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  1. Immunology/Inflammation Apoptosis
  2. COX Apoptosis
  3. Ketorolac

Ketorolac  (Synonyms: 酮咯酸; RS37619)

目錄號(hào): HY-B0580 純度: 99.93%
COA 產(chǎn)品使用指南 技術(shù)支持

Ketorolac (RS37619) 是一種非甾體抗炎劑,為非選擇性的 COX 抑制劑,對(duì) COX-1COX-2IC50 值分別為 20 nM 和 120 nM。Ketorolac被用作 0.5% 滴眼液,用于過(guò)敏性結(jié)膜炎、黃斑囊狀水腫、術(shù)中瞳孔縮小、術(shù)后眼炎疼痛的研究。Ketorolac 也是一種 DDX3 抑制劑,可用于癌癥的研究。

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Ketorolac Chemical Structure

Ketorolac Chemical Structure

CAS No. : 74103-06-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥385
In-stock
50 mg ¥350
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100 mg ¥490
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Other Forms of Ketorolac:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

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(xiàn)

生物活性

Ketorolac (RS37619) is a non-steroidal anti-inflammatory drug (NSAID), acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. Ketorolac tromethamine is used as 0.5% ophthalmic solution for the research of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Ketorolac tromethamine is also a DDX3 inhibitor that can be used for cancer research[1][4].

IC50 & Target[1]

COX-1

20 nM (IC50)

COX-2

120 nM (IC50)

DDX3

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
13 μM
Compound: Toradol
Inhibition of PAK1/COX2 in human A549 cells harboring Ki-RAS mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
Inhibition of PAK1/COX2 in human A549 cells harboring Ki-RAS mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 27889630]
A549 IC50
36 μM
Compound: Toradol
Inhibition of PAK1 in human A549 cells using myelin basic protein as substrate preincubated for 24 hrs followed by PAK1 immunoprecipation and substrate addition measured after 60 mins by ATP-Glo kinase assay
Inhibition of PAK1 in human A549 cells using myelin basic protein as substrate preincubated for 24 hrs followed by PAK1 immunoprecipation and substrate addition measured after 60 mins by ATP-Glo kinase assay
[PMID: 27889630]
B16-F10 IC50
30 μM
Compound: Toradol
Cytotoxicity against PAK1-independent mouse B16F10 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against PAK1-independent mouse B16F10 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 27889630]
體外研究
(In Vitro)

Ketorolac (RS37619) salt (0-30 μM; 48 h) effectively kills the oral cancer cells[4].
Ketorolac salt (0-5 μM; 48 h) inhibits the expression of DDX3 protein, and induces apoptosis in H357 cells[4].
Ketorolac salt (0-2.5 μM; 0-16 h) inhibits the proliferation of oral cancer cells[4].
Ketorolac salt (0-50 μM) directly interacts with DDX3 and inhibits the ATPase activity[4].

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

Cell Viability Assay[4]

Cell Line: HOK, SCC4, SCC9 and H357 cells
Concentration: 0-30 μM
Incubation Time: 48 h
Result: Showed inhibition with IC50s of 2.6, 7.1 and 8.1 μM against H357, SCC4 and SCC9 cells, respectively. And the normal HOK cell line did not show any cell death effect.

Cell Proliferation Assay[4]

Cell Line: H357
Concentration: 0.5, 1.0, 1.5, 2.0 and 2.5 μM
Incubation Time: 0, 8 and 16 h
Result: Inhibited the proliferation.

Western Blot Analysis[4]

Cell Line: H357
Concentration: 1, 2.5 and 5 μM
Incubation Time: 48 h
Result: Significantly reduced DDX3 protein expression levels, but not completely ablated as compared to DMSO treated cells. Up regulated the expression of E-cadherin.

Apoptosis Analysis[4]

Cell Line: H357
Concentration: 2.5 and 5 μM
Incubation Time: 48 h
Result: Induced apoptosis.
體內(nèi)研究
(In Vivo)

Ketorolac (RS37619) (0.4% ketorolac tromethamine ophthalmic solution) shows powerful ocular anti-inflammatory activities in rabbits[1].
Ketorolac (4 mg/kg/day, p.o.; 2 weeks) has no detrimental effect in the volume fraction of bone trabeculae formed inside the alveolar socket in rats[2].
Ketorolac (60 μg; intrathecal injection; once) attenuates the damage caused by spinal cord ischemia in rats[3].
Ketorolac salt (20 and 30 mg/kg; i.p.; two times in a week for 3 weeks) reduces oral carcinogenesis in mice[4].

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

Animal Model: New Zealand White rabbits (2.0–2.7 kg), LPS endotoxin-induced ocular inflammation[1]
Dosage: 50 μL ketorolac tromethamine ophthalmic solution 0.4%
Administration: In eyes, twice, 2 hours and 1 hour before LPS challenge
Result: Resulted in a nearly complete inhibition (98.7%) of LPS endotoxin-induced increases in FITC (fluorescein isothiocyanate)-dextran in the anterior chamber, and resulted in a nearly complete inhibition (97.5%) of LPS endotoxin-induced increases in aqueous PGE2 concentrations in the aqueous humor.
Animal Model: Male Wistar rats (400–450 g), spinal cord ischemia model[3]
Dosage: 30 and 60 μg
Administration: Intrathecal injection, 1 h before the ischemia induction for once
Result: Significantly reduced the motor disturbances and improved the survival rate at 60 μg.
Animal Model: Significantly reduced the motor disturbances and improved the survival rate at 60 μg.
Dosage: 20 mg/kg and 30 mg/kg
Administration: IP injection, two times in a week for 3 weeks
Result: Decreased tumor burden, reduced expression of DDX3 and anti-apoptotic proteins (Bcl-2 and Mcl-1).
Clinical Trial
分子量

255.27

Formula

C15H13NO3

CAS 號(hào)
性狀

固體

顏色

White to light yellow

中文名稱

酮咯酸;酮洛酸

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 250 mg/mL (979.36 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.9174 mL 19.5871 mL 39.1742 mL
5 mM 0.7835 mL 3.9174 mL 7.8348 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)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(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.93%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)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
DMSO 1 mM 3.9174 mL 19.5871 mL 39.1742 mL 97.9355 mL
5 mM 0.7835 mL 3.9174 mL 7.8348 mL 19.5871 mL
10 mM 0.3917 mL 1.9587 mL 3.9174 mL 9.7936 mL
15 mM 0.2612 mL 1.3058 mL 2.6116 mL 6.5290 mL
20 mM 0.1959 mL 0.9794 mL 1.9587 mL 4.8968 mL
25 mM 0.1567 mL 0.7835 mL 1.5670 mL 3.9174 mL
30 mM 0.1306 mL 0.6529 mL 1.3058 mL 3.2645 mL
40 mM 0.0979 mL 0.4897 mL 0.9794 mL 2.4484 mL
50 mM 0.0783 mL 0.3917 mL 0.7835 mL 1.9587 mL
60 mM 0.0653 mL 0.3265 mL 0.6529 mL 1.6323 mL
80 mM 0.0490 mL 0.2448 mL 0.4897 mL 1.2242 mL
100 mM 0.0392 mL 0.1959 mL 0.3917 mL 0.9794 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:
Ketorolac
目錄號(hào):
HY-B0580
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