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Carprofen/卡洛芬 {[allProObj[0].p_purity_real_show]}

货号:A240973 同义名: Carprodyl; NSC 297935

Carprofen是一种非甾体抗炎剂,通过抑制 COX-2(IC50 = 3.9 μM)和 FAAH(IC50 = 78.6 μM)表现出抗炎和止痛作用,对 COX-1 活性抑制较弱。

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Type HazMat fee for 500 gram (Estimated)
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Carprofen/卡洛芬 化学结构 CAS号:53716-49-7
Carprofen/卡洛芬 化学结构
CAS号:53716-49-7
Carprofen/卡洛芬 3D分子结构
CAS号:53716-49-7
Carprofen/卡洛芬 化学结构 CAS号:53716-49-7
Carprofen/卡洛芬 3D分子结构 CAS号:53716-49-7
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Carprofen/卡洛芬 纯度/质量文件 产品仅供科研

货号:A240973 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 COX COX-1 COX-2 其他靶点 纯度
Piroxicam 98%
Salicylic acid 98%
Phenacetin 98%
Etodolac 99%
Flunixin meglumine 98%
Ibuprofen L-lysine 98%
Nabumetone 98%
Acemetacin 98%
Diflunisal 98%
Pranoprofen 98%
Ampiroxicam 98%
Meloxicam 98%
Sulindac 98%
Ketoprofen 98%
Mefenamic Acid 95%
Bromfenac sodium 98%
Oxaprozin 99%
Aspirin 99%
Nepafenac 98%
Zaltoprofen 99%
Salicin 98%
Suprofen 99%+
Xanthohumol 99%
Parecoxib 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

98%
Etoricoxib 99%
Niflumic Acid 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

99+%
Ibuprofen +

COX-1, IC50: 13 μM

+

COX-2, IC50: 370 μM

98%
Indomethacin ++

COX1, IC50: 0.28 μM

+

COX-2, IC50: 14 μM

97%
Lornoxicam ++++

COX-1, IC50: 5 nM

++++

COX-2, IC50: 8 nM

98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

+++

COX-2, IC50: 50 nM

99%
Asaraldehyde 98%
Naproxen +

COX-1, IC50: 8.7 μM

+

COX-2, IC50: 5.2 μM

98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

+++

COX-2, IC50: 200 nM

98%
NS-398 ++

COX-2, IC50: 3.8 μM

95%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

+++

COX-2, IC50: 150 nM

98%+
Nimesulide +

COX-2, IC50: 26 μM

98%
Lumiracoxib ++

COX-1, Ki: 3 μM

+++

COX-2, Ki: 60 nM

98%
Rutaecarpine 95%
Celecoxib ++++

COX-2, IC50: 40 nM

98%
Carprofen ++++

canine COX2, IC50: 30 nM

98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

++

COX-2 (human), IC50: 3.50 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Carprofen/卡洛芬 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].

