-induced proliferation and cell cycle progression in a dose-dependent way. W 54011 also inhibited the proliferative effects of 10 nM C5a and dose-dependently inhibited the formation of ring-shaped structures induced by C5a [2].
In gerbils, oral administration of W-54011 (3-30 mg/kg) dose-dependently inhibited C5a-induced neutropenia [1].
References:
Sumichika H, Sakata K, Sato N, et al. Identification of a potent and orally active non-peptide C5a receptor antagonist. J Biol Chem. 2002 Dec 20;277(51):49403-7.
Kurihara R, Yamaoka K, Sawamukai N, et al. C5a promotes migration, proliferation, and vessel formation in endothelial cells. Inflamm Res. 2010 Aug;59(8):659-66.
| Cas No. | 405098-33-1 | SDF | |
| Chemical Name | N-(4-(dimethylamino)benzyl)-N-(4-isopropylphenyl)-7-methoxy-1,2,3,4-tetrahydronaphthalene-1-carboxamide hydrochloride | ||
| Canonical SMILES | CC(C1=CC=C(N(C(C2CCCC3=C2C=C(OC)C=C3)=O)CC4=CC=C(N(C)C)C=C4)C=C1)C.Cl | ||
| Formula | C30H37ClN2O2 | M.Wt | 493.08 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 3 mg/mL | 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 | 2.0281 mL | 10.1403 mL | 20.2807 mL |
| 5 mM | 0.4056 mL | 2.0281 mL | 4.0561 mL |
| 10 mM | 0.2028 mL | 1.014 mL | 2.0281 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 5 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *