2. Immunology/Inflammation Apoptosis
  3. COX Apoptosis
  4. DuP-697

DuP-697 是邻位二芳基杂环的成员，并且是一种有效，不可逆，选择性和口服活性的 COX-2 抑制剂 (对于人 COX-2 和 COX-1，IC50 分别为 10 nM 和 800 nM)。DuP-697 对 HT29 大肠癌细胞具有抗增殖作用 (IC50 为 42.8 nM)，抗血管生成和促凋亡作用。DuP-697 可抑制前列腺素的合成，并具有抗炎，抗癌和退烧的作用。

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DuP-697 Chemical Structure

DuP-697 Chemical Structure

CAS No. : 88149-94-4

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规格 价格 是否有货 数量
1 mg ￥450
In-stock
5 mg ￥990
In-stock
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Customer Review

DuP-697 相关抗体

Top Publications Citing Use of Products

查看 COX 亚型特异性产品:

查看所有亚型
COX COX-1 COX-2 COX-3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects[1][2][3].

IC50 & Target[3]

hCOX-2

10 nM (IC50)

hCOX-1

800 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
0.002 μM
Compound: DuP-697
In vitro inhibition of PGE-2 produced by arachidonic acid-stimulated CHO cells stably expressing human Prostaglandin G/H synthase 2
In vitro inhibition of PGE-2 produced by arachidonic acid-stimulated CHO cells stably expressing human Prostaglandin G/H synthase 2
[PMID: 9873621]
CHO IC50
0.0021 μM
Compound: DuP-697
Inhibition of PGE-2 production by arachidonic acid-stimulated CHO cells expressing human Prostaglandin G/H synthase 2
Inhibition of PGE-2 production by arachidonic acid-stimulated CHO cells expressing human Prostaglandin G/H synthase 2
10.1016/S0960-894X(96)00501-X
U-937 IC50
0.007 μM
Compound: DuP-697
Inhibition of Prostaglandin G/H synthase 1 was measured by the inhibition of PGE-2 produced by microsomes from U937 cells at subsaturating arachidonic acid conc.
Inhibition of Prostaglandin G/H synthase 1 was measured by the inhibition of PGE-2 produced by microsomes from U937 cells at subsaturating arachidonic acid conc.
[PMID: 9873621]
体外研究
(In Vitro)

DuP-697 (0-100 nM; 24 hours; HT29 cells) treatment shows antiproliferative with an IC50 value of 42.8 nM[1].
DuP-697 (25-100 nM; 72 hours; HT29 cells) treatment causes concentration dependent apoptosis in HT29 cells. The percentage of UR (apoptosis portion) area increases gradually according to the concentration of DuP-697 from 7% in control group to 52% in 100 nM DuP-697[1].
DuP-697 in 100, 10 and 1 nM concentrations cause antiangiogenic effect. Antiangiogenic scores of DuP-697 are 1.2, 0.8 and 0.5, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DuP-697 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HT29 cells
Concentration: 0 nM, 12.5 nM, 25 nM, 50 nM, 100 nM
Incubation Time: 24 hours
Result: Exhibited decreasing CI values in a concentration dependent manner. Showed statistically significant cytotoxic effect.

Apoptosis Analysis[1]

Cell Line: HT29 cells
Concentration: 25 nM, 50 nM, 100 nM
Incubation Time: 72 hours
Result: Caused concentration dependent apoptosis in HT29 cells.
体内研究
(In Vivo)

DuP-697 is a potent inhibitor of paw swelling in nonestablished and established adjuvant arthritis in rats (ED50 = 0.03 and 0.18 mg/kg/day, respectively). DuP-697 has no effect on phenylquinone writhing in rats (ED50 greater than 100 mg/kg), but is analgetic against inflammation-related pain in the Randall-Selitto assay (ED50 = 3.5 mg/kg) and is a very potent antipyretic agent (ED50 = 0.05 mg/kg). DuP-697 (5 mg/kg i.v.) does not alter renal blood flow or the renal vascular response to angiotensin II in furosemide-pretreated, volume-depleted rats[2].
DuP-697 is a moderate inhibitor of bull seminal vesicle prostaglandin (PG) synthesis (IC50 of 24 μM) and a potent inhibitor of rat brain PG synthesis (IC50 of 4.5 μM) but was ineffective against rat kidney PG synthesis (IC50 of 75 μM)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

411.31

Formula

C17H12BrFO2S2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMF 中的溶解度 : ≥ 54 mg/mL (131.29 mM)

DMSO 中的溶解度 : ≥ 15 mg/mL (36.47 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

Ethanol 中的溶解度 : ≥ 7 mg/mL (17.02 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4313 mL 12.1563 mL 24.3126 mL
5 mM 0.4863 mL 2.4313 mL 4.8625 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.67%

COA (294 KB) HNMR (98 KB) LCMS (206 KB)

产品使用指南 (1538 KB)
参考文献

DuP-697 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO / DMF 1 mM 2.4313 mL 12.1563 mL 24.3126 mL 60.7814 mL
5 mM 0.4863 mL 2.4313 mL 4.8625 mL 12.1563 mL
10 mM 0.2431 mL 1.2156 mL 2.4313 mL 6.0781 mL
15 mM 0.1621 mL 0.8104 mL 1.6208 mL 4.0521 mL
DMSO / DMF 20 mM 0.1216 mL 0.6078 mL 1.2156 mL 3.0391 mL
25 mM 0.0973 mL 0.4863 mL 0.9725 mL 2.4313 mL
30 mM 0.0810 mL 0.4052 mL 0.8104 mL 2.0260 mL
DMF 40 mM 0.0608 mL 0.3039 mL 0.6078 mL 1.5195 mL
50 mM 0.0486 mL 0.2431 mL 0.4863 mL 1.2156 mL
60 mM 0.0405 mL 0.2026 mL 0.4052 mL 1.0130 mL
80 mM 0.0304 mL 0.1520 mL 0.3039 mL 0.7598 mL
100 mM 0.0243 mL 0.1216 mL 0.2431 mL 0.6078 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DuP-69788149-94-4DuP697DuP 697COXApoptosisCyclooxygenaseCOX- 2annexin-Vapoptosisantiproliferativeantiangiogeniccolorectalcanceranti-inflammatoryprostaglandinantipyreticInhibitorinhibitorinhibit

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目录号：
HY-103387
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