ENZYME INHIBITORS AND DRUGS

ANTI-INFLAMMATORY DRUGS

EI-122
Anthralin
1,8-Dihydroxyanthrone
99%, MW=226.2 [1143-38-0] Storage: RT.
Widely used anti-psoriatic drug. Inhibits leukotriene biosynthesis (IC₅₀=7.5 然) and LTB₄ omega oxidation¹.
l g

EI-206
Auranofin
99%, MW=678.5 [34031-32-8] Storage: RT.
Widely used anti-arthritic drug. Inhibits various leukocyte activation pathways at multiple sites^2,3. Inhibits mediator release from human basophils, pulmonary mast cells and macrophages⁴. Inhibits 5-LO in human neutrophils⁵.
l00 mg
500 mg

EI-126
Dexamethasone
99%, MW=392.5 [50-02-2] Storage: RT
Anti-inflammatory glucocorticoid. Induces the production of phospholipase A₂ inhibitory protein (lipocortin)⁶. Inhibits induction of nitric oxide synthase⁷ (IC₅₀=5 nM). Induces apoptosis⁸.
1 g
5 g

EI-121
Disodium cromoglycate (DSCG, cromolyn sodium)
99%, crystalline solid, MW=512.3 [15826-37-6] Storage: RT
DSCG partially but significantly inhibits the effects of LTD₄ on pulmonary airway resistance⁹. Mast cell stabilizer¹⁰. Reduces mediator induced plasma leakage¹¹.
1 g
5 g

EI-207
Ebselen
2-Phenyl-1,2-benzisoselenazol-3(2H)-one
99%, MW=274.2 [60940-34-3] Storage: RT.
Novel selenium-containing anti-inflammatory agent. Inhibits 5-LO, CO, NADPH oxidase, and protein kinase C. Potent antioxidant. Possesses a unique glutathione peroxidase-like activity¹².
20 mg
100 mg

EI-208
NPC-14686
99%, MW=401.4, Storage: 0蚓
Novel anti-inflammatory agent. Blocks neutrophil recruitment (IC₅₀=16 然)¹³ via inhibition of leukocyte adhesion to endothelial cells¹⁴.
200 mg
1 g

EI-114
Oxatomide
99%, MW=426.6 [60607-34-3] Storage: RT
Suppresses PAF induced bronchoconstriction in the guinea pig (ED₅₀=0.9 mg/kg orally)¹⁵. Inhibits the release¹⁶ and actions¹⁷ of leukotrienes and other mediators¹⁵. Clinically useful anti-allergic drug¹⁸.
50 mg
250 mg

ARACHIDONOYL-CoA SYNTHETASE INHIBITORS

EI-116
EDYA
8,11-Eicosadiynoic acid
98%, MW=304.5, Storage: 0蚓.
Inhibits arachidonic acid uptake by platelets. Inhibits arachidonic acid specific and nonspecific acyl-CoA synthetase. Inhibits D5-desaturase and cyclooxygenase¹⁹.
1 mg
10 mg

EI-218
Triacsin C
2E, 4E, 7E-Undecatriene-1-triazene
~90%, MW=207.3 [76896-80-5] Storage: -20蚓, Solution in DMSO. Selectively inhibits arachidonoyl-CoA synthetase in intact cells and the nonspecific acyl-CoA synthetase in cell sonicates IC50=3.6-8.7 mM^20,21,22. Inhibits neutrophil functions²³.
100 mg
1 mg

CYCLOOXYGENASE INHIBITORS

EI-164
Ibuprofen
(?-2-(4-Isobutylphenyl)-propionic acid
99%, MW=206.3 [15687-27-1] Storage: RT
Selective cyclooxygenase inhibitor (IC₅₀=14.9 然)²⁴. Inhibits PGH synthase-1 and PGH synthase-2 with comparable potency (ID₅₀=8.9-14 and 7.2-8.2然 respectively, data is for (S) isomer)²⁵. Clinically useful NSAID. Inhibits the neutrophil dependent edema response of rabbit skin to C5a/PGE₂²⁶.
1 g
5 g

EI-276
(S)-Ibuprofen
(S)-(+)-2-(4-Isobutylphenyl)-propionic acid
99%, MW=206.3 [51146-56-6] Storage: RT
Active enantiomer of ibuprofen. Inhibits PGH synthase-1 and PGH synthase-2 with comparable potency, ID₅₀=8.9-14 and 7.2-8.2然 respectively²⁵.
1 g

