Ezetimibe Research Grade Compound (NPC1L1 Inhibitor) Supplier — UPOR Biotech
Ezetimibe (SCH 58235) is a potent, selective inhibitor of intestinal cholesterol absorption — a small-molecule azetidinone (β-lactam) that binds the NPC1L1 sterol transporter at the enterocyte brush border, blocking cholesterol and phytosterol uptake without inhibiting hepatic cholesterol synthesis. Research Grade (RUO) reference standard (CAS 163222-33-1, C₂₄H₂₁F₂NO₃, MW 409.43 g/mol) for hypercholesterolemia and lipid-lowering pharmacology research, supplied with COA, HPLC, and heavy-metal documentation. ISO 9001, cGMP, and FDA facility registration. Bulk supplier of research-grade ezetimibe — premium NPC1L1 reference compound from UPOR Biotech.
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Ezetimibe (CAS 163222-33-1, C₂₄H₂₁F₂NO₃, MW 409.43 g/mol) is a potent, selective inhibitor of intestinal cholesterol absorption — an azetidinone (β-lactam) small molecule originally designated SCH 58235. Ezetimibe acts at the apical membrane of enterocytes, where it binds the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1) and blocks the intestinal uptake of cholesterol and phytosterols, reducing the delivery of dietary cholesterol to the liver. Because its action is localized to the intestinal brush border, ezetimibe does not inhibit hepatic cholesterol synthesis (unlike statins) and does not increase bile-acid excretion — a mechanism that distinguishes it from every other lipid-lowering drug class. UPOR Biotech supplies ezetimibe as a single (3R,4S) stereoisomer with a controlled impurity profile, characterized by HPLC and released at ≥98.0% purity for research use.
As a research-grade compound, UPOR Biotech’s ezetimibe is positioned for cholesterol and lipid pharmacology research: hypercholesterolemia and LDL-C models, NPC1L1-mediated sterol-transport studies, and statin-combination (ezetimibe + statin) lipid-lowering protocols. Each lot is supplied with COA, MSDS, HPLC analysis, and heavy-metal data, and production follows ISO 9001, cGMP, and FDA facility registration standards. Packaging is available in 1 g, 5 g, 10 g, and 50 g units. Research Use Only (RUO) — not for human diagnostic or therapeutic use.
Ezetimibe vs Statins — Absorption Inhibitor vs Synthesis Inhibitor
Ezetimibe and statins lower cholesterol through complementary mechanisms. Ezetimibe is a cholesterol absorption inhibitor — it blocks intestinal cholesterol absorption by binding the NPC1L1 transporter at the enterocyte brush border, reducing the delivery of dietary cholesterol to the liver. Statins are cholesterol synthesis inhibitors — they inhibit hepatic HMG-CoA reductase, the rate-limiting enzyme of endogenous cholesterol synthesis. Because the two mechanisms target different sides of cholesterol balance — dietary intake versus de novo synthesis — they are frequently co-studied in lipid-lowering research, and the combination mirrors the rationale for combined absorption- and synthesis-inhibitor therapy.
Technical Specifications
| Property | Specification |
|---|---|
| Product Name | Ezetimibe (SCH 58235) — Research Grade Reference Standard |
| Synonyms | Ezetimibe; SCH 58235 |
| CAS Number | 163222-33-1 |
| Molecular Formula | C₂₄H₂₁F₂NO₃ |
| Molecular Weight | 409.43 g/mol |
| IUPAC Name | (3R,4S)-1-(4-Fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one |
| Compound Class | Azetidinone (β-lactam) small-molecule NPC1L1 inhibitor |
| Biological Target | NPC1L1 (Niemann-Pick C1-Like 1) intestinal sterol transporter |
| Stereochemistry | Single stereoisomer; (3R,4S) absolute configuration |
| Mechanism | Selective inhibition of intestinal cholesterol and phytosterol absorption via NPC1L1 binding at the enterocyte brush border |
| Purity (HPLC) | ≥98.0% |
| Appearance | White to off-white crystalline solid |
| Melting Point | ~163–166°C |
| Optical Rotation | Single stereoisomer; consistent optical profile per lot |
| Solubility | DMSO ≥50 mg/mL |
| Heavy Metals | ≤10 ppm |
| Water Content | ≤1.0% |
| Related Substances | Controlled impurity profile by HPLC |
| Grade | Research Grade (RUO) |
| Applications | Hypercholesterolemia/lipid-lowering research; NPC1L1 sterol-transport studies; statin-combination lipid pharmacology; analytical reference standard |
| Certifications | ISO 9001, cGMP, FDA facility registration |
| Packaging | 1 / 5 / 10 / 50 g |
| Storage | 2–8°C, protected from light and moisture |
| Shelf Life | 3 years |
| Disclaimer | Research Use Only (RUO) — not for human diagnostic or therapeutic use |
Key Benefits — Ezetimibe Research Grade
Selective NPC1L1 Cholesterol-Absorption Inhibition
Ezetimibe is a potent, selective inhibitor of NPC1L1 — the sterol transporter responsible for intestinal cholesterol and phytosterol uptake. By binding NPC1L1 at the enterocyte apical membrane, it blocks cholesterol absorption at its source, providing a mechanistically distinct route to LDL-C lowering in research models.
