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  2. Immunology/Inflammation
  3. COX
  4. FR-188582

FR-188582 是高選擇性的環(huán)氧合酶 (COX-2) 抑制劑，IC50 值為 17 nM。

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FR-188582 Chemical Structure

FR-188582 Chemical Structure

CAS No. : 189699-82-9

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查看 COX 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC50 value of 17 nM.

IC50 & Target[1]

COX-2

17 nM (IC50)

體外研究
(In Vitro)

In a recombinant human cyclooxygenase (COX) enzyme activity, FR-188582 (FR188582) inhibits COX-2 with an IC50 value of 17 nM, and the inhibition of prostaglandin (PG) E2 formation by FR188582 isover 6000 times more selective for COX-2 than COX-1[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Oral administration of FR-188582 (0.01-3.2 mg/kg) reverses paw edema in adjuvant arthritic rats and shows a therapeutic effect in a dose-dependent manner with ED50 values (95% C.L.) of 0.074 (0.00021-0.53) and 0.063 (0.0039-0.31) mg/kg for adjuvant-injected paws and adjuvant-uninjected paws, respectively. The anti-inflammatory effect of FR-188582 (FR188582) is threefold more potent than that of Indomethacin with ED50 values (95% C.L.) of 0.24 (0.047-1.8) and 0.20 (0.021-0.79) mg/kg for adjuvant-injected paws and adjuvant-uninjected paws, respectively[1].

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

332.80

Formula

C16H13ClN2O2S
CAS 號
性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
純度 & 產(chǎn)品資料
參考文獻
Kinase Assay
[1]

Human recombinant COX-1 and COX-2 are expressed in Chinese hamster ovary cells. The appropriate COX enzyme (1 μg for COX-1 and/or 3 μg for COX-2) is preincubated in 100 mM Tris-HCl buffer (pH 7.3) containing hematin (2 μM) and tryptophan (5 mM) with drugs (0.0001-100 μM) dissolved in 1% DMSO for 5 min at 37°C prior to the addition of Arachidonic acid (10 μM) for 5 min at 37°C. Reactions are terminated by the addition of 1N HCl, and PGE2 production is measured by radioimmunoassay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats[1]
Female Lewis rats (140-180g) at the age of 8 weeks are used. Adjuvant arthritis is induced in female Lewis rats by intradermal injection into the plantar suface of the right hind paw of 0.5 mg of a suspension of heat-killed and dried Mycobacterium tuberculosis H37 RA in 0.05 mL of liquid Paraffin (day 0). The drugs, suspended and diluted on 0.5% methylcellulose, are given orally once a day therapeutically from day 15 to day 24 after adjuvant injection. Paw volume is measured before and 15,18,21,24 days after adjuvant injection with the Volume Meter TK-105, and edema is expressed as the increase in paw volume after adjuvant injection relative to the pre-injection value for each animal.The anti-inflammatory effect is expressed as the difference in paw edema compared with that of vehicle-treated adjuvant-control rats.

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

FR-188582 相關(guān)分類

  • 摩爾計算器

  • 稀釋計算器

The molarity calculator equation

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

質(zhì)量   濃度   體積   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start) × 體積 (start) = 濃度 (final) × 體積 (final)
× = ×
C1   V1   C2   V2
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：
FR-188582
目錄號：
HY-U00146
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