EI-131
Indomethacin
99%, MW=357.8 [53-86-1] Storage: RT
Inhibits cyclooxygenase (IC₅₀=0.1 然) selectively over lipoxygenases (IC₅₀=100 然 for 5-, 12- and 15-LO)^27,28. Preferentially inhibits PGH synthase-1 over PGH synthase-2 (ID₅₀=4.9-8.1 and 130-160 然 respectively)²⁵. Activates PPAR a and g receptors and induces adipocyte differentiation (EC₅₀=8 mM)²⁹. A clinically useful NSAID.
1 g
5 g

EI-260
6-Methoxy-2-Naphthylacetic acid
99%, MW=216.2 [23981-47-7] Storage: RT
Cyclooxygenase inhibitor selective for PGH synthase-2 over of PGH synthase-1 (IC₅₀=15-55 and 200-280 然 respectively)²⁵.
10 mg
50 mg

EI-133
Naproxen
99%, MW=230.3 [22204-53-1] Storage: RT
Cyclooxygenase inhibitor³⁰. Clinically useful NSAID.
1 g
5 g

EI-261
NS-398
98%, MW=314.4 [123653-11-2] Storage: RT
Cyclooxygenase inhibitor. Selectively inhibits PGH synthase-2 (IC₅₀=1 然) with no inhibition of PGH synthase-1 at concentrations up to 100 然³¹.
5 mg
25 mg

EI-219
Piroxicam
99%, MW=331.3 [36322-90-4] Storage: RT
Cyclooxygenase inhibitor³². More selective for PGHS-1 (IC₅₀=17.7 然) over PGHS-2 (IC₅₀=>500 然)³³. Clinically useful NSAID.
1 g
5 g

AP-200
Sulindac sulfide
99%, MW=340.4 [32004-67-4] Storage: RT
Active metabolite of sulindac. Inhibits cyclooxygenase. More selective for PGHS-1 (ID₅₀=0.5然) over PGHS-2 (ID₅₀=14然)²⁵. Induces apoptosis by a cyclooxygenase independent mechanism³⁴.
5 mg
25 mg

AP-201
Sulindac sulfone
99%, MW=372.4 [59864-04-9] Storage: RT
Induces apoptosis but does not inhibit cyclooxygenase³⁴.
5 mg
25 mg

DUAL LO/CO INHIBITORS

EI-135
Curcumin
99%, MW=368.4 [458-37-7] Storage: RT
Dual inhibitor of 5-lipoxygenase (IC₅₀=8 然) and cyclooxygenase (IC₅₀=52 然)^35,36.
1 g
5 g

ET-004
ETYA
5,8,11,14-Eicosatetraynoic acid
98%, MW=296.5 [1191-85-1] Storage: 0蚓. Inhibits arachidonic acid uptake³⁷. Inhibits arachidonic acid specific and nonspecific acyl-CoA synthetase³⁷. Inhibits cyclooxygenase (ID₅₀=8 然) and all lipoxygenases (ID₅₀=10, 0.3 and 0.2 然 for 5-, 12- and 15-LO respectively)^27,38,39 in whole cells. Inhibits PLA₂⁴⁰ and cytochrome P-450. Stimulates luteinizing hormone release from cultured pituitary cells⁴².
20 mg
100 mg

EI-163
Meclofenamate sodium
99%, MW=318.1 [6385-02-0] Storage: RT
Dual 5-lipoxygenase (IC₅₀=46.8 然) and cyclooxygenase I and II inhibitor²⁵ (IC₅₀=0.6 然)⁴³. Clinically useful NSAID.
1 g
5 g

EI-134
Phenidone
1-Phenyl-3-pyrazolidinone
97%, MW=162.2 [92-43-3] Storage: RT.
Dual lipoxygenase (IC₅₀=24 然)³⁵ and cyclooxygenase (IC₅₀=11.8 然)³⁵ inhibitor⁴⁴.
5 g

CYTOCHROME P-450 INHIBITORS AND INDUCERS

EI-259
1-Aminobenzotriazole
99%, MW=134.1 [1614-12-6] Storage: RT
Suicide substrate for cytochrome P-450⁴⁵. Inhibits oxidative drug metabolism in vivo^46,47.
20 mg
100 mg

EI-162
Benzylimidazole
99%, MW=158.2 [4238-71-5] Storage: RT
Induces various cytochrome P-450 isozymes including lauric acid hydroxylase⁴⁸. Decreases plasma triglyceride levels in rats⁴⁸. Inhibits thromboxane A₂ synthase⁴⁹ .
1 g
5 g

EI-160
Clofibrate
2-(p-Chlorophenoxy)-2-methylpropionic acid ethyl ester
99%, MW=242.7 [637-07-0] Storage: RT.
Induces cytochrome P-450 IVA1 and IVA3 which catalyze the omega-oxidation of fatty acids and prostaglandins^50,51
1 g
5 g

