产品说明书

Carprofen

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Chemical Structure| 53716-49-7 同义名 : Carprodyl;NSC 297935;Rovera;Imafen;Novox;quellin;C 5720;Ro 20-5720;Ridamyl;Rimadyl;Imadyl
CAS号 : 53716-49-7
货号 : A240973
分子式 : C15H12ClNO2
纯度 : 98%
分子量 : 273.714
MDL号 : MFCD00079028
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(383.61 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

SC 5% DMSO + 30% PEG400 + 2% tween 80 +H2O 2.5 mg/mL clear

生物活性
靶点

  • COX-2

    canine COX2, IC50:30 nM
描述 Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively[3]. Carprofen (10 µg/mL) shows cytoprotective effects in CCL (cranial) and CaCL (caudal) cells and decreases apoptosis of both cells. Carprofen (10 μg/mL) had the greatest cytoprotective effects for CCL and CaCL cells[4]. Carprofen acts in vivo on target tissues as COX-1-sparing drugs by sparing gastric PGE1 and PGE2 synthesis and production of TXB2 (thromboxane B2) by platelets[5]. The administration of maropitant alone and carprofen alone produced clinically significant sparing effects on the sevoflurane MAC-BAR (minimum alveolar concentration for blunting adrenergic response) in dogs. However, the combination of maropitant and carprofen did not produce any additive effect on the sevoflurane MAC-BAR reduction[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.65mL

0.73mL

0.37mL

18.27mL

3.65mL

1.83mL

36.53mL

7.31mL

3.65mL
参考文献

[1]Bialer M, Johannessen SI, et al. Progress report on new antiepileptic drugs: a summary of the Seventh Eilat Conference (EILAT VII). Epilepsy Res. 2004 Sep-Oct;61(1-3):1-48.

[2]Ricketts AP, Lundy KM, Seibel SB. Evaluation of selective inhibition of canine cyclooxygenase 1 and 2 by carprofen and other nonsteroidal anti-inflammatory drugs. Am J Vet Res. 1998 Nov;59(11):1441-6.

[3]Favia AD, Habrant D, Scarpelli R, et al. Identification and characterization of carprofen as a multitarget fatty acid amide hydrolase/cyclooxygenase inhibitor. J Med Chem. 2012;55(20):8807-8826

[4]Waldherr K, Zurbriggen A, Spreng DE, Forterre S. In vitro cytoprotective effects of acetylsalicylic acid, carprofen, meloxicam, or robenacoxib against apoptosis induced by sodium nitroprusside in canine cruciate ligament cells. Am J Vet Res. 2012;73(11):1752-1758

[5]Sessions JK, Reynolds LR, Budsberg SC. In vivo effects of carprofen, deracoxib, and etodolac on prostanoid production in blood, gastric mucosa, and synovial fluid in dogs with chronic osteoarthritis. Am J Vet Res. 2005;66(5):812-817

[6]Fukui S, Ooyama N, Tamura J, et al. Interaction between maropitant and carprofen on sparing of the minimum alveolar concentration for blunting adrenergic response (MAC-BAR) of sevoflurane in dogs. J Vet Med Sci. 2017;79(3):502-508