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  1. Immunology/Inflammation
  2. COX
  3. Firocoxib

Firocoxib  (Synonyms: 非羅考昔; ML 1785713)

目錄號: HY-14670 純度: 99.92%
COA 產(chǎn)品使用指南 技術(shù)支持

Firocoxib (ML 1785713) 是一種有效的,選擇性的,口服活性的 COX-2 抑制劑,IC50 為 0.13 μM。Firocoxib 對 COX-2 的選擇性比對 COX-1 的選擇性高 58 倍 (IC50 為 7.5 μM)。Firocoxib 具有抗炎作用。

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Firocoxib Chemical Structure

Firocoxib Chemical Structure

CAS No. : 189954-96-9

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100 mg ¥4163
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Other Forms of Firocoxib:

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

Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects[1].

IC50 & Target[1]

COX-2

0.13 μM (IC50)

COX-1

7.5 μM (IC50)

體外研究
(In Vitro)

The COX-1:COX-2 selectivity ratios generally are established by comparing the IC50 for COX-1 to the IC50 for COX-2. The IC80 value more closely resembles the steady-state plasma drug concentration than does the IC50 value[1].
The selectivity ratio for Firocoxib based on the IC80 values is 121 (IC80 of 0.36 μM and 43.6 μM for COX-2 and COX-1, respectively), indicating that selectivity for COX-2 is not reduced at concentrations higher than the IC50. Notably, Firocoxib concentrations that yield 80% to 95% inhibition of COX-2 produce < 20% inhibition of 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)

Firocoxib (0.75-1.5mg/kg; oral gavage; female domestic shorthair cats) treatment efficacious in attenuating fever when administered to cats 1 or 14 hours before LPS challenge[1].
Pharmacokinetic properties of Firocoxib are determined after i.v. (2 mg/kg) and oral (3 mg/kg) administration in male cats. Firocoxib has moderate to high oral bioavailability (54% to 70%), low plasma clearance (4.7 to 5.8 mL/min/kg), and an elimination half-life of 8.7 to 12.2 hours[1].

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

Animal Model: 14 healthy female domestic shorthair cats (11-15 months old, 2.9-3.9 kg) with lipopolysaccharide (LPS)[1]
Dosage: 0.75 mg/kg, 1.5 mg/kg
Administration: Oral gavage
Result: Was efficacious in attenuating fever when administered to cats 1 or 14 hours before LPS challenge.
分子量

336.40

Formula

C17H20O5S

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

非羅考昔

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : ≥ 52 mg/mL (154.58 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)

* "≥" 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 2.9727 mL 14.8633 mL 29.7265 mL
5 mM 0.5945 mL 2.9727 mL 5.9453 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 (protect from light, stored under nitrogen)。-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

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
參考文獻

Firocoxib 相關(guān)分類

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 (protect from light, stored under nitrogen)。-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
DMSO 1 mM 2.9727 mL 14.8633 mL 29.7265 mL 74.3163 mL
5 mM 0.5945 mL 2.9727 mL 5.9453 mL 14.8633 mL
10 mM 0.2973 mL 1.4863 mL 2.9727 mL 7.4316 mL
15 mM 0.1982 mL 0.9909 mL 1.9818 mL 4.9544 mL
20 mM 0.1486 mL 0.7432 mL 1.4863 mL 3.7158 mL
25 mM 0.1189 mL 0.5945 mL 1.1891 mL 2.9727 mL
30 mM 0.0991 mL 0.4954 mL 0.9909 mL 2.4772 mL
40 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8579 mL
50 mM 0.0595 mL 0.2973 mL 0.5945 mL 1.4863 mL
60 mM 0.0495 mL 0.2477 mL 0.4954 mL 1.2386 mL
80 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9290 mL
100 mM 0.0297 mL 0.1486 mL 0.2973 mL 0.7432 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:
Firocoxib
目錄號:
HY-14670
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