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

DuP-697 是鄰位二芳基雜環(huán)的成員，并且是一種有效，不可逆，選擇性和口服活性的 COX-2 抑制劑 (對于人 COX-2 和 COX-1，IC50 分別為 10 nM 和 800 nM)。DuP-697 對 HT29 大腸癌細胞具有抗增殖作用 (IC50 為 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，抗癌和退燒的作用。

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DuP-697 Chemical Structure

DuP-697 Chemical Structure

CAS No. : 88149-94-4

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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥450
In-stock
5 mg ￥990
In-stock
10 mg   詢價  
50 mg   詢價  

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查看 COX 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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)

細胞效力
(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]
體外研究
(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.

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.
體內(nèi)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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMF 中的溶解度 : ≥ 54 mg/mL (131.29 mM)

DMSO 中的溶解度 : ≥ 15 mg/mL (36.47 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

Ethanol 中的溶解度 : ≥ 7 mg/mL (17.02 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.67%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
DuP-697
目錄號：
HY-103387
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