Inhibitor SourceBook™ Second Edition

Nitric Oxide Synthase (NOS) Inhibitors, continued
Calbiochem • Inhibitor SourceBook
Nitric Oxide/Oxidative Stress
Product Cat. No. Comments Size Price
N G -Monomethyl-L-arginine,
Monoacetate Salt
475886 (N w -Me-L-Arg; N G -Me-L-Arg, AcOH; L-NMMA)
A cell-permeable, L-arginine analog that acts as a competitive inhibitor
of all three isoforms of NOS (IC 50 = 650 nM for nNOS; IC 50 = 700 nM for
eNOS; IC 50 = 3.9 mM for iNOS).
L-NIL, Dihydrochloride 482100 [L-N 6 -(1-Iminoethyl)lysine, DiHCl]
A potent, cell-permeable, and selective NOS inhibitor that exhibits
greater selectivity for iNOS (IC 50 = 3.3 mM) compared to nNOS (IC 50 =
92 mM).
nNOS Inhibitor I 490070 {(4S)-N-(4-Amino-5[aminoethyl]aminopentyl)-N´-nitroguanidine, TFA}
A potent, cell-permeable, and highly selective inhibitor of nNOS (K i =
20 nM). Displays >2500-fold and 92-fold selectivity over eNOS and
iNOS, respectively.
N G -Nitro-L-arginine 483120 (L-NNA; N G -NO 2 -L-Arg)
A potent, cell-permeable, reversible inhibitor of bNOS (K i = 25 nM) and
eNOS (K i = 90 nM).
N G -Nitro-L-arginine Methyl Ester,
Hydrochloride
483125 (L-NAME, HCl; N w -NO 2 -L-Arg-OMe; N G -NO 2 -L-Arg-OMe)
A cell-permeable, more soluble analog of arginine and a competitive,
slowly reversible inhibitor of eNOS (IC 50 = 500 nM).
p-Nitroblue Tetrazolium Chloride 484235 (NBT; Nitro BT)
NADPH-diaphorase substrate that competitively inhibits NOS
(IC 50 = 3–4 mM).
7-Nitroindazole 483400 (7-Ni)
7-Nitroindazole, Sodium Salt 484500 (7-NiNa)
7-Nitroindazole, 3-Bromo-,
Sodium Salt
A cell-permeable, reversible and competitive inhibitor of nitric oxide
synthase (NOS) with high selectivity for the bNOS (IC 50 = 7 0 nM). Also
inhibits bovine eNOS (IC 50 = 800 nM). Binds to the heme group of NOS.
A more soluble form of 7-Nitroindazole (Cat. No. 483400). Its solubility
in artificial cerebrospinal fluid permits its use as an inhibitor of NOS in
brain tissue.
203912 (BrNINa)
Sodium salt of 3-Bromo-7-Nitroindazole (Cat. No. 2039 ) that is more
soluble in aqueous solutions and still penetrates the brain.
,3-PBITU, Dihydrobromide 512774 [S,S´-1,3-Phenylene-bis(1,2-ethanediyl)-bis-isothiourea, 2HBr]
A highly potent, cell-permeable, competitive inhibitor of human nitric
oxide synthase. Exhibits approximately 200 fold higher selectivity for
iNOS (K i = 47 nM) compared to eNOS (K i = 9.0 mM).
PPM- 8 529570 (2-Benzoylamino-1,4-naphthoquinone)
A novel, cell-permeable, anti-inflammatory agent that inhibits the
expression of inducible nitric oxide synthase (iNOS; IC 50 ~5 mM).
Acts by blocking the activation of NF-kB in vitro and in vivo.
N G -Propyl-L-arginine 537200 (N-PLA; N w -Propyl-L-arginine)
A potent, cell-permeable, competitive, and time-dependent inhibitor
of nNOS (K i = 57 nM for nNOS; K i = 80 mM for iNOS; K i = 8.5 mM for
eNOS).
-Pyrrolidinecarbodithioic Acid,
Ammonium Salt
548000 (Ammonium Pyrrolidinedithiocarbamate; APDC; PDTC, NH 4 )
A cell-permeable inhibitor of inducible NOS inhibits the induction of
nitric oxide synthase activity in rat alveolar macrophages.
SKF-525A, Hydrochloride 567300 (Proadifen)
A cell-permeable inhibitor of neuronal nitric oxide synthase
(IC = 90 mM).
50
L-Thiocitrulline, Dihydrochloride 589411 (2-Thioureido-L-norvaline)
A potent, cell-permeable, inhibitor of nNOS (K i = 60 nM) compared to
iNOS (K i = 3.6 mM).
TRIM 643500 [1-(2-Trifluoromethylphenyl)imidazole]
A potent, cell-permeable, inhibitor of nNOS (IC 50 = 28.2 mM) and iNOS
(IC 50 = 27.0 mM), however, it is only a weak inhibitor of eNOS
(IC 50 = .06 mM).
25 mg
50 mg
00 mg
$65
$ 4
$2 0
0 mg $ 7
mg
5 mg
$70
$2
00 mg $33
00 mg $33
250 mg
g
$37
$ 29
00 mg $83
0 mg $48
0 mg $98
50 mg $8
0 mg $98
5 mg $75
00 mg $34
g $2 5
0 mg $ 07
00 mg $48
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