Carprofen/卡洛芬 细胞实验

Cell Line
Concentration Treated Time Description References
T24 bladder cancer cells 40-100 μM 48 h Induced p75NTR expression and inhibited cell survival Mol Cancer Ther. 2008 Nov;7(11):3539-45
DU-145 prostate cancer cells 40-100 μM 48 h Induced p75NTR expression and inhibited cell survival, inducing apoptosis via the p38 MAPK pathway Mol Cancer Ther. 2008 Nov;7(11):3539-45
PC-3 prostate cancer cells 40-100 μM 48 h Induced p75NTR expression and inhibited cell survival, inducing apoptosis via the p38 MAPK pathway Mol Cancer Ther. 2008 Nov;7(11):3539-45
H4 neuroglioma cells 100 μM overnight Evaluate the effects of NSAIDs on Aβ42 secretion. Carprofen was the most potent compound, reducing Aβ42 by more than 90%. Neurobiol Dis. 2010 Sep;39(3):449-56
Mycobacterium tuberculosis H37Rv 400 mg/L 4 h Assess the effect of carprofen on gene expression in Mycobacterium tuberculosis J Antimicrob Chemother. 2020 Nov 1;75(11):3194-3201
Mycobacterium smegmatis 62.5 mg/L 5 days Evaluate the effect of carprofen on extracellular polymeric substances (EPS) in Mycobacterium smegmatis biofilms J Antimicrob Chemother. 2020 Nov 1;75(11):3194-3201
Mycobacterium smegmatis 250 mg/L 5 days Assess the inhibitory effect of carprofen on biofilm formation in Mycobacterium smegmatis J Antimicrob Chemother. 2020 Nov 1;75(11):3194-3201
Mycobacterium smegmatis 62.5 mg/L 60 min Evaluate the inhibitory effect of carprofen on efflux pumps in Mycobacterium smegmatis J Antimicrob Chemother. 2020 Nov 1;75(11):3194-3201
Mycobacterium smegmatis 250 mg/L 24 h Determine the minimum inhibitory concentration (MIC) of carprofen against Mycobacterium smegmatis J Antimicrob Chemother. 2020 Nov 1;75(11):3194-3201

Carprofen/卡洛芬 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Transgenic mice T7A6 mice Food 10 mg/kg Daily for 6 months Evaluate the effect of Carprofen on Aβ42 levels in muscle. Carprofen had no significant effect on Aβ42 levels in muscle. Neurobiol Dis. 2010 Sep;39(3):449-56
Mice Inflammatory pain model (CFA-induced) Intraperitoneal injection 5 mg/kg Starting 1 hour prior to testing on days 2, 4 and 5 following saline/CFA injection. To evaluate the effect of carprofen on voluntary gait changes in CFA-induced inflammatory pain model. Results showed that carprofen did not significantly reverse CFA-induced gait changes but completely attenuated CFA-induced heat and mechanical hypersensitivity. Neuropharmacology. 2018 Mar 1;130:18-29
Rats Excisional wound pain model Subcutaneous injection 5 mg/kg Single dose, evaluated at 1, 4, and 24 hours post-administration To evaluate the effect of Carprofen on pain responses to thermal and mechanical stimulation in an excisional wound pain model. Results showed that Carprofen increased the withdrawal time to thermal stimulation at 1 and 4 hours post-administration but had no significant effect on mechanical withdrawal thresholds. Korean J Pain. 2021 Apr 1;34(2):165-175
Canine Healthy dogs Oral 4.4 mg/kg Single dose, observed for 6 hours Evaluated the effect of Carprofen on growth factor and cytokine release, showing increased TGF-β1 concentrations at 6 h and significantly decreased IL-10 concentrations Gels. 2024 Jun 12;10(6):396
Mice STR/Ort mice spontaneous osteoarthritis model Intraperitoneal injection 5 mg/kg 3 consecutive days To evaluate the effect of carprofen on osteoarthritis-related pain relief. Results showed that carprofen treatment did not modify any gait measurements or treadmill noncompliance, suggesting that gait changes in STR/Ort mice were not due to pain. Arthritis Rheumatol. 2014 Jul;66(7):1832-42

Carprofen/卡洛芬 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

Carprofen/卡洛芬 实验方案

计算器
存储液制备 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

Carprofen/卡洛芬 技术信息

CAS号53716-49-7
分子式C15H12ClNO2
分子量 273.71
SMILES Code CC(C1=CC(NC2=C3C=C(Cl)C=C2)=C3C=C1)C(O)=O
MDL No. MFCD00079028
别名 Carprodyl; NSC 297935; Rovera; Imafen; Novox; quellin; C 5720; Ro 20-5720; Ridamyl; Rimadyl; Imadyl
运输蓝冰
InChI Key PUXBGTOOZJQSKH-UHFFFAOYSA-N
Pubchem ID 2581
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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