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Chemistry

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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

NCGC00181764-01
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 Weight 290.6 g/mol
Molecular Formula C9H13N4O3Zn-
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count6
Rotatable Bond Count4
Exact Mass289.027907 g/mol
Monoisotopic Mass289.027907 g/mol
Topological Polar Surface Area110 Ų
Heavy Atom Count17
Formal Charge-1
Complexity265
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count2
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.


ABOUT THIS PAGE

NCGC00181764-01 Manufacturers

A NCGC00181764-01 manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of NCGC00181764-01, including repackagers and relabelers. The FDA regulates NCGC00181764-01 manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. NCGC00181764-01 API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

NCGC00181764-01 Suppliers

A NCGC00181764-01 supplier is an individual or a company that provides NCGC00181764-01 active pharmaceutical ingredient (API) or NCGC00181764-01 finished formulations upon request. The NCGC00181764-01 suppliers may include NCGC00181764-01 API manufacturers, exporters, distributors and traders.

click here to find a list of NCGC00181764-01 suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

NCGC00181764-01 JDMF

The Pharmaceuticals and Medical Devices Agency (PMDA) established the Japan Drug Master File (JDMF), also known as the Master File (MF), to permit Japanese and foreign manufacturers of drug substances, intermediates, excipients, raw materials, and packaging materials (‘Products’) to voluntarily register confidential information about the production and management of their products in Japan.

The NCGC00181764-01 Drug Master File in Japan (NCGC00181764-01 JDMF) empowers NCGC00181764-01 API manufacturers to present comprehensive information (e.g., production methods, data, etc.) to the review authority, i.e., PMDA (Pharmaceuticals & Medical Devices Agency).

PMDA reviews the NCGC00181764-01 JDMF during the approval evaluation for pharmaceutical products. At the time of NCGC00181764-01 JDMF registration, PMDA checks if the format is accurate, if the necessary items have been included (application), and if data has been attached.

click here to find a list of NCGC00181764-01 suppliers with JDMF on PharmaCompass.

NCGC00181764-01 GMP

NCGC00181764-01 Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of NCGC00181764-01 GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right NCGC00181764-01 GMP manufacturer or NCGC00181764-01 GMP API supplier for your needs.

NCGC00181764-01 CoA

A NCGC00181764-01 CoA (Certificate of Analysis) is a formal document that attests to NCGC00181764-01's compliance with NCGC00181764-01 specifications and serves as a tool for batch-level quality control.

NCGC00181764-01 CoA mostly includes findings from lab analyses of a specific batch. For each NCGC00181764-01 CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

NCGC00181764-01 may be tested according to a variety of international standards, such as European Pharmacopoeia (NCGC00181764-01 EP), NCGC00181764-01 JP (Japanese Pharmacopeia) and the US Pharmacopoeia (NCGC00181764-01 USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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