COX-2 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S5711 Deracoxib

Deracoxib (SC-046) is a COX-2 inhibitor with >48-fold selectivity over COX-1. It also exhibits inhibitory activity against phosphodiesterase (Ki = 3.6 μM against human PDE4D3).

S2349 Rutaecarpine

Rutaecarpine是从 Evodia rutaecarpa和相关草药中分离的indolopyridoquinazolinone生物碱。是一种新型的COX2抑制剂。

S4656 Parecoxib


S4049 Valdecoxib


Selective COX-2, IC50: 5 nM
S3043 Rofecoxib

Rofecoxib 是一种COX-2抑制剂,IC50为18 nM。

Selective COX-2, IC50: 18 nM
S4136 Carprofen

Carprofen 抑制犬科COX2,IC50为30 nM。

Selective canine COX2, IC50: 30 nM
S1261 Celecoxib (SC 58635)

Celecoxib是一种选择性COX-2抑制剂,在Sf9细胞中IC50为40 nM。

Selective COX-2, IC50: 40 nM
S2903 Lumiracoxib

Lumiracoxib是一种新型,选择性的COX-2抑制剂,Ki为0.06 μM;对COX1Ki值为3 μM。

Selective COX-2, Ki: 60 nM
S1959 Tolfenamic Acid

Tolfenamic Acid是一种COX-2抑制剂,IC50为0.2 μM。

Selective COX-2, IC50: 0.2 μM
s8433 NS-398 (NS398)

NS-398是一种选择性的COX-2抑制剂,对人源重组的COX-1和COX-2的IC50分别为75 μM和1.77μM。

Selective COX-2, IC50: 3.8 μM
S2040 Nimesulide

Nimesulide是一种选择性COX-2抑制剂,IC50为26 μM。

Selective COX-2, IC50: 26 μM
S9190 Oroxin B

Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.

S3899 Hederagenin

Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB.

S2531 Asaraldehyde


S0931 Jaceosidin

Jaceosidin induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin exhibits anti-cancer, anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation. Jaceosidin is a flavonoid isolated from Artemisia vestita.

S3255 Pectolinarigenin

Pectolinarigenin, an active anti-inflammatory ingredient in Cirsium chanroenicum, is a dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX).

S3283 Marmesin

Marmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) is a natural coumarin with COX-2 and 5-LOX dual inhibitory activity.

S3872 Guaiacol

Guaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.

S3018 Niflumic acid

Niflumic acid是环氧合酶-2 (COX-2)抑制剂,用于治疗关节和肌肉疼痛。

S3816 Dehydroevodiamine

Dehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.

S9208 Ginsenoside Rb3

Ginsenoside Rb3, extracted from the plant Panax ginseng, plays important roles in cardiovascular diseases, including myocardial ischemia-reperfusion (I/R) injury. Ginsenoside Rb3 (0.1-10 μM) is tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. Ginsenoside Rb3 shows the significant activity with an IC50 of 8.2 μM. Ginsenoside Rb3 also

S4028 Dexamethasone Sodium Phosphate

Dexamethasone Sodium Phosphate是一种白介素受体抑制剂,抑制COX-2

S6850 NE 52-QQ57

NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric

S2995 4-Hydroxyphenylpyruvic acid

4-Hydroxyphenylpyruvic acid (4-HPPA), an abundant colon metabolite of polyphenols, is a potent scavenger that suppresses levels of free radicals and cyclooxygenase-2 (COX-2) and contributes to reduced risk of colon cancer development.

S2595 FK-3311

FK-3311 (COX-2 Inhibitor V) is a selective, cell-permeable and orally available inhibitor of cyclooxygenase-2 (COX-2) with antiinflammatory. FK-3311 has protective effects against hepatic warm ischemia-reperfusion injury by marked inhibition of TxA2.

S4651 Etoricoxib


S0761 Desmethyl Celecoxib

Desmethyl Celecoxib is a selective inhibitor of cyclooxygenase-2 (COX-2) with IC50 of 32 nM. Desmethyl Celecoxib has anti-inflammatory activities. Desmethyl Celecoxib is an analog of Celecoxib with the optimal yield of 75%.

S5595 3-Carene

3-Carene (Carene, Delta-3-Carene) is a bicyclic monoterpene in essential oils extracted from pine trees. 3-Carene have potent pharmacological effects on COX-2 overexpression and LPS-induced migration of Raw264.7 macrophages. 3‐carene is shown to significantly stimulate the activity and expression of alkaline phosphatase, an early phase marker of osteoblastic differentiation.

S1576 Sulfasalazine (NSC 667219)

Sulfasalazine 是一种磺胺剂,是Mesalazine的衍生物,主要用作抗炎剂。

S3261 Myrislignan

Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan inhibits interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α). Myrislignan significantly inhibits the expressions of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) dose-dependently in LPS-stimulated macrophage cells. Myrislignan inhibits the NF-κB signalling pathway activation.

S9502 Madecassic acid

Madecassic acid (Brahmic acid), a natural triterpene first isolated from C. asiatica, has diverse anti-inflammatory and anti-diabetic effects, blocking NF-κB activation in macrophages and causing by iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 inhibition.

