MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 528424 | Name: CGP-28014

Description:

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

CGP-28014 is a catechol-O-methyltransferase inhibitor potentially for the treatment of Parkinson's disease.Although CGP-28014 increases the renal excretion of both dopamine and dihydroxyphenylacetic acid (DOPAC) it does not affect renal sodium handling indicating a different mechanism of action. CGP-28014 significantly reduced the levels of homovanillic acid (HVA), but did not modify DA and 3,4-dihydroxyphenylacetic acid (DOPAC).

Chemical Structure

CGP-28014
CGP-28014
CAS#111757-17-6

Theoretical Analysis

MedKoo Cat#: 528424

Name: CGP-28014

CAS#: 111757-17-6

Chemical Formula: C12H19N3O

Exact Mass: 221.1528

Molecular Weight: 221.30

Elemental Analysis: C, 65.13; H, 8.65; N, 18.99; O, 7.23

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
Bulk Inquiry
Related CAS #
No Data
Synonym
CGP-28014; CGP 28014; CGP28014
IUPAC/Chemical Name
(E)-N'-(6-oxo-1,6-dihydropyridin-2-yl)-N,N-dipropylformimidamide
InChi Key
MEYPAYJYAZKERR-JLHYYAGUSA-N
InChi Code
InChI=1S/C12H19N3O/c1-3-8-15(9-4-2)10-13-11-6-5-7-12(16)14-11/h5-7,10H,3-4,8-9H2,1-2H3,(H,14,16)/b13-10+
SMILES Code
CCCN(CCC)/C=N/C1=CC=CC(N1)=O
Appearance
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

Preparing Stock Solutions

The following data is based on the product molecular weight 221.30 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.

Recalculate based on batch purity %
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
1: Kambur O, Talka R, Ansah OB, Kontinen VK, Pertovaara A, Kalso E, Männistö PT. Inhibitors of catechol-O-methyltransferase sensitize mice to pain. Br J Pharmacol. 2010 Dec;161(7):1553-65. doi: 10.1111/j.1476-5381.2010.00999.x. PubMed PMID: 20726980; PubMed Central PMCID: PMC3010567. 2: Hansell P, Odlind C, Männistö PT. Different renal effects of two inhibitors of catechol-O-methylation in the rat: entacapone and CGP 28014. Acta Physiol Scand. 1998 Apr;162(4):489-94. PubMed PMID: 9597116. 3: Männistö PT. Catechol O-methyltransferase: characterization of the protein, its gene, and the preclinical pharmacology of COMT inhibitors. Adv Pharmacol. 1998;42:324-8. PubMed PMID: 9327906. 4: Psylla M, Günther I, Antonini A, Vontobel P, Reist HW, Zollinger A, Leenders KL. Cerebral 6-[18F]fluoro-L-DOPA uptake in rhesus monkey: pharmacological influence of aromatic amino acid decarboxylase (AAAD) and catechol-O-methyltransferase (COMT) inhibition. Brain Res. 1997 Aug 29;767(1):45-54. PubMed PMID: 9365014. 5: Günther I, Psylla M, Reddy GN, Antonini A, Vontobel P, Reist HW, Zollinger A, Nickles RJ, Beer HF, Schubiger PA, et al. Positron emission tomography in drug evaluation: influence of three different catechol-O-methyltransferase inhibitors on metabolism of [NCA] 6-[18F]fluoro-L-dopa in rhesus monkey. Nucl Med Biol. 1995 Oct;22(7):921-7. PubMed PMID: 8547890. 6: Kaakkola S, Gordin A, Männistö PT. General properties and clinical possibilities of new selective inhibitors of catechol O-methyltransferase. Gen Pharmacol. 1994 Sep;25(5):813-24. Review. PubMed PMID: 7835624. 7: Törnwall M, Kaakkola S, Tuomainen P, Kask A, Männistö PT. Comparison of two new inhibitors of catechol O-methylation on striatal dopamine metabolism: a microdialysis study in rats. Br J Pharmacol. 1994 May;112(1):13-8. PubMed PMID: 7518301; PubMed Central PMCID: PMC1910326. 8: Ménnistó PT. Clinical Potential of Catechol-OMethyltransferase (COMT) Inhibitors as Adjuvants in Parkinson's Disease. CNS Drugs. 1994 Mar;1(3):172-9. doi: 10.2165/00023210-199401030-00002. PubMed PMID: 27520516. 9: Wiese C, Cogoli-Greuter M, Weinreich R, Winterhalter KH. COMT inhibitors and metabolism of fluorodopa enantiomers in aggregating cell cultures. Naunyn Schmiedebergs Arch Pharmacol. 1993 Dec;348(6):582-5. PubMed PMID: 8133902. 10: Törnwall M, Männistö PT. Effects of three types of catechol O-methylation inhibitors on L-3,4-dihydroxyphenylalanine-induced circling behaviour in rats. Eur J Pharmacol. 1993 Nov 30;250(1):77-84. PubMed PMID: 8119326. 11: Bieck PR, Antonin KH, Farger G, Nilsson EB, Schmidt EK, Dostert P, Strolin Benedetti M, Waldmeier PC. Clinical pharmacology of the new COMT inhibitor CGP 28,014. Neurochem Res. 1993 Nov;18(11):1163-7. PubMed PMID: 8255368. 12: Steulet AF, Stöcklin K, Wicki P, Waldmeier P. Effects of CGP 28014 on the in vivo release and metabolism of dopamine in the rat striatum assessed by brain microdialysis. Neurochem Res. 1993 Nov;18(11):1131-6. PubMed PMID: 8255364. 13: Törnwall M, Tuomainen P, Männistö PT. Modulation of rat brain endogenous dopamine metabolism by new inhibitors of catechol O-methyltransferase. Eur J Pharmacol. 1993 Aug 3;239(1-3):39-45. PubMed PMID: 8223912. 14: Männistö PT, Tuomainen P, Tuominen RK. Different in vivo properties of three new inhibitors of catechol O-methyltransferase in the rat. Br J Pharmacol. 1992 Mar;105(3):569-74. PubMed PMID: 1628144; PubMed Central PMCID: PMC1908463. 15: Waldmeier PC, Baumann PA, Feldtrauer JJ, Hauser K, Bittiger H, Bischoff S, von Sprecher G. CGP 28014, a new inhibitor of cerebral catechol-O-methylation with a non-catechol structure. Naunyn Schmiedebergs Arch Pharmacol. 1990 Sep;342(3):305-11. PubMed PMID: 1980718. 16: Bieck PR, Nilsson E, Antonin KH. Effect of the new selective COMT inhibitor CGP 28014 A on the formation of 3-O-methyldopa (3OMD) in plasma of healthy subjects. J Neural Transm Suppl. 1990;32:387-91. PubMed PMID: 2128511. 17: Waldmeier PC, De Herdt P, Maitre L. Effects of the COMT inhibitor, CGP 28014, on plasma homovanillic acid and O-methylation of exogenous L-dopa in the rat. J Neural Transm Suppl. 1990;32:381-6. PubMed PMID: 2128510.

View History

CGP-20712

CGP-20712