Selective NPC1L1Intestinal Brush-Border Local Action
Ezetimibe acts locally in the intestinal brush border without systemic inhibition of hepatic cholesterol synthesis or increased bile-acid excretion. This intestinal-sparing profile makes ezetimibe a clean, mechanistically isolated tool for studying cholesterol absorption independent of hepatic pathways.
Local ActionComplementary to Statin Synthesis Inhibition
Because ezetimibe blocks cholesterol absorption while statins inhibit hepatic cholesterol synthesis, the two mechanisms are complementary. Co-administration studies enable research into combined absorption- plus synthesis-inhibitor lipid-lowering pharmacology and its effect on LDL-C.
Statin-Complementary≥98% HPLC Purity Reference Standard
Supplied as a reference-standard grade small molecule with ≥98.0% purity by HPLC, defined (3R,4S) stereochemistry, and a controlled impurity profile. Each lot ships with full analytical documentation — COA, HPLC, MSDS, and heavy-metal data — for reproducible research.
Reference StandardApplications
Hypercholesterolemia & LDL-C Research
Study ezetimibe’s cholesterol-absorption-inhibition mechanism in cell, animal, and experimental models of hypercholesterolemia. Ezetimibe is a reference tool for evaluating LDL-C lowering via reduced intestinal cholesterol delivery.
NPC1L1 Sterol-Transport Studies
Use ezetimibe to probe NPC1L1-mediated cholesterol and phytosterol transport in Caco-2, HepG2, and knockout models — defining the molecular pharmacology of the intestinal sterol transporter.
Statin-Combination Lipid Pharmacology
Evaluate ezetimibe + statin combinations to study complementary absorption- and synthesis-inhibition pathways, mirroring the rationale of combination lipid-lowering therapy in research protocols.
Cholesterol Metabolism & Bile-Acid Research
Investigate whole-body cholesterol balance — dietary absorption, hepatic synthesis, and bile-acid economy — using ezetimibe to isolate the intestinal absorption arm of cholesterol metabolism.
Atherosclerosis Model Development
Deploy ezetimibe in hypercholesterolemic and atherosclerotic model systems to modulate dietary cholesterol input and characterize plaque progression and lipid-lowering interventions.
Analytical Reference Standard & Method Development
Employ ezetimibe as an analytical reference standard for HPLC, LC-MS, and assay method development and validation — with COA, HPLC, and heavy-metal documentation for traceability.
Frequently Asked Questions
Ezetimibe (SCH 58235) is a selective NPC1L1 cholesterol absorption inhibitor — an azetidinone (β-lactam) small molecule. It binds the Niemann-Pick C1-Like 1 (NPC1L1) sterol transporter on the apical membrane of enterocytes, blocking intestinal absorption of cholesterol and phytosterols and reducing the delivery of dietary cholesterol to the liver. Because it acts locally at the intestinal brush border, it does not inhibit hepatic cholesterol synthesis or increase bile-acid excretion. UPOR Biotech supplies ezetimibe at ≥98% HPLC purity as a single (3R,4S) stereoisomer for research use only.
Ezetimibe and statins lower cholesterol through different mechanisms. Ezetimibe is a cholesterol absorption inhibitor — it blocks intestinal cholesterol uptake by binding NPC1L1 at the enterocyte brush border. Statins are cholesterol synthesis inhibitors — they inhibit hepatic HMG-CoA reductase, the rate-limiting enzyme of endogenous cholesterol synthesis. The two mechanisms are complementary and are frequently co-studied in lipid-lowering research, reflecting the rationale for combined absorption- and synthesis-inhibitor therapy.
Ezetimibe is used in hypercholesterolemia and LDL-C research, NPC1L1-mediated sterol-transport studies, and statin-combination lipid pharmacology (ezetimibe + statin protocols). Additional applications include cholesterol metabolism and bile-acid balance research, atherosclerosis model development, and use as an analytical reference standard for HPLC and LC-MS method development. All supplied material is Research Grade (RUO).
Store ezetimibe at 2–8°C, protected from light and moisture, in the original sealed container. For assay work, prepare stock solutions in DMSO (≥50 mg/mL), aliquot to avoid repeated freeze-thaw cycles, and keep stock solutions protected from light. Handle with standard laboratory precautions per the MSDS. Under these conditions, shelf life is 3 years from the date of analysis.
Every shipment includes: COA (HPLC ≥98.0% purity, impurity profile, heavy metals ≤10 ppm), MSDS, HPLC Analysis, Heavy-Metal Data, and Lot Traceability. Production follows ISO 9001, cGMP, and FDA facility registration standards. Ezetimibe is supplied as Research Grade (RUO) — Research Use Only, not for human diagnostic or therapeutic use.