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Inhibitor SourceBook™ Second Edition

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Other <strong>Inhibitor</strong>s of Biological Interest<br />

Phosphodiesterase <strong>Inhibitor</strong>s, continued<br />

Product Cat. No. Comments Size Price<br />

3-Isobutyl- -methylxanthine 410957 (IBMX)<br />

8-Methoxymethyl-3-isobutyl- -<br />

methylxanthine<br />

4-{[3´,4´-(Methylenedioxy)benzyl]<br />

amino}-6-methoxyquinazoline<br />

A cell-permeable, non-specific inhibitor of cAMP and cGMP<br />

phosphodiesterases (IC 50 = 2–50 mM).<br />

454202 (8-Methoxymethyl-IBMX)<br />

A cell-permeable, selective inhibitor of PDE I (IC 50 = 4 mM).<br />

58 Orders Phone 800 854 34 7<br />

Calbiochem • <strong>Inhibitor</strong> SourceBook<br />

Fax 800 776 0999<br />

Web www.emdbiosciences.com/calbiochem<br />

250 mg<br />

g<br />

$45<br />

$ 7<br />

0 mg $ 0<br />

475250 A potent and specific inhibitor of PDE V (IC 50 = 230 nM). mg $69<br />

Milrinone 475840 [1,6-Dihydro-2-methyl-6-oxo-(3,4´-bipyridine)-5-carbonitrile]<br />

A cell-permeable, selective inhibitor of PDE III (IC 50 = 300 nM).<br />

MY-5445 474925 [1-(3-Chlorophenylamino)-4-phenylphthalazine]<br />

A cell-permeable, selective inhibitor of PDE V (IC 50 = 600 nM).<br />

N Phosphodiesterase 4 <strong>Inhibitor</strong> 524717 [3,5-Dimethyl-1-(3-nitrophenyl)-1H-pyrazole-4-carboxylic acid ethyl<br />

ester]<br />

A high-affinity active site binding inhibitor of phosphodiesterases<br />

IVB and IVD (IC 50 = 33 and 2 nM, respectively).<br />

Phosphodiesterase V <strong>Inhibitor</strong> II 524714 (PDE V <strong>Inhibitor</strong> II)<br />

A cell-permeable, potent, and highly selective phosphodiesterase V<br />

inhibitor (IC 50 = 5 nM for bovine aorta PDE V; IC 50 > 0 mM for human<br />

recombinant PDE I & III, and for bovine aorta PDE II & IV).<br />

Ro-20- 724 557502 [4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone]<br />

A cell-permeable, selective inhibitor of PDE IV (IC 50 = 2 mM).<br />

Rolipram 557330 {4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone}<br />

A cell-permeable, selective and competitive inhibitor of PDE IV<br />

(IC 50 = 800 nM). Does not inhibit PDE I or PDE II, even at<br />

00 mM. Only a weak inhibitor of PDE III (IC 50 = 00 mM). A rolipraminsensitive<br />

PDE IV subtype is also known to exist.<br />

Trequinsin, Hydrochloride 382425 [9,10-Dimethoxy-2-mesitylimino-3-methyl-2,3,6,7-tetrahydro-4Hpyrimido-(6,1-a)-isoquinolin-4-one,<br />

HCl; HL 725]<br />

A cell-permeable and extremely potent inhibitor of PDE III<br />

(IC 50 = 300 pM) and platelet aggregation in vitro.<br />

0 mg $ 75<br />

0 mg $ 7<br />

0 mg $ 29<br />

5 mg $84<br />

00 mg $6<br />

5 mg $ 28<br />

0 mg $ 82<br />

Vinpocetine 677500 A selective inhibitor of PDE I (IC 50 = 20 mM). 20 mg $67<br />

W-5, Hydrochloride 681625 [N-(6-Aminohexyl)-1-naphthalenesulfonamide, HCl]<br />

A cell-permeable, calmodulin antagonist that inhibits PDE I<br />

(IC 50 = 240 mM).<br />

W-7, Hydrochloride 681629 [N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide, HCl]<br />

A calmodulin antagonist that inhibits PDE I (IC 50 = 28 mM). A cerebral<br />

vasodilator.<br />

W- 2, Hydrochloride 681635 [N-(4-Aminobutyl)-2-naphthalenesulfonamide, HCl]<br />

A calmodulin antagonist that inhibits PDE I (IC 50 = 260 mM).<br />

W- 3, Hydrochloride 681636 [N-(4-Aminobutyl)-5-chloro-2-naphthalenesulfonamide, HCl]<br />

A calmodulin antagonist that inhibits PDE I (IC 50 = 68 mM).<br />

Zaprinast 684500 {1,4-Dihydro-5-(2-propoxyphenyl)-7H-1,2,3-triazolo<br />

[4,5-d]pyrimidine-7-one; M&B22948}<br />

Phosphodiesterase <strong>Inhibitor</strong> Set I<br />

A cell-permeable, selective inhibitor of PDE V (IC 50 = 450 nM). Inhibits<br />

PDE IX at much higher concentrations (IC 50 = 35 mM).<br />

mg $77<br />

0 mg $77<br />

mg $77<br />

mg $77<br />

25 mg $49<br />

Provided as a set of 4 vials. Each set contains 0 mg of 8-Methoxymethyl-3-isobutyl- -methylxanthine (Cat. No. 454202), a Ca 2+ /CaM-dependent<br />

PDE (PDE I) inhibitor; mg of 4-{[3,4 -(Methylenedioxy)benzyl]amino}-6-methoxyquinazoline (Cat. No. 475250), a cGMP-specific PDE (PDE V)<br />

inhibitor; 5 mg of Rolipram (Cat. No. 557330), a cAMP-specific PDE (PDE IV) inhibitor; and 0 mg of Trequinsin, Hydrochloride (Cat. No. 382425), a<br />

cGMP-inhibited PDE (PDE III) inhibitor.<br />

Cat. No. 524718 1 set $347

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