Polmacoxib是一种双重抑制剂,抑制 COX-2 (IC50 ~ 0.1 μg/ml) 和碳酸酐酶,具有口服活性。该药物在小鼠模型中表现出抑制大肠腺瘤和肿瘤生长的能力,具有抗炎和抗肿瘤潜力,适用于癌症及炎症疾病的研究。
规格 | 价格 | 会员价 | 库存 | 数量 | |||
---|---|---|---|---|---|---|---|
{[ item.pr_size ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | COX ↓ ↑ | COX-1 ↓ ↑ | COX-2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Piroxicam | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Salicylic acid | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Phenacetin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Etodolac | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Flunixin meglumine | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ibuprofen L-lysine | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Nabumetone | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Acemetacin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Diflunisal | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Pranoprofen | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ampiroxicam | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Meloxicam | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Sulindac | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ketoprofen | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Mefenamic Acid | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Bromfenac sodium | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Oxaprozin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Aspirin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Nepafenac | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Zaltoprofen | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Salicin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Suprofen | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Xanthohumol | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Parecoxib | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Tolfenamic Acid |
+++
COX-2, IC50: 0.2 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Etoricoxib | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Niflumic Acid | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Valdecoxib |
++++
COX-2, IC50: 5 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ibuprofen |
+
COX-1, IC50: 13 μM |
+
COX-2, IC50: 370 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Indomethacin |
++
COX1, IC50: 0.28 μM |
+
COX-2, IC50: 14 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Lornoxicam |
++++
COX-1, IC50: 5 nM |
++++
COX-2, IC50: 8 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Meclofenamic acid sodium |
++++
COX-1, IC50: 40 nM |
+++
COX-2, IC50: 50 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Rofecoxib |
++++
COX-2, IC50: 18 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Asaraldehyde | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Naproxen |
+
COX-1, IC50: 8.7 μM |
+
COX-2, IC50: 5.2 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Diclofenac Sodium Salt |
+++
COX-1, IC50: 60 nM |
+++
COX-2, IC50: 200 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
NS-398 |
++
COX-2, IC50: 3.8 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Amfenac Sodium Hydrate |
++
COX-1, IC50: 250 nM |
+++
COX-2, IC50: 150 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Nimesulide |
+
COX-2, IC50: 26 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Lumiracoxib |
++
COX-1, Ki: 3 μM |
+++
COX-2, Ki: 60 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Rutaecarpine | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Celecoxib |
++++
COX-2, IC50: 40 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Carprofen |
++++
canine COX2, IC50: 30 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ketorolac |
++
COX-1 (human), IC50: 1.23 μM |
++
COX-2 (human), IC50: 3.50 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | Carbonic Anhydrase ↓ ↑ | Carbonic Anhydrase I ↓ ↑ | Carbonic Anhydrase II ↓ ↑ | Carbonic Anhydrase IV ↓ ↑ | Carbonic Anhydrase IX ↓ ↑ | Carbonic Anhydrase XII ↓ ↑ | 其他靶点 | 纯度 | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Topiramate | ✔ | Calcium Channel | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Dichlorphenamide | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Mafenide Acetate | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Benzenesulphonamide | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Dorzolamide HCl |
+
Carbonic anhydrase I, Ki: 6000 nM |
++++
Carbonic anhydrase II, Ki: 1.9 nM |
+++
Carbonic anhydrase IV, Ki: 31 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
Methazolamide |
++
hCAI, Ki: 50 nM |
+++
hCAII, Ki: 14 nM |
++
bCAIV, Ki: 36 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
Tioxolone |
+
CAI, Ki: 91 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
U-104 |
++
CAIX, Ki: 45.1 nM |
++++
CAXII, Ki: 4.5 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Polmacoxib (CG100649) is a pioneering orally active nonsteroidal anti-inflammatory drug (NSAID) with the unique capability of dual inhibition, targeting COX-2 with an IC50 approximately 0.1 μg/ml and carbonic anhydrase[1]. This first-in-class agent shows promise in inhibiting the growth of colorectal adenomas and tumors in mouse models[2]. |
体内研究 | Polmacoxib efficacy extends to tumor volume and weight reduction in subcutaneous xenograft mouse models using athymic nude mice, where Polmacoxib at doses between 7-15 mg/kg daily from day 27 post-injection to day 111, diminishes tumor volume and weight by 58% and 48%, respectively. This is in comparison to Celecoxib, which shows a 48% and 36% reduction under similar conditions[2]. Additionally, Polmacoxib's effects in orthotopic xenograft mouse models using athymic nu/nu mice, where treatment began on day 14 and continued for eight weeks, revealed a significant reduction in CRC growth. Tumor weight decreased by 70% with a 7 mg/kg dosage and by 83% with a 15 mg/kg dosage, compared to a 70% reduction achieved with a significantly higher dose of 500 mg/kg of Celecoxib[2]. |
体外研究 | In vitro, Polmacoxib effectively curtails COX-2 activity and PGE2 production in human colon cancer cells, HCA-7 and HT-29, at lower doses than Celecoxib when tested over 24 hours with concentrations up to 1 μg/ml. Moreover, when administered orally at a dose of 7 mg/kg daily for eight weeks, it significantly hinders intestinal polyp development in ApcMin/+ mice, demonstrating its preventive potential in colorectal cancer (CRC)[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.77mL 0.55mL 0.28mL |
13.84mL 2.77mL 1.38mL |
27.67mL 5.53mL 2.77mL |
CAS号 | 301692-76-2 |
分子式 | C18H16FNO4S |
分子量 | 361.387 |
别名 | CG100649 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 250 mg/mL(691.78 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |