Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Pharmacological inhibition of COX can provide relief from the symptoms of inflammation and pain. Drugs, like Aspirin, that inhibit cyclooxygenase activity have been available to the public for about 100 years. Two cyclooxygenase isoforms have been identified and are referred to as COX-1 and COX-2. Under many circumstances the COX-1 enzyme is produced constitutively (i.e., gastric mucosa) whereas COX-2 is inducible (i.e., sites of inflammation). Non-steroidal anti-inflammatory drugs (NSAID), such as aspirin and ibuprofen, exert their effects through inhibition of COX. The main COX inhibitors are the non-steroidal anti-inflammatory drugs (NSAIDs).


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Flurbiprofen axetil

Flurbiprofen axetil is a non-selective cyclooxygenase (COX) inhibitor. Flurbiprofen axetil has anti-inflammatory effect[1].

  • CAS Number: 91503-79-6
  • MF: C19H19FO4
  • MW: 330.350
  • Catalog: COX
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 424.3±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 203.0±22.2 °C

SC-58125

SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo, and it also can inhibit edema at the inflammatory site and is analgesic[1][2][3].

  • CAS Number: 162054-19-5
  • MF: C17H12F4N2O2S
  • MW: 384.348
  • Catalog: COX
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 512.6±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 263.8±30.1 °C

LFS-1107

LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research[1].

  • CAS Number: 1799330-91-8
  • MF: C12H11N5OS2
  • MW: 305.38
  • Catalog: c-Myc
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ginsenoside Compound K

Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.

  • CAS Number: 39262-14-1
  • MF: C36H62O8
  • MW: 622.873
  • Catalog: COX
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 723.1±60.0 °C at 760 mmHg
  • Melting Point: 178 °C
  • Flash Point: 391.1±32.9 °C

(-)-bornyl ferulate

(-)-Bornyl ferulate is a 5-lipoxygenase and COX inhibitor with IC50s of 10.4 μM and 12.0 μM, respectively[1].

  • CAS Number: 55511-07-4
  • MF: C20H26O4
  • MW: 330.41800
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5,8,11,14-Icosatetraynoic acid

Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively)[1]. Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM[2].

  • CAS Number: 1191-85-1
  • MF: C20H24O2
  • MW: 296.403
  • Catalog: PPAR
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 490.3±45.0 °C at 760 mmHg
  • Melting Point: 79-81ºC
  • Flash Point: 226.6±23.4 °C

COX-2-IN-14

COX-2-IN-14 (compound 2a) is a potent and selective COX-2 (cyclooxygenase-2) inhibitor. COX-2-IN-14 shows effective binding at the active site of COX-2 co-crystal. COX-2-IN-14 exhibits a high level of in vivo anti-inflammatory activity, reducing ear edema and myeloperoxidase (MPO) activity in mice[1].

  • CAS Number: 2428387-48-6
  • MF: C18H18N4O6
  • MW: 386.36
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ketorolac D4

Ketorolac D4 (RS37619 D4) is the deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2[1][2].

  • CAS Number: 1216451-53-4
  • MF: C15H9D4NO3
  • MW: 259.29300
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Xanthohumol

Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities.

  • CAS Number: 6754-58-1
  • MF: C21H22O5
  • MW: 354.396
  • Catalog: COX
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 576.5±50.0 °C at 760 mmHg
  • Melting Point: 157-159ºC
  • Flash Point: 203.4±23.6 °C

Pelubiprofen

Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects[1].

  • CAS Number: 69956-77-0
  • MF: C16H18O3
  • MW: 258.312
  • Catalog: COX
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 457.4±34.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 244.5±22.2 °C

Anti-inflammatory agent 56

Anti-inflammatory agent 56 (Compound 9) is a selective COX-2 inhibitor (IC50: 0.54 μM). Anti-inflammatory agent 56 has anti-oxidant and anti-inflammatory effects. Anti-inflammatory agent 56 inhibits oxidative stress induced cell death. Anti-inflammatory agent 56 inhibits oxidative stress and neuroinflammation by inhibiting Keap1, COX-2 and iNOS. Anti-inflammatory agent 56 has low acute toxicity in mice (LD50: 1000 mg/kg)[1].

  • CAS Number: 2413127-32-7
  • MF: C21H15F3N4O4S
  • MW: 476.43
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pectolinarigenin

Pectolinarigenin, isolated from Cirsium chanroenicum, is a dual inhibitor of COX-2/5-LOX. Anti-inflammatory activity[1]. Pectolinarigenin has potent inhibitory activities on melanogenesis[2].

  • CAS Number: 520-12-7
  • MF: C17H14O6
  • MW: 314.289
  • Catalog: COX
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 565.5±50.0 °C at 760 mmHg
  • Melting Point: 220-223°
  • Flash Point: 212.3±23.6 °C

Revaprazan Hydrochloride

Revaprazan hydrochloride is a novel acid pump antagonist (APA). Revaprazan hydrochloride reduces COX-2 expression and has significant anti-inflammatory actions activities in H. pylori infection[1].

  • CAS Number: 178307-42-1
  • MF: C22H24ClFN4
  • MW: 398.904
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 205-208°
  • Flash Point: N/A

Crocin II

Crocin II is isolated from the fruit of Gardenia jasminoides with antioxidant, anticancer, and antidepressant activity.Crocin II inhibits NO production with an IC50 value of 31.1 μM.Crocin II suppresses the expressions of protein and m-RNA of iNOS and COX-2[1].

  • CAS Number: 55750-84-0
  • MF: C38H54O19
  • MW: 814.824
  • Catalog: COX
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 1032.1±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 309.8±27.8 °C

Sulindac

Sulindac is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2.

  • CAS Number: 38194-50-2
  • MF: C20H17FO3S
  • MW: 356.411
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 581.6±50.0 °C at 760 mmHg
  • Melting Point: 182-185°C
  • Flash Point: 305.6±30.1 °C

Ibuprofen Impurity F

Ibuprofen Impurity F is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1].

  • CAS Number: 65322-85-2
  • MF: C13H18O2
  • MW: 206.28100
  • Catalog: COX
  • Density: 1.034 g/cm3
  • Boiling Point: 327.445ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 224.48ºC

Phenyl β-D-glucopyranoside

Phenyl β-D-glucopyranoside has anti-cancer and anti-inflammatory activities. Phenyl β-D-glucopyranoside inhibits nitric oxide (NO) production, and the expression of iNOS and COX-2. Phenyl β-D-glucopyranoside also inhibits the nuclear translocation of NF-κB[1].

  • CAS Number: 1464-44-4
  • MF: C12H16O6
  • MW: 256.25
  • Catalog: COX
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 482.1±45.0 °C at 760 mmHg
  • Melting Point: 176-178ºC(lit.)
  • Flash Point: 245.4±28.7 °C

Broussonin E

Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis[1].

  • CAS Number: 90902-21-9
  • MF: C17H20O4
  • MW: 288.338
  • Catalog: JAK
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 464.9±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 235.0±27.3 °C

Acetaminophen-13C2,15N

Acetaminophen-13C2,15N is the 13C and 15N labeled Acetaminophen[1]. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM;is a widely used antipyretic and analgesic agent[2][3][4]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[5].

  • CAS Number: 360769-21-7
  • MF: C613C2H915NO2
  • MW: 154.14
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Diclofenac Epolamine

Flector Patch (Diclofenac epolamine) is a non-steroidal anti-inflammatory drug (NSAID)[1]. Flector Patch is used for relieving arthritis Pain, acute Pain, osteoarthritis, and actinic Keratosis. Flector Patch has good skin absorption characteristics without local adverse reactions and allergies[2].

  • CAS Number: 119623-66-4
  • MF: C20H24Cl2N2O3
  • MW: 411.32
  • Catalog: COX
  • Density: N/A
  • Boiling Point: 412ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 203ºC

Esclentic acid

Esculentic acid is a selective COX-2 inhibitor and has anti-inflammatory effect. Esculentic acid is a pentacyclic triterpenoid that can be extracted from the Chinese herb Phytolacca esculenta[1][2].

  • CAS Number: 103974-74-9
  • MF: C30H48O5
  • MW: 488.70
  • Catalog: COX
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 609.4±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 336.4±28.0 °C

2,5-Di-tert-butylhydroquinone

2,5-Di-tert-butylhydroquinone (DTBHQ), the indirect food additive, regulates the activity of 5-lipoxygenase as well as the activity of COX-2 (IC50=1.8 and 14.1 μM for 5-LO and COX-2, respectively) [1].

  • CAS Number: 88-58-4
  • MF: C14H22O2
  • MW: 222.323
  • Catalog: COX
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 334.4±37.0 °C at 760 mmHg
  • Melting Point: 216-218 °C(lit.)
  • Flash Point: 151.5±21.1 °C

Indometacin

Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells.

  • CAS Number: 53-86-1
  • MF: C19H16ClNO4
  • MW: 357.78800
  • Catalog: Bacterial
  • Density: 1.32g/cm3
  • Boiling Point: 499.4ºC at 760 mmHg
  • Melting Point: 155-162 °C
  • Flash Point: 255.8ºC

Anti-inflammatory agent 20

Anti-inflammatory agent 20 (compound 5a) is a potent inhibitor of NO activity. Anti-inflammatory agent 20 shows anti-inflammatory activity. Anti-inflammatory agent 20 suppresses LPS-induced inflammation via inhibiting the activation of NF-κB and MAPK signaling and thereby reducing IL-6, TNF-α, iNOS, and COX-2 upregulation[1].

  • CAS Number: 2127403-65-8
  • MF: C39H66N2O8
  • MW: 690.95
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Axinelline A

Axinelline A is a potent COX inhibitor with IC50s of 2.22 μM and 8.89 μM against COX-2 and COX-1, respectively. Axinelline A shows anti-inflammatory activity[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FPL 62064

FPL 62064 is a potent 5-lipoxygenase (5-LOX) and COX dual inhibitor, with IC50 values of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase (cyclooxygenase), respectively. FPL 62064 has potent anti-inflammatory activity[1][2].

  • CAS Number: 103141-09-9
  • MF: C16H15N3O
  • MW: 265.310
  • Catalog: COX
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 442.6±25.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 221.5±23.2 °C

Rofecoxib-d5

Rofecoxib D5 (MK 966 D5) is the deuterium labeled Rofecoxib. Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells)[1][2].

  • CAS Number: 544684-93-7
  • MF: C17H14O4S
  • MW: 314.35600
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

10-Shogaol

[10]-Shogaol is an antioxidant from Zingiber officinale for human skin cell growth and a migration enhancer. [10]-Shogaol inhibits COX-2 with an IC50 of 7.5 μM and has antiproliferation activity[1][2][3].

  • CAS Number: 36752-54-2
  • MF: C21H32O3
  • MW: 332.47700
  • Catalog: COX
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Meloxicam-13C,d3

Meloxicam-13C,d3 is deuterium labeled Meloxicam. Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively.

  • CAS Number: 1309936-00-2
  • MF: C1313CH10D3N3O4S2
  • MW: 355.41
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-(6-Methoxynaphthalen-2-yl)propanoic acid

(±)-Naproxen ((Rac)-Naproxen) is a racemate of Naproxen (HY-15030). Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively.

  • CAS Number: 23981-80-8
  • MF: C14H14O3
  • MW: 230.259
  • Catalog: COX
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 403.9±20.0 °C at 760 mmHg
  • Melting Point: 157ºC
  • Flash Point: 154.5±15.3 °C