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NCGC00181764-01

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Also known as: 107667-60-7, Zinc l-carnosine, Beta-alanyl-l-histidinato zinc, Ncgc00181764-01, Dsstox_cid_28541, Dsstox_rid_82813

Molecular Formula

C₉H₁₃N₄O₃Zn-

Molecular Weight

290.6 g/mol

InChI Key

GFWBKUDRXMQSFD-FJXQXJEOSA-M

Polaprezinc is an orally bioavailable chelate composed of zinc and L-carnosine, with potential gastroprotective, anti-oxidant, anti-ulcer and anti-inflammatory activities. Upon administration, polaprezinc increases the expression of various anti-oxidant enzymes, such as superoxide dismutase 1 (SOD-1), SOD-2, heme oxygenase-1 (HO-1), glutathione S-transferase (GST), glutathione peroxidase (GSH-px), peroxidredoxin-1 (PRDX1; PRXI) and PRXD5 (PRXV) in the gastric mucosa, which protect cells against reactive oxygen species (ROS). In addition, this agent inhibits the activity of the transcription factor nuclear factor-kappaB (NF-kappaB) and reduces the expression of several pro-inflammatory cytokines, such as interleukin (IL) 1beta, IL-6, IL-8, and tumor necrosis factor alpha (TNF-a). Polaprezinc also increases the expression of various growth factors, such as platelet-derived growth factor-B (PDGF-B), vascular endothelial growth factor (VEGF), and nerve growth factor (NGF), and various heat shock proteins (HSPs), including HSP90, HSP70, HSP60, HSP47, HSP27, and HSP10. This protects against damages to, and accelerates healing of the gastric mucosa.

1 2D Structure

NCGC00181764-01

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

3-aminopropanoyl-[(1S)-1-carboxy-2-(1H-imidazol-5-yl)ethyl]azanide;zinc

2.1.2 InChI

InChI=1S/C9H14N4O3.Zn/c10-2-1-8(14)13-7(9(15)16)3-6-4-11-5-12-6;/h4-5,7H,1-3,10H2,(H3,11,12,13,14,15,16);/p-1/t7-;/m0./s1

2.1.3 InChI Key

GFWBKUDRXMQSFD-FJXQXJEOSA-M

2.1.4 Canonical SMILES

C1=C(NC=N1)CC(C(=O)O)[N-]C(=O)CCN.[Zn]

2.1.5 Isomeric SMILES

C1=C(NC=N1)C[C@@H](C(=O)O)[N-]C(=O)CCN.[Zn]

2.2 Synonyms

2.2.1 MeSH Synonyms

1. Ahz-zinc

2. Beta-alanyl-l-histidinato Zinc

3. Z 103

4. Z-103

5. Zinc Carnosine

6. Zinc L-carnosine

7. Zinc L-carnosine Complex

8. Zinc N-(3-aminopropionyl)histidine

2.2.2 Depositor-Supplied Synonyms

1. 107667-60-7

2. Zinc L-carnosine

3. Beta-alanyl-l-histidinato Zinc

4. Ncgc00181764-01

5. Dsstox_cid_28541

6. Dsstox_rid_82813

7. Dsstox_gsid_48615

8. Chembl3184454

9. Dtxsid7048615

10. Tox21_112950

11. Akos037515832

12. Db09221

13. Cas-107667-60-7

14. E76520

15. 667p607

2.3 Create Date

2011-05-03

3 Chemical and Physical Properties

Molecular Formula	C₉H₁₃N₄O₃Zn-
Molecular Weight	290.6 g/mol
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	4
Exact Mass	289.027907 g/mol
Monoisotopic Mass	289.027907 g/mol
Topological Polar Surface Area	110 Å²
Heavy Atom Count	17
Formal Charge	-1
Complexity	265
Isotope Atom Count	0
Defined Atom Stereocenter Count	1
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	2

4 Drug and Medication Information

4.1 Drug Indication

Peptic ulcer disease, dyspepsia.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Used to treat/manage peptic ulcer disease or irritation of the gastrointestinal tract by promoting tissue healing by the elimination of free radicals.

5.2 MeSH Pharmacological Classification

Anti-Ulcer Agents

Various agents with different action mechanisms used to treat or ameliorate PEPTIC ULCER or irritation of the gastrointestinal tract. This has included ANTIBIOTICS to treat HELICOBACTER INFECTIONS; HISTAMINE H2 ANTAGONISTS to reduce GASTRIC ACID secretion; and ANTACIDS for symptomatic relief. (See all compounds classified as Anti-Ulcer Agents.)

5.3 Absorption, Distribution and Excretion

Absorption

Intestinal absorption of L-CAZ was studied in rats by Sano et al. using 14C- and 65Zn-labeled compounds. They suggested that L-CAZ dissociates to its components, L-carnosine and zinc, during intestinal absorption.

Route of Elimination

Intestinal absorption of the drug was examined using 14C- and 65Zn-labeled compounds. Polaprezinc metabolizes into its components, L-carnosine and zinc, during intestinal absorption. It was found that the excretion rates after one administration using 14C-labeled L-CAZ to rats were 4.1% in urine, 13.3% in feces, and 38.8% in exhalation. The study using 65Zn-labeled Paleprozinc were 0.3% in urine and 85.0% in the feces. The absorption rate of zinc is estimated to be approximately 11%.

5.4 Metabolism/Metabolites

Excretion rates of polaprezinc after a single administration using 14C-labeled drug to rats are 4.1% in urine, 13.3% in feces, and 38.8% in exhalation, and those using 65Zn-labeled L-CAZ are 0.3% in urine and 85.0% in feces. The absorption rate of zinc is estimated to be about 11%.

5.5 Biological Half-Life

The half-life of polaprezinc has been studied in rats and found to be approximately 2 hours.

5.6 Mechanism of Action

Polaprezinc increases the expression of various antioxidant enzymes, including superoxide dismutase 1 (SOD-1), SOD-2, heme oxygenase-1 (HO-1), glutathione S-transferase (GST), glutathione peroxidase (GSH-px), peroxidredoxin-1 (PRDX1; PRXI) and PRXD5 (PRXV). This process occurs in the gastric mucosa, defending mucosal cells against reactive oxygen species. This drug inhibits the activity of the transcription factor nuclear factor-kappaB (NF-kB) and decreases the expression of various inflammatory cytokines, including interleukin (IL) 1beta, IL-6, IL-8, and tumor necrosis factor alpha (TNF-a). Polaprezinc also promotes the expression of numerous growth factors, including as platelet-derived growth factor-B (PDGF-B), vascular endothelial growth factor (VEGF), and nerve growth factor (NGF), in addition to various heat shock proteins (HSPs), including HSP90, HSP70, HSP60, HSP47, HSP27, and HSP10. This process promotes tissue growth and protects against damage the gastric mucosa.

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