EI-262
7-Ethoxyresorufin
98%, MW=241.2 [5725-91-7] Storage: RT
Fluorimetric substrate for cytochrome P450 IA1⁵². Inhibits vasorelaxant responses to acetylcholine⁵³.
2 mg
10 mg

EI-107
Ketoconazole
99%, MW=531.4 [65277-42-1] Storage: RT
Inhibits cytochrome P-450 dependent steps in the biosynthesis of steroid hormones in vivo^54,55. Antimetastatic⁵⁶ and antineoplastic activity⁵⁵. Antipsoriatic activity⁵⁷. Orally active 5-lipoxygenase⁵⁸ and thromboxane synthase inhibitor⁵⁹.
50 mg
500 mg

EI-132
Methoxsalen
8-Methoxypsoralen
99%, MW=216.2 [298-81-7] Storage: RT.
A potent suicide inhibitor of cytochrome P-450^60,61. Antipsoriatic activity following ultraviolet light exposure⁶².
1 g

EI-161
Muscone
99%, MW=238.4 [541-91-3] Storage: RT
Induces rat liver microsomal cytochrome P-450^63,64
100 mg
500 mg

EI-256
Metyrapone
99%, MW=226.34 [54-36-4] Storage: RT
Inhibits cytochrome P-450-mediated prostaglandin w/w-1 hydroxylase activity^63,64
1 g

EI-103
17-ODYA

EI-105
SKF-525A廈Cl
Proadifen
99%, MW=389.9 [62-68-0] Storage: RT
Cytochrome P-450 inhibitor⁶⁵. Inhibits cytochrome P-450-dependent arachidonate metabolism⁶⁶ (90% at 50 然)⁶⁷. Calcium antagonist⁶⁸. Stimulates endothelial cell prostacyclin production while inhibiting platelet thromboxane synthesis⁶⁹.
250 mg
1 g

GLUTATHIONE S-TRANSFERASE INHIBITORS

EI-128
Ethacrynic acid
99%, MW=303.1 [58-54-8] Storage: RT
Inhibits LTC₄ biosynthesis by inhibition of glutathione S-transferase (GST). Inhibits human and rat GST⁷⁰ isozymes (IC₅₀=5.3, 1.1 and 4 然 for a-, ? and p-isozymes respectively)⁷¹. Inhibits 15-hydroxyprostaglandin dehydrogenase⁷².
1 g
5 g

LEUKOTRIENE A₄ HYDROLASE AND EPOXIDE HYDROLASE INHIBITORS

EI-212
Bestatin
99%, MW=308.4 [65391-42-6] Storage: 0蚓
Inhibits LTA₄ hydrolase in a rapid, reversible, dose-dependent manner (IC₅₀=4 然)⁷³. Aminopeptidase inhibitor⁷⁴. Immunomodulator⁷⁵.
5 mg
25 mg

EI-213
Captopril
99%, MW=217.3 [62571-86-2] Storage: RT
Reversible and competitive inhibitor of LTA₄ hydrolase (IC₅₀=11 然)⁷⁶. Angiotensin-converting enzyme (ACE) inhibitor⁷⁷.
1 g
5 g

EI-104
Leukotriene A₃ methyl ester
Potent suicide inhibitor of LTA₄ hydrolase.

EI-108
4-PCO
4-Phenylchalcone oxide
99%, MW=300.4, Storage: 0蚓
Potent and selective inhibitor of microsomal⁷⁸ and cytosolic epoxide hydrolase (IC₅₀=68 nM)⁷⁹. Inhibits epoxide hydrolysis of epoxyeicosatrienoic acids⁸⁰.
20 mg
100 mg

LEUKOTRIENE METABOLISM INHIBITORS

EI-113
Acivicin
AT-125, U-42126
99%, MW=178.6 [42228-92-2] Storage: 0蚓
Irreversible inhibitor of g-glutamyl transpeptidase (ID₅₀=0.54 mM). Inhibits the enzymatic conversion of LTC₄ to LTD₄^81,82,83. Potent anti-tumor⁸⁴ and anti-leishmania agent⁸⁵.
100 mg
500 mg

EI-103
17-ODYA
17-Octadecynoic acid
99%, MW=280.4 [34450-18-5] Storage: 0蚓
Potent suicide inhibitor of LTB₄ w-oxidase (IC₅₀<5 然)⁸⁶. Potent and selective inhibitor of fatty acid w-hydroxylase (IC₅₀<100 nM)⁸⁷.
1 mg
10 mg

LIPOXYGENASE INHIBITORS

EI-216
AA-861
95%, MW=326.4 [80809-81-0] Storage: 0蚓
Potent, selective and orally active 5-lipoxygenase inhibitor^88,89,90.
20 mg
100 mg