S3304 Stylopine

Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) reduces nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-alpha) and interleukin-1beta (IL-1beta), and the IL-6 production and cyclooxygenase-2 (COX-2) activity caused by the LPS stimulation. Stylopine is a major component of the leaf of Chelidonium majus L.

S6685 Mavacoxib

Mavacoxib (Trocoxil) is a selective, long-acting cyclooxygenase-2 (COX-2) inhibitor. Mavacoxib is a novel nonsteroidal anti-inflammatory drug (NSAID).

S3931 Ginsenoside Rd

Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP

S2047 Lornoxicam

Lornoxicam是COX-1COX-2抑制剂,IC50分别为5 nM和8 nM。

Pan COX-2, IC50: 8 nM
S5698 Ketorolac tromethamine salt

Ketorolac tromethamine is a synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic and antipyretic properties. It is a non-selective COX inhibitor with IC50s of 20 nM for both COX-1 and COX-2.

Pan COX2, IC50: 20 nM
S5192 S-(+)-Ketoprofen

S-(+)-Ketoprofen (Compound 1, Actron, (S)-Ketoprofen, Dexketoprofen) is a potent inhibitor of cyclooxygenase (COX) with IC50 of 1.9 nM and 27 nM for COX-1 and COX-2, respectively.

Pan COX-2, IC50: 27 nM
S4295 Meclofenamate Sodium

Meclofenamate Sodium是一种双COX-1/COX-2抑制剂,其IC50 分别为40 nM 和 50 nM,用于治疗关节、肌肉疼痛,关节炎以及痛经。

Pan COX-2, IC50: 50 nM
S4149 Amfenac Sodium Monohydrate

Amfenac Sodium Monohydrate是一种非甾体类镇痛消炎药。对COX1COX2的IC50分别为250 nM和150 nM。

Pan COX-2, IC50: 150 nM
S1903 Diclofenac Sodium

Diclofenac Sodium是非选择性COX抑制剂,作用于绵羊COX-1COX-2IC50分别为60和220 nM。

Pan COX-2, IC50: 200 nM
S5010 Indometacin Sodium

Indometacin Sodium (Indomethacin Sodium) is the sodium salt of indomethacin, which is a non-selective, reversible, and competitive inhibitor of cyclooxygenases 1 and 2 with anti-inflammatory, analgesic-antipyretic and tocolytic effects.

Pan COX2, IC50: 0.78 μM
S1396 Resveratrol (SRT501)

Resveratrol具有广泛靶点,包括环氧酶(如COX, IC50=1.1 μM)、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素,具有抗癌,抗炎,降血糖和其他有益心血管的作用。

Pan COX2, IC50: 1.3 μM
S1646 Ketorolac

Ketorolac是一种非选择性的COX抑制剂,作用于人类COX-1COX-2时, IC50分别为1.23 µM和3.50 µM。

Pan COX-2 (human), IC50: 3.50 μM
S1626 Naproxen Sodium

Naproxen Sodium 是一种非选择性环氧合酶(COX)抑制剂,作用于COX-1COX-2时,IC50分别为8.7 μM和5.2 μM。

Pan COX-2, IC50: 5.2 μM
S6686 SC-560

SC-560 is a highly selective COX-1 inhibitor with IC50 of 9 nM, compared with the IC50 of 6.3 μM for COX-2, nearly 1,000-fold higher than with COX-1.

Pan COX-2, IC50: 6.3 μM
S1723 Indomethacin (NSC-77541)

Indomethacin是一种非选择性的COX1COX2的抑制剂,IC50分别为0.1 μg/mL和5 μg/mL。常用于降低发热、减缓疼痛、僵硬和肿胀。

Pan COX-2, IC50: 14 μM
S1638 Ibuprofen (NSC 256857)

Ibuprofen 是一种抗炎类抑制剂,作用于COX-1COX-2IC50分别为13 μM和370 μM。

Pan COX-2, IC50: 370 μM
S4230 Oxaprozin

Oxaprozin 是一种非麻醉性,非甾体类抗炎药(NSAID),用于缓解与骨关节炎和类风湿关节炎相关的炎症,肿胀,僵硬,关节疼痛。

S3017 Aspirin (NSC 27223)

Aspirin是水杨酸类不可逆的COX1 and COX2抑制剂,常用作止痛药来缓解轻微疼痛,作为解热药减少发热,并作为一种抗炎药物。

S3008 Zaltoprofen


S1761 Suprofen

Suprofen 是一种双重的COX-1/COX-2抑制剂,用作抗炎症的镇痛剂或者退热剂。

S1255 Nepafenac


S4078 Mefenamic Acid

Mefenamic Acid是一种竞争性COX-1COX-2抑制剂。

S4248 Bromfenac Sodium

Bromfenac Sodium是一种非甾体类抗炎药(NSAID),具有抗炎活性,通过抑制环氧合酶1和2可阻断前列腺素的合成。

S1645 Ketoprofen

Ketoprofen 是双重 COX1/2 抑制剂,是非选择性的NSAID,作用于人重组COX-1和COX-2的 IC50分别为0.5 μM和2.33 μM。

s7889 Xanthohumol

Xanthohumol,来自啤酒花的一种异戊烯化查耳酮,抑制COX-1和COX-2活性,并表现出化学预防作用。Phase 1。

S2351 Salicin