GW 627368 |
Catalog No.GC14812
One-Click Copy Product Info
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GW 627368(GW 627368X)은 인간 프로스타노이드 EP4 및 TP 수용체에 대해 각각 pKi 값이 7.0 및 6.8인 추가 인간 TP 수용체 친화성을 갖는 프로스타노이드 EP4 수용체의 새롭고 강력하며 선택적인 경쟁 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 439288-66-1
Sample solution is provided at 25 µL, 10mM.
GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor with additional human TP receptor affinity, with pKi values of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively[1].
GW627368 (GW627368X) appears to bind to human prostanoid TP receptors but not the TP receptors of other species[1].GW627368 (GW627368X) (10 μM) produces 100% inhibition of U-46619 (EC100)-induced aggregation (approximate pA2 approximately 7.0) in human washed platelets[1].GW627368 (GW627368X) is devoid of agonist activity and actually produced a significant and concentration-related reduction in basal cAMP levels with pIC50 value of 6.3[1].GW627368 (GW627368X) induces inhibition of proliferation and invasion of human SUM149 IBC tumor cells beginning at 0.1 μM, with inhibition of proliferation and invasion of MDA-MB-231 non-IBC cells at higher concentrations[2].
GW627368 (GW627368X) (0-15 mg/kg; p.o.; every alternate day for 28 days) shows significant tumor regression characterized by tumor reduction and induction of apoptosis[3].
References:
[1]. Wilson RJ, et al. GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist. Br J Pharmacol. 2006 Jun;148(3):326-39.
[2]. Robertson FM, et al. Molecular and pharmacological blockade of the EP4 receptor selectively inhibits both proliferation and invasion of human inflammatory breast cancer cells. J Exp Ther Oncol. 2008;7(4):299-312.
[3]. Parida S, et al. Molecular inhibition of prostaglandin E2 with GW627368X: Therapeutic potential and preclinical safety assessment in mouse sarcoma model. Cancer Biol Ther. 2015;16(6):922-32.
| Cas No. | 439288-66-1 | SDF | |
| Chemical Name | 2-(4-(4,9-diethoxy-1-oxo-1H-benzo[f]isoindol-2(3H)-yl)phenyl)-N-(phenylsulfonyl)acetamide | ||
| Canonical SMILES | O=C1N(C2=CC=C(CC(NS(=O)(C3=CC=CC=C3)=O)=O)C=C2)CC(C1=C4OCC)=C(C5=CC=CC=C45)OCC | ||
| Formula | C30H28N2O6S | M.Wt | 544.62 |
| Solubility | DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:2): 0.3 mg/ml,DMSO: 10 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. |
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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 | 1.8361 mL | 9.1807 mL | 18.3614 mL |
| 5 mM | 367.2 μL | 1.8361 mL | 3.6723 mL |
| 10 mM | 183.6 μL | 918.1 μL | 1.8361 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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 36 reference(s) in Google Scholar.)