EI-106
Baicalein
5,6,7-Trihydroxyflavone
98%, MW=270.2 [491-67-8] Storage: 0蚓
Selective 12-lipoxygenase inhibitor (ID₅₀=0.12 然, platelet 12-LO)⁹¹. Inhibits leukotriene biosynthesis (at higher concentrations) and release of lysosomal enzymes⁹². Inhibits adjuvant induced arthritis⁹³.
10 mg
50 mg

EI-124
Caffeic acid
97%, MW=180.2 [331-39-5] Storage: RT
Selective inhibitor of 5-lipoxygenase (IC₅₀=3.7 然)⁹⁴.
1 g
5 g

EI-211
CDC
Cinnamyl-3,4-dihydroxy-a-cyanocinnamate
98%, MW=321.3 [132465-11-3] Storage: RT
Selective 12-lipoxygenase inhibitor IC₅₀=0.063 然, 3.33 然 and 1.89 然 for 12-, 15- and 5-LO respectively in isolated enzyme preparations⁹⁵.
10 mg
50 mg

ET-003
ETI
5,8,11-Eicosatriynoic acid
98%, MW=300.4 [13488-22-7] Storage: 0蚓
Inhibits lipoxygenases (ID₅₀=3, 20 and 20 然 for 5-, 12- and 15-LO respectively) selectively over cyclooxygenase (ID₅₀=50 然) in whole cells^27,96,97.
1 mg
10 mg

EI-100
Esculetin
6,7-dihydroxycoumarin
98%, MW=178.1 [305-01-1] Storage: RT
Inhibitor of 5-lipoxygenase (ID₅₀=4 然) and 12-lipoxygenase (ID₅₀=2.5 然). Does not inhibit cyclooxygenase⁹⁸.
1 g

EI-130
Gossypol
96%, MW=518.6 [303-45-7] Storage: 0蚓
Inhibits RBL-1 5-lipoxygenase (IC₅₀=0.3 然) and 12-lipoxygenase (IC₅₀=0.7 然)⁹⁹. Antispermatogenic activity¹⁰⁰. Inhibits PAF and leukotriene induced guinea pig parenchyma contractions¹⁰¹.
100 mg
500 mg

EI-210
L-655,238 (REV 5901, para isomer)
a-Pentyl-4-(2-quinolinylmethoxy)-benzenemethanol
98%, MW=335.4, Storage: RT
Potent and selective inhibitor (IC₅₀=100 nM) of 5-LO-activating protein (FLAP)¹⁰². For a review of FLAP see reference 103.
10 mg
50 mg

EI-266
MK-886
99%, MW=494.0 [118414-82-7] Storage: RT
A potent and selective inhibitor of 5-lipoxygenase activating protein (FLAP)¹⁰³. Binds to FLAP with high affinity and prevents the activation of 5-lipoxygenase. IC₅₀s for leukotriene biosynthesis: 2.5 nM in intact leukocytes; 1.1 mM in whole blood^104,105.
5 mg
25 mg

EI-101
NDGA
Nordihydroguaiaretic acid
97%, MW=302.4 [500-38-9] Storage: RT
Selective inhibitor of lipoxygenases (IC₅₀=0.2, 30 and 30 然 for 5-, 12- and 15-LO respectively) over cyclooxygenase (IC₅₀=100 然)^27,106. Inhibits rat epidermal and hepatic microsomal cytochrome P-450(ID₅₀=40 然)¹⁰⁷.
1 g

EI-209
REV-5901
A dual activity leukotriene D₄ antagonist and selective 5-lipoxygenase inhibitor (IC₅₀=6 然).

PHOSPHOLIPASE INHIBITORS

PROSTACYCLIN SYNTHASE INHIBITORS

HP-015
15-HPETE
Inhibits prostacyclin synthase.

EI-217
Tranylcypromine廈Cl
trans-2-Phenylcyclopropylamine廈Cl
99%, MW=169.7 [1986-47-6] Storage: 0蚓
Inhibits prostacyclin synthase^108,109. Monoamine oxidase inhibitor.
1 g
5 g

THROMBOXANE SYNTHASE INHIBITORS

EI-119
Carboxyheptyl imidazole
99%, MW=210.3, Storage: -20蚓
Thromboxane synthase inhibitor^110,111,112.
10 mg
50 mg

EI-120
Carbethoxyhexyl imidazole
99%, MW=224.3, Storage: -20蚓
Thromboxane synthase inhibitor¹¹².
10 mg
50 mg

EI-111
Furegrelate sodium (U-63557A)
98%, MW=275.2 [85666-17-7] Storage: RT
Potent and selective orally active inhibitor of thromboxane A₂ synthase (ED₅₀=10 ng/ml, human platelets)^113-116. For reviews of TXA₂ synthase inhibitors see references 117 and 118.
100 mg
500 mg

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