U-0521 | CAS#5466-89-7 | COMT Inhibitor

U-0521
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 561075

CAS#: 5466-89-7

Description: U-0521 is a catechol-O-methyltransferase (COMT) inhibitor. U-0521 enhances the availability and utilization of levodopa in the brain.

Chemical Structure

U-0521

CAS# 5466-89-7

Instruction

Theoretical Analysis

MedKoo Cat#: 561075
Name: U-0521
CAS#: 5466-89-7
Chemical Formula: C10H12O3
Exact Mass: 180.08
Molecular Weight: 180.203
Elemental Analysis: C, 66.65; H, 6.71; O, 26.63

Price and Availability

Size	Price	Availability	Quantity
20mg	USD 300	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: U-0521, U0521, U 0521

IUPAC/Chemical Name: 3',4'-Dihydroxy-2-methylpropiophenone

InChi Key: VDQLKIBLTMPAHI-UHFFFAOYSA-N

InChi Code: InChI=1S/C10H12O3/c1-6(2)10(13)7-3-4-8(11)9(12)5-7/h3-6,11-12H,1-2H3

SMILES Code: CC(C)C(C1=CC=C(O)C(O)=C1)=O

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 180.20 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Cumming P, Boyes BE, Martin WR, Adam M, Ruth TJ, McGeer EG. Altered metabolism of [18F]-6-fluorodopa in the hooded rat following inhibition of catechol-O-methyltransferase with U-0521. Biochem Pharmacol. 1987 Aug 1;36(15):2527-31. PubMed PMID: 3111485.

2: Lloyd T, Waldman CD. The antihypertensive effect of U-0521 (3',4'-dihydroxy-2-methylpropiophenone). Life Sci. 1982 Nov 8;31(19):2121-7. PubMed PMID: 7176811.

3: Reches A, Jiang D, Fahn S. Catechol-O-methyltransferase inhibition by U-0521 increases striatal utilization of levodopa. Naunyn Schmiedebergs Arch Pharmacol. 1982 Jul;320(1):34-7. PubMed PMID: 7121609.

4: Henseling M. Accumulation of 3H-(-)noradrenaline in the rabbit aorta not related to uptake1 and uptake2, but sensitive to 3,4-dihydroxy-2-methylpropiophenone (U-0521) and oxytetracycline. Naunyn Schmiedebergs Arch Pharmacol. 1983 Jun;323(2):121-7. PubMed PMID: 6888566.

5: Rice PJ, Abraham ST, Huang NY, Doman RJ. Extraneuronal uptake inhibitor U-0521 decreases contractile responses in rat vas deferens. Gen Pharmacol. 1997 Sep;29(3):437-9. PubMed PMID: 9378252.

6: Bryan LJ, O'Donnell SR. Comparison of the effects of tropolone, beta-thujaplicin and U-0521 on the extraneuronal accumulation of isoprenaline in guinea-pig trachealis smooth muscle cells. A quantitative fluorescence histochemical study. Naunyn Schmiedebergs Arch Pharmacol. 1979 Jul;307(3):235-41. PubMed PMID: 492345.

7: Lloyd T, Boyd B, Walega MA, Ebersole BJ, Weisz J. A comparison of 2-hydroxyestradiol and U-0521 (3'4'-dihydroxy-2-methylpropiophenone, Upjohn) as in situ and in vitro inhibitors of tyrosine hydroxylase. J Neurochem. 1982 Apr;38(4):948-54. PubMed PMID: 6121005.

8: Fahn S, Comi R, Snider SR, Prasad AL. Effect of a catechol-O-methyl transferase inhibitor, U-0521, with levodopa administration. Biochem Pharmacol. 1979 Apr 1;28(7):1221-5. PubMed PMID: 444281.

9: Reches A, Jiang D, Fahn S. Effect of 3',4'-dihydroxy-2-methyl-propriophenone (U-0521) on catechol-O-methyltransferase activity and on DOPA accumulation in rat red blood cells and corpus striatum. Biochem Pharmacol. 1982 Nov 1;31(21):3415-8. PubMed PMID: 7150363.

10: Bryan LJ, Fleig H, Trendelenburg U. A comparative study of the properties of the catechol-O-methyltransferase inhibitors, U-0521 and tropolone acetamide, in rat perfused heart. Naunyn Schmiedebergs Arch Pharmacol. 1983 Feb;322(1):6-19. PubMed PMID: 6843690.

11: Paiva MQ, Guimarães S. The oil immersion technique for studying the disposition of drugs inducing relaxation; influence of U-0521 and hydrocortisone on the disposition of isoprenaline. J Pharm Pharmacol. 1980 Dec;32(12):868-9. PubMed PMID: 6110758.

12: Giles RE, Miller JW. Studies on the potentiation of the inotropic actions of certain catecholamines by U-0521 (3',4'-dihydroxy-alpha-methyl propiophenone). J Pharmacol Exp Ther. 1967 Jul;157(1):55-61. PubMed PMID: 6029491.

13: Sterin-Borda L, Gimeno MF, Borda ES, Gimeno AL. A positive influence of frequency on the inotrophic response of isolated rat atria to certain adrenergic amines. Effects of cocaine and U-0521 (3',4'-dihydroxy-2-methyl propiophenone. Proc Soc Exp Biol Med. 1977 Nov;156(2):315-20. PubMed PMID: 928402.

14: Gimeno AL, Gimeno MF, Sterin-Borda L, Cossio PM, Sterin-Speziale N, Diez C, Seara SM, Arana RM. Altered inotropic and chronotropic effects of noradrenaline on isolated rat atria exposed to chagasic sera. Influences of cocaine, normetanephrine and U-0521 (3'-4'-dihydroxy-2-methyl propiophenone. Cardiovasc Res. 1979 Dec;13(12):723-31. PubMed PMID: 119577.

15: Giles RE, Miller JW. The catechol-O-methyl transferase activity and endogenous catecholamine content of various tissues in the rat and the effect of administration of U-0521 (3',4'-dihydroxy-2-methyl propiophenone). J Pharmacol Exp Ther. 1967 Nov;158(2):189-94. PubMed PMID: 5625691.

16: Kaumann AJ, Wittmann R, Birnbaumer L, Hoppe BH. Activation of myocardial beta-adrenoceptors by the nitrogen-free low affinity ligand 3',4'-dihydroxy-alpha-methylpropiophenone (U-0521). Naunyn Schmiedebergs Arch Pharmacol. 1977 Feb;296(3):217-28. PubMed PMID: 14306.

17: Branco D, Osswald W. The fate of isoprenaline after inhibition of O-methylation and of extraneuronal uptake. Eur J Pharmacol. 1980 Oct 17;67(2-3):247-53. PubMed PMID: 7461032.

18: Barone S, Panek D, Bennett L, Stitzel RE, Head RJ. The influence of oestrogen and oestrogen metabolites on the sensitivity of the isolated rabbit aorta to catecholamines. Naunyn Schmiedebergs Arch Pharmacol. 1987 May;335(5):513-20. PubMed PMID: 3614387.

19: Percy E, Kaye DM, Lambert GW, Gruskin S, Esler MD, Du XJ. Catechol-O-methyltransferase activity in CHO cells expressing norepinephrine transporter. Br J Pharmacol. 1999 Oct;128(3):774-80. PubMed PMID: 10516661; PubMed Central PMCID: PMC1571673.

20: Nuutila J, Kaakkola S, Männistö PT. Potentiation of central effects of L-dopa by an inhibitor of catechol-O-methyltransferase. J Neural Transm. 1987;70(3-4):233-40. PubMed PMID: 2960778.

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