Picolinic acid does not have a single defined biological target. It is used as a chemical intermediate in the synthesis of BACE 2 inhibitors for diabetes treatment. As a chelating agent, it can bind metal ions. It is also an isomer of niacin (nicotinic acid), which has the carboxyl side chain at the 3-position. Its biological effects are related to its chemical properties rather than specific receptor targeting.

Picolinic acid is not evaluated for direct pharmacological activity in cell-based assays. Its primary use is as a chemical intermediate and as a matrix for mass spectrometry. In the synthesis of BACE 2 inhibitors, it serves as a building block. Its chelating properties may be relevant in certain biochemical applications. No specific in vitro pharmacological activity has been reported.

In comparison to the control, topical administration of 1.5% PCL, 0.8% PCL, 0.369% PCL (pH7), 0.369% PCL (pH4), and 0.5% CDV significantly reduced the number of Ad-positive cultures and their entire length (days 1–14). The Ad5/NZW rabbit eye model's advertising shedding. The effectiveness of picolinic acid on the length of AD shedding appeared to follow a concentration-dependent pattern, however it was not statistically significant. Concentrations of picolinic acid do not cause any appreciable ocular toxicity [1].
Picolinic acid is not used for in vivo pharmacological applications. It is used as a chemical intermediate in the synthesis of pharmaceutical compounds and as a matrix for MALDI-TOF mass spectrometry. No direct in vivo pharmacological studies have been reported for this compound. It is used exclusively in laboratory synthesis and analytical applications.

Picolinic acid does not have established receptor binding assay protocols. Its chemical properties are characterized by standard analytical methods including NMR and HPLC. Physical properties: molecular weight 123.11 g/mol; molecular formula C6H5NO2; IUPAC name: 2-Pyridinecarboxylic acid; synonyms: 2-Picolinic acid, Pyridine-2-carboxylic acid, 2-Carboxypyridine; melting point: 134-142°C; appearance: white needle-like crystals; solubility: soluble in acetic acid, almost insoluble in ether, chloroform, and carbon disulfide. No specific biochemical assay protocols are applicable.

Cellular studies with Picolinic acid are not typically conducted as it is not a pharmacologically active agent. If used in cell-based research, it would be as a chemical intermediate or as a control compound. Standard cell culture protocols would apply if cellular effects were to be evaluated. No specific cellular activity has been reported.

In vivo studies are not conducted with Picolinic acid as it is not a drug candidate. It is used as a chemical intermediate in the synthesis of pharmaceutical compounds. No animal model studies have been reported for this compound. It is used exclusively in laboratory synthesis and analytical applications.

Picolinic acid has a molecular weight of 123.11 g/mol and a molecular formula of C6H5NO2. IUPAC name: 2-Pyridinecarboxylic acid. Synonyms: 2-Picolinic acid, Pyridine-2-carboxylic acid, 2-Carboxypyridine, o-Pyridinecarboxylic acid. Melting point: 134-142°C. Appearance: white needle-like crystals. Solubility: soluble in acetic acid, almost insoluble in ether, chloroform, and carbon disulfide. Storage: typically at room temperature.

No toxicology data are available for Picolinic acid as it is a chemical intermediate rather than a pharmaceutical compound. Standard safety precautions for handling carboxylic acids should be followed. The compound is intended for laboratory use only and is not intended for human consumption or therapeutic use. Appropriate personal protective equipment should be used when handling this compound.

[1]. A Novel Topical Antiviral Agent, PCL–016 (Picolinic Acid), Inhibits Adenovirus Replication in the Ad5/NZW Rabbit Ocular Model. ARVO Annual Meeting Abstract. May 2005 Volume 46, Issue 13.

Picolinic acid is a pyridine monocarboxylic acid with its carboxyl group at the 2-position. It is an intermediate in tryptophan metabolism. It serves as a matrix material for MALDI and is also a human metabolite. It is the conjugate acid of Picolinic acid esters. PCL-016, or Picolinic acid, is the active pharmaceutical ingredient of tryptophan, a Picolinic acid metabolite. It possesses anti-infective and immunomodulatory effects, with approximately 25-50 mg produced daily by the human body through the breakdown of tryptophan. PCL-016 plays a crucial role in zinc transport. As a therapeutic agent, this molecule inhibits the function of zinc finger proteins (ZFPs) by binding to them, altering their structure, and disrupting zinc binding. ZFPs are involved in viral replication and packaging, as well as normal cellular homeostasis. Picolinic acid has been shown to possess antiviral activity both in vitro and in vivo, sometimes synergistically with other cytokines (such as interferon-gamma) to influence immune responses. Therefore, acne vulgaris, herpes, and other viral infections are potential therapeutic targets for PCL-016.
Picolinic acid has been reported to be found in Fusarium lateritium, Aloe africana, and other organisms with relevant data.
See also: Nicotinamide (note moved to) Picolinic acid (note moved to).
Drug Indications

It has been studied for the treatment of acne, cold sores (herpes labialis), and sexually transmitted diseases.
Mechanism of Action

As a therapeutic agent, this molecule inhibits the function of zinc finger proteins (ZFPs) by binding to them, altering their structure, and disrupting zinc binding.
Pharmacodynamics

PCL-016, or Picolinic acid, is a Picolinic acid metabolite of tryptophan. It exerts its anti-infective and immunomodulatory effects by participating in zinc transport. ZFPs are involved in viral replication and packaging, as well as normal cellular homeostasis. Both in vitro and in vivo studies have demonstrated that Picolinic acid possesses antiviral activity.
Picolinic acid is also known as 2-Pyridinecarboxylic acid, 2-Picolinic acid, and 2-Carboxypyridine. It is an isomer of niacin. It is used in the preparation of BACE 2 inhibitors for diabetes treatment and as a matrix for MALDI-TOF mass spectrometry for nucleotide analysis. No clinical trials or regulatory approvals have been reported.

C6H5NO2

123.11

123.032

98-98-6

Picolinic acid-d4;284487-61-2

1018

White to off-white solid powder

1.3±0.1 g/cm3

292.5±13.0 °C at 760 mmHg

139-142 °C(lit.)

130.7±19.8 °C

0.0±0.6 mmHg at 25°C

1.571

-0.1

1

3

1

9

114

0

SIOXPEMLGUPBBT-UHFFFAOYSA-N

InChI=1S/C6H5NO2/c8-6(9)5-3-1-2-4-7-5/h1-4H,(H,8,9)

pyridine-2-carboxylic acid

PCL-016; NVTL-0001; NV-02

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~812.28 mM)
H2O : ≥ 50 mg/mL (~406.14 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (20.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (20.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (20.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 100 mg/mL (812.28 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)