NE 52-QQ57 |
Catalog No.GC31906
One-Click Copy Product Info
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NE 52-QQ57 es un antagonista de GPR4 selectivo y disponible por vÍa oral con una IC50 de 70 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1401728-56-0
Sample solution is provided at 25 µL, 10mM.
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM[1]. Anti-inflammatory activities[1].
NE 52-QQ57 (compound 13) shows a significant anti-inflammatory effect in the rat antigen induced arthritis model after oral administration at 30 mg/kg bid for 20 days[1].NE 52-QQ57 (30 mg/kg bid po for 4 days) also prevents angiogenesis in the mouse chamber model as well as pain as demonstrated in the rat complete Freund's adjuvant model[1].|| Animal Model:|Female FVB mice (8-10 weeks)[1]|Dosage:|30 mg/kg bid po|Administration:|Oral, 4 days, bid|Result:|Treatment with GPR4 antagonist 3 at 30 mg/ kg po bid starting on day 0, the day of the chamber implantation, showS a statistically significant reduction (46.8 ± 10.6%) of tissue growth by day 4. The blood levels of 13 on day 4 at 2 and 16 h after compound application in this model are 9.03 ± 2.87 and 0.09 ± 0.06 μM[1].|| Animal Model:|Male Wistar Han rats[1]|Dosage:|3, 10, and 30 mg/kg|Administration:|Oral, 20 days, bid|Result:|GPR4 antagonist 3 displays not only higher exposures in the rat AIA but also lower plasma protein binding in rat (95%)[1].
[1]. Velcicky J, et al. Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis. J Med Chem. 2017 May 11;60(9):3672-3683.
| Cas No. | 1401728-56-0 | SDF | |
| Canonical SMILES | CCC1=NN(C(C)=CC(C)=N2)C2=C1CC3=CC=C(C4=NN=C(C5CCNCC5)O4)C=C3 | ||
| Formula | C24H28N6O | M.Wt | 416.52 |
| Solubility | DMSO : 25 mg/mL (60.02 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. |
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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 | 2.4008 mL | 12.0042 mL | 24.0085 mL |
| 5 mM | 480.2 μL | 2.4008 mL | 4.8017 mL |
| 10 mM | 240.1 μL | 1.2004 mL | 2.4008 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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)