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COX-2-IN-6 是一种具有有效性、选择性且可口服的环氧化酶-2 (COX-2) 抑制剂,对 COX-2 具有抑制作用,IC50 为 0.84 μM,Ki 为 69 nM。COX-2-IN-6 对 COX-2 驱动的 PGE2 合成具有抑制作用,IC50 为 0.60 μM。COX-2-IN-6 可用于预防结直肠癌。
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COX-2-IN-6 是一种具有有效性、选择性且可口服的环氧化酶-2 (COX-2) 抑制剂,对 COX-2 具有抑制作用,IC50 为 0.84 μM,Ki 为 69 nM。COX-2-IN-6 对 COX-2 驱动的 PGE2 合成具有抑制作用,IC50 为 0.60 μM。COX-2-IN-6 可用于预防结直肠癌。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 752 | 现货 | |
5 mg | ¥ 1,650 | 现货 | |
10 mg | ¥ 2,480 | 现货 | |
25 mg | ¥ 4,480 | 现货 | |
50 mg | ¥ 6,470 | 现货 | |
100 mg | ¥ 8,720 | 现货 | |
500 mg | ¥ 17,300 | 现货 |
产品描述 | COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is used to prevent colorectal cancer. COX-2-IN-6 can be used to prevent colorectal cancer. |
靶点活性 | COX-2:0.84 μM |
体外活性 | COX-2-IN-6 (Compound 10) inhibits human COX-2/COX-1 enzyme and COX-2/COX-1-driven PGE2 synthesis in HEK293 cells, with IC50 of 0.84 μM、>50 μM、0.60 μM and, >50 μM, respectively.[1] COX-2-IN-6 exhibits stability in human or mouse liver microsomes and hepatocytes in vitro. The T1/2 value of human hepatocytes is 3.1 min, and the T1/2 value of mouse hepatocytes is 3.0 min.[1] |
体内活性 | COX-2-IN-6 (Compound 10) (30, 100, 300 mg/kg; oral; single dose; APCmin/mouse model) inhibits adenoma progression and extends survival in the APCmin/+ mouse model.[1] COX-2-IN-6 (10 mg/kg; oral; single dose; APCmin/+ mouse model) exhibits high colonic exposure (>4300 ng/g) and low systemic exposure (<6 ng/mL), C/P distribution ratio > 1200 in 4 hours.[1] |
分子量 | 409.5 |
分子式 | C20H27NO6S |
CAS No. | 2756347-91-6 |
Smiles | O(CC(C)(C)O)C1=C(C=C(CO)C(OCCC)=N1)C2=CC=C(S(C)(=O)=O)C=C2 |
密度 | 1.234 g/cm3 (Predicted) |
存储 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 60 mg/mL (146.52 mM), Sonication is recommended. ![]() | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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