| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
This compound is classified as a drug metabolite rather than a direct therapeutic target. It is generated from CPT-11 via cytochrome P-450 3A4 (CYP3A4) metabolism. RPR132595A hydrochloride has been identified as one of the major metabolites of irinotecan, useful for studying metabolic pathways and drug-drug interactions involving CYP3A4.
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| ln Vitro |
RPR132595A is a bioactive metabolite of CPT-11 that retains pharmacological activity. The compound is used primarily for the identification and quantification of irinotecan metabolites in biological samples. Its presence in plasma and urine is monitored to assess metabolic clearance pathways and potential drug interactions that may affect irinotecan efficacy or toxicity.
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| ln Vivo |
As a metabolite of CPT-11, RPR132595A circulates in the body following administration of the parent drug. It is formed in the liver via CYP3A4 metabolism and subsequently excreted into urine. Its pharmacokinetic profile is important for understanding the disposition and elimination pathways of irinotecan. This metabolite can be measured in plasma and urine samples during preclinical and clinical studies to evaluate metabolic clearance.
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| Enzyme Assay |
In vitro enzyme assay protocol for CYP3A4-mediated metabolite generation: Human liver microsomes (0.5 mg/mL) are incubated with CPT-11 (1-100 uM) in 100 mM potassium phosphate buffer (pH 7.4) containing an NADPH-regenerating system (1.3 mM NADP+, 3.3 mM glucose-6-phosphate, 0.4 U/mL glucose-6-phosphate dehydrogenase, 3.3 mM MgCl2) at 37degC for 30-60 min. The reaction is terminated by adding ice-cold acetonitrile. RPR132595A formation is quantified by LC-MS/MS using a C18 column and positive ion electrospray ionization. Kinetic parameters (Km, Vmax) are determined by Michaelis-Menten analysis.
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| Cell Assay |
Cell-based metabolism assay protocol: Primary human hepatocytes or HepG2 cells overexpressing CYP3A4 are cultured in Williams E medium. Cells are treated with CPT-11 (1-50 uM) for 0-24 hours. At designated time points, culture medium is collected and cells are lysed. RPR132595A concentration is determined using LC-MS/MS. The involvement of specific CYP isoforms is confirmed using selective inhibitors (e.g., ketoconazole for CYP3A4).
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| Animal Protocol |
Animal metabolism study protocol: Male Sprague-Dawley rats (or other relevant species) receive a single intravenous or oral dose of CPT-11 (5-20 mg/kg). Blood samples are collected at multiple time points (0, 0.5, 1, 2, 4, 8, 12, 24, 48 hours) via tail vein. Urine is collected over 0-24 hours and 24-48 hours intervals using metabolic cages. Plasma and urine samples are processed by protein precipitation and analyzed for RPR132595A concentration by LC-MS/MS to determine formation kinetics and cumulative urinary excretion.
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| ADME/Pharmacokinetics |
RPR132595A is produced via cytochrome P-450 3A4 (CYP3A4) metabolism of the parent drug CPT-11. The metabolite is ultimately eliminated from the body primarily through urinary excretion. As a hydrophilic metabolite, it shows favorable renal clearance properties. The half-life of RPR132595A in circulation is expected to correlate with the elimination kinetics of CPT-11 and its other metabolites.
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| Toxicity/Toxicokinetics |
Toxicity data for RPR132595A hydrochloride are limited as it is a research metabolite rather than a therapeutic agent. CPT-11 has known clinical toxicities including diarrhea (both early and late-onset) and myelosuppression (neutropenia and thrombocytopenia). However, the specific contribution of the RPR132595A metabolite to irinotecan-induced toxicities requires further investigation. As a research compound, RPR132595A hydrochloride is intended for laboratory use only.
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| References | |
| Additional Infomation |
RPR132595A (NPC) hydrochloride is an analytical reference standard for CPT-11 metabolite detection and quantification. It is a major metabolite of irinotecan generated via CYP3A4-mediated metabolism and plays a role in the drug"s disposition and clearance pathways. The compound has not been independently developed for clinical therapy but serves as a biomarker for CYP3A4 activity and drug-metabolizing enzyme studies. The free base form (CAS 185304-42-1) is also available for research purposes.
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| Molecular Formula |
C28H31CLN4O6
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| Molecular Weight |
555.02
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| Related CAS # |
RPR132595A;185304-42-1
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| Appearance |
Yellow to orange solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~50 mg/mL (~90.09 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.25 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 12.5 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. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.25 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 12.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8017 mL | 9.0087 mL | 18.0174 mL | |
| 5 mM | 0.3603 mL | 1.8017 mL | 3.6035 mL | |
| 10 mM | 0.1802 mL | 0.9009 mL | 1.8017 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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