Polmacoxib

Name: Polmacoxib
Brand: TargetMol
SKU: T21294
Price: 283 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 97.88%

货号 T21294Cas号 301692-76-2

别名 帕马考昔, CG-100649, CG100649, CG 100649

Polmacoxib (CG 100649) 是一流的 NSAID 候选药物，是碳酸酐酶 (CA) 和 COX-2 的双重抑制剂。它在小鼠模型中抑制大肠腺瘤和肿瘤生长。

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Polmacoxib

一键复制产品信息

很棒

纯度: 97.88%

货号 T21294 别名 帕马考昔, CG-100649, CG100649, CG 100649Cas号 301692-76-2

Polmacoxib (CG 100649) 是一流的 NSAID 候选药物，是碳酸酐酶 (CA) 和 COX-2 的双重抑制剂。它在小鼠模型中抑制大肠腺瘤和肿瘤生长。

规格	价格	库存
1 mg	¥ 283	现货
5 mg	¥ 662	现货
10 mg	¥ 1,090	现货
25 mg	¥ 1,820	现货
50 mg	¥ 2,730	现货
100 mg	¥ 3,970	现货
200 mg	¥ 5,670	现货
1 mL x 10 mM (in DMSO)	¥ 728	现货

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产品介绍

Polmacoxib AI Summary

Polmacoxib exhibits potent in vitro inhibitory activity against prostaglandin G/H synthase 2 (COX-2) with an IC50 of 0.003 μg/mL and prostaglandin G/H synthase 1 (COX-1) with an IC50 of 0.3 μg/mL. It shows high selectivity for COX-2 over COX-1 with a selectivity ratio of 100.0. In vivo, Polmacoxib effectively inhibits carrageenan-induced rat foot edema by 47.0% when administered at 3 mg/kg orally and shows significant anti-inflammatory activity in adjuvant-induced arthritis in rats, with ED50 values ranging from 0.01 to 0.1 mg/kg/day. Additionally, the compound displays analgesic properties by reducing thermal stimuli-induced nociceptive responses by 92.0% at a dose of 1 mg/kg in carrageenan-stimulated Sprague-Dawley rats and diminishes the number of abdominal constrictions in ICR mice with an ED50 of 12.3 mg/kg. However, at a dose of 5 mg/kg, Polmacoxib exhibits gastric ulcerogenicity with an activity value of 1.5..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Polmacoxib (CG 100649) is a first-in-class NSAID drug candidate, is a dual inhibitor of carbonic anhydrase (CA) and COX-2. Polmacoxib inhibits premalignant and malignant colorectal lesions in mouse models, partly through inhibiting tumor cell proliferation.
靶点活性	COX-2:0.1 μg/mL (IC50)
别名	帕马考昔, CG-100649, CG100649, CG 100649

化学信息

分子量	361.39
分子式	C₁₈H₁₆FNO₄S
CAS No.	301692-76-2
Smiles	CC1(C)OC(=C(C1=O)c1cccc(F)c1)c1ccc(cc1)S(N)(=O)=O
密度	1.361 g/cm3 (Predicted)
颜色	White
物理性状	Solid

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

H2O: Insoluble

DMSO: 55 mg/mL (152.19 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7671 mL	13.8355 mL	27.6709 mL	138.3547 mL
5 mM	0.5534 mL	2.7671 mL	5.5342 mL	27.6709 mL
10 mM	0.2767 mL	1.3835 mL	2.7671 mL	13.8355 mL
20 mM	0.1384 mL	0.6918 mL	1.3835 mL	6.9177 mL
50 mM	0.0553 mL	0.2767 mL	0.5534 mL	2.7671 mL
100 mM	0.0277 mL	0.1384 mL	0.2767 mL	1.3835 mL