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- Aminohippuric acid
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Aminohippuric acid | CAS No: 61-78-9 | GMP-certified suppliers
A medication that serves as a diagnostic agent to measure effective renal plasma flow and assess renal tubular excretory function for nephrological evaluation and clinical research.
Therapeutic categories
Primary indications
- Used to measure effective renal plasma flow (ERPF) and to determine the functional capacity of the tubular excretory mechanism
Product Snapshot
- Aminohippuric acid is available as an injectable liquid solution for intravenous administration
- It is primarily used for diagnostic applications to measure effective renal plasma flow and assess tubular excretory function
- The product is approved and available in regulatory markets including the US and Canada
Clinical Overview
Pharmacologically, aminohippurate is processed by the kidneys through glomerular filtration followed by active secretion in the proximal tubules. At low plasma concentrations (approximately 1.0 to 2.0 mg/100 mL), roughly 90% of aminohippurate is cleared from the renal bloodstream in a single passage, which supports its utility in accurately quantifying ERPF. At elevated plasma concentrations of 40 to 60 mg/100 mL, aminohippurate saturates the renal tubular secretion mechanism, allowing measurement of the transport maximum (Tm) for tubular secretion. These measurements are typically accompanied by inulin clearance tests to determine glomerular filtration rate (GFR), essential for interpreting secretory capacity.
The mechanism of action involves the renal clearance of aminohippurate via filtrative and secretory pathways, enabling direct evaluation of renal excretory function by quantitative urine analysis. Its high clearance rate and relatively low toxicity at diagnostic doses contribute to its continued use in renal function testing.
Safety considerations include the compound’s general tolerability at diagnostic plasma levels, with minimal toxicity reported. However, due to its renal handling characteristics, cautious use is warranted in patients with compromised kidney function or impaired tubular secretion.
Aminohippuric acid is recognized globally as an approved diagnostic agent, with applications primarily in clinical research and nephrological evaluation. Several pharmaceutical-grade sources provide this API, and procurement should emphasize compliance with pharmacopeial standards, batch-to-batch consistency, and purity specifications to ensure accurate and reliable clinical use. Analytical verification of identity, potency, and absence of contamination is critical for maintaining quality in formulation and diagnostic applications.
Identification & chemistry
| Generic name | Aminohippuric acid |
|---|---|
| Molecule type | Small molecule |
| CAS | 61-78-9 |
| UNII | Y79XT83BJ9 |
| DrugBank ID | DB00345 |
Pharmacology
| Summary | Aminohippurate is primarily utilized to assess effective renal plasma flow by exploiting its high renal clearance through glomerular filtration and active tubular secretion. It targets renal proximal tubule transporters involved in organic anion secretion, enabling quantification of tubular secretory capacity. Its pharmacodynamics facilitate evaluation of renal excretory function without significant systemic toxicity at diagnostic concentrations. |
|---|---|
| Mechanism of action | Aminohippurate is filtered by the renal glomeruli and secreted into the urine by the proximal tubules. By measuring the amount of drug in the urine it is possible to determine functional capacity and effective renal plasma flow. |
| Pharmacodynamics | Aminohippurate (p-aminohippuric acid, PAH, PAHA) is the glycine amide of p-aminobenzoic acid. It is filtered by the glomeruli and is actively secreted by the proximal tubules. At low plasma concentrations (1.0 to 2.0 mg/100 mL), an average of 90 percent of aminohippurate is cleared by the kidneys from the renal blood stream in a single circulation. It is ideally suited for measurement of ERPF since it has a high clearance, is essentially nontoxic at the plasma concentrations reached with recommended doses, and its analytical determination is relatively simple and accurate. Aminohippurate is also used to measure the functional capacity of the renal tubular secretory mechanism or transport maximum (Tm<sub>PAH</sub>). This is accomplished by elevating the plasma concentration to levels (40-60 mg/100 mL) sufficient to saturate the maximal capacity of the tubular cells to secrete aminohippurate. Inulin clearance is generally measured during Tm<sub>PAH</sub> determinations since glomerular filtration rate (GFR) must be known before calculations of secretory Tm measurements can be done. |
Formulation & handling
- Aminohippuric acid is a small molecule suitable for intravenous administration in liquid or injection solution form.
- Its relatively high water solubility and negative LogP indicate good aqueous stability but limited membrane permeability.
- As a low molecular weight compound, it does not require special peptide or biologic handling procedures.
Regulatory status
| Lifecycle | The API is currently marketed in Canada and the US, with primary patent protections having expired, leading to increased availability of generic formulations and a mature market landscape. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Aminohippuric acid is manufactured and packaged by a single originator company, Merck & Co., with branded products primarily available in the US and Canadian markets. The current presence of branded formulations suggests limited geographic distribution. Patent status is not indicated, so the extent of generic competition cannot be determined from the available data. |
|---|
Safety
| Toxicity | The intravenous LD<sub>50</sub> in female mice is 7.22 g/kg. |
|---|
- Intravenous LD50 in female mice is 7
- 22 g/kg, indicating low acute toxicity at typical exposure levels
- Handle with appropriate protective equipment to avoid exposure due to potential nephrotoxic effects
Aminohippuric acid is a type of Diagnostic agents
Diagnostic agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used in the field of medical diagnostics. These agents play a vital role in diagnosing various diseases and conditions by aiding in the visualization and identification of specific biomarkers or structures within the body.
Diagnostic agents encompass a wide range of substances, including contrast agents, radiopharmaceuticals, and imaging agents. Contrast agents are commonly used in medical imaging techniques such as X-rays, magnetic resonance imaging (MRI), and computed tomography (CT) scans. They enhance the visibility of certain tissues or organs, allowing healthcare professionals to detect abnormalities more accurately.
Radiopharmaceuticals are another type of diagnostic agent that combines a radioactive component with a pharmaceutical compound. These agents emit radiation that can be detected by specialized imaging equipment, enabling the visualization of metabolic processes and the identification of abnormal cellular activity.
Imaging agents are designed to target specific molecular structures or biomarkers within the body. They can be used to detect and visualize specific proteins, enzymes, or receptors associated with certain diseases or conditions. By targeting these specific biomarkers, imaging agents provide valuable information about the presence, location, and extent of a disease, aiding in diagnosis and treatment planning.
Overall, diagnostic agents are essential tools in modern medicine, facilitating accurate and timely diagnoses. These pharmaceutical APIs enable healthcare professionals to identify and monitor diseases at an early stage, leading to better patient outcomes and improved treatment strategies.
