301692-76-2
301692-76-2
Chemical Structure
Polmacoxib
Synonym(s): CG100649
- CAS No.: 301692-76-2
- Formula:C18H16FNO4S
- Molecular Weight:361.39
IUPAC Name: 4-(3-(3-fluorophenyl)-5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)benzenesulfonamide
InChIKey: IJWPAFMIFNSIGD-UHFFFAOYSA-N
SMILES: O=S(C1=CC=C(C(OC2(C)C)=C(C3=CC=CC(F)=C3)C2=O)C=C1)(N)=O
Biological Activity: Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase[1]. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models[2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Polmacoxib | 99.48% | Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models. | ||||||||||||||||||||
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Polmacoxib (Standard) | ≥98% | Polmacoxib (Standard) is the analytical standard of Polmacoxib. This product is intended for research and analytical applications. Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models. | ||||||||||||||||||||
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DRF-4848 | DRF-4848 is a COX-2 inhibitor. DRF-4848 can be used for the research of inflammation. | |||||||||||||||||||||
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L 651142 | L 651142 is a weak platelet activating factor (PAF) receptor antagonist. L 651142 inhibits the binding of [3H]PAF to rabbit platelet, human platelet or human lung membranes with Kis of 0.839 μM, 1.82 μM, 3.64 μM, respectively. | |||||||||||||||||||||
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VU0487836 | 99.86% | VU0487836 is a selective cyclooxygenase-1 (COX-1) inhibitor with an IC50 of 0.36 μM against ovine-derived COX-1. VU0487836 serves as a prototype for the development of radiological imaging agents targeting COX-1 for ovarian cancer. VU0487836 is applicable to relevant research on ovarian cancer. | ||||||||||||||||||||
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Exisulind | 98.04% | Exisulind is an inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac. Exisulind inhibits aldose reductase with an IC50 of 367 nM in vitro and may contribute to the beneficial pharmacological effects of sulindac on type 2 diabetic complications. | ||||||||||||||||||||
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Firocoxib | 99.54% | Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects. | ||||||||||||||||||||
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Rofecoxib | 99.89% | Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells). | ||||||||||||||||||||
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Sulindac sulfone | 98.10% | Sulindac sulfone is an orally active metabolite of Sulindac (HY-B0008). Sulindac sulfone activates PPARγ and drives transcriptional induction of SSAT by binding to the PPRE-2 element. Sulindac sulfone induces Apoptosis. Sulindac sulfone negatively regulates the function of VDAC1/2 to inhibit the mTORC1 pathway, reduces Cyclin D1 levels, and induces G1 cell cycle arrest in colon cancer cells. Sulindac sulfone exerts colon cancer preventive effects through a COX-independent mechanism. Sulindac sulfone can be used in research related to colon cancer. | ||||||||||||||||||||
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Fendleryl B | Fendleryl B is a compound isolated from the extract of the edible mushroom Gambas edible mushroom. Fendleryl B can be used in the study of neurological diseases. | |||||||||||||||||||||
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SC57666 | 98.94% | SC57666 is a selective COX2 inhibitor with an IC50 of 26 nM. | ||||||||||||||||||||
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SC58451 | SC58451 is a potent and selective Cox-2 inhibitor. | |||||||||||||||||||||
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References
- [1]. Kim SH, et al. CG100649, a novel COX-2 inhibitor, inhibits colorectal adenoma and carcinoma growth in mouse models. Invest New Drugs. 2014;32(6):1105-1112. [Content Brief]
- [2]. Flick AC, et al. Synthetic Approaches to the New Drugs Approved During 2015 [published correction appears in J Med Chem. 2017 Oct 26;60(20):8680]. J Med Chem. 2017;60(15):6480-6515. [Content Brief]
