Avanafil Research Grade Compound (PDE5 Inhibitor) Supplier — UPOR Biotech
Avanafil is a highly selective PDE5 inhibitor — a pyrimidine-carboxamide small molecule that potentiates cGMP signaling with IC50 5.2 nM and >121-fold selectivity over other PDE isozymes. A defining second-generation compound in erectile dysfunction and urology pharmacology research. Research Grade (RUO) reference standard — bulk supplier from UPOR Biotech.
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Avanafil (CAS 330784-47-9, C₂₃H₂₆ClN₇O₃, MW 483.95 g/mol) is a highly selective, orally available phosphodiesterase-5 (PDE5) inhibitor and a pyrimidine-carboxamide small molecule — a second-generation member of the PDE5-inhibitor class (referenced as Stendra/Spedra, framed here strictly as an RUO reference standard). As a single (S) enantiomer, avanafil inhibits PDE5 with an IC50 of 5.2 nM, preventing the hydrolysis of cGMP in corpus-cavernosum smooth muscle. By sustaining elevated intracellular cGMP, avanafil potentiates nitric-oxide (NO)-mediated smooth-muscle relaxation and supports the erectile response. Its defining pharmacological profile is >121-fold selectivity over other PDE isozymes — most notably sparing PDE6 (retinal) and PDE11 (testicular) — which underlies its differentiated off-target profile in reference literature. This high isozyme discrimination, combined with fast absorption kinetics, positions avanafil as a key comparator compound in PDE5-inhibitor pharmacology.
As a Research Grade (RUO) compound, UPOR Biotech’s avanafil is positioned for urology and cardiovascular pharmacology research — including ED mechanism studies, PDE isozyme selectivity assays, and cGMP/NO signaling research. Supplied as a ≥98% HPLC-pure reference standard with documented single-enantiomer stereochemistry, it supports analytical method development and preclinical study design where batch-to-batch consistency is critical. Research Use Only (RUO) — not for human diagnostic or therapeutic use. Every shipment is accompanied by COA, MSDS, HPLC chromatogram, and heavy-metals data, and manufacturing facilities hold ISO 9001, cGMP, and FDA facility registration. Available in 1/5/10/50 g packaging with a 3-year shelf life under refrigerated storage.
Avanafil vs Sildenafil — Second-Generation PDE5 Inhibitor
When comparing avanafil vs sildenafil, avanafil’s defining advantage in reference studies is faster onset of action combined with >121-fold PDE5 selectivity. Sildenafil’s therapeutic dose shows measurable PDE6 cross-reactivity, which is associated with transient visual side effects (cyanopsia); avanafil’s high PDE5/PDE6 discrimination markedly reduces this in comparative assays. This isozyme-selectivity profile — together with rapid absorption and a shorter half-life — makes avanafil a key differentiator in PDE5-inhibitor research and a preferred comparator for onset-kinetics and selectivity studies. Both compounds potentiate PDE5-mediated cGMP signaling, but avanafil’s selectivity margin and onset profile define the second-generation distinction.
Technical Specifications
| Property | Specification |
|---|---|
| Product Name | Avanafil — Research Grade (RUO) — PDE5 Inhibitor Reference Compound |
| Synonyms | Avanafil; TA-1790 |
| CAS Number | 330784-47-9 |
| Molecular Formula | C₂₃H₂₆ClN₇O₃ |
| Molecular Weight | 483.95 g/mol |
| IUPAC Name | 4-[[(3-Chloro-4-methoxyphenyl)methyl]amino]-2-[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl)-5-pyrimidinecarboxamide |
| Compound Class | Small-molecule PDE5 inhibitor (pyrimidine-carboxamide) |
| Stereochemistry | Single (S) enantiomer |
| Mechanism of Action | Selective PDE5 inhibition (IC50 5.2 nM) — prevents cGMP hydrolysis in corpus-cavernosum smooth muscle |
| Isozyme Selectivity | >121-fold over other PDE isozymes; spares PDE6 and PDE11 |
| Purity (HPLC) | ≥98.0% (area normalization) |
| Related Substances | ≤2.0% total impurities |
| Appearance | White to off-white solid |
| Melting Point | ~130–132°C |
| Solubility | DMSO ≥50 mg/mL; sparingly soluble in aqueous buffers |
| Optical Rotation | Consistent with single (S) enantiomer reference standard |
| Water Content (KF) | ≤0.5% |
| Residual Solvents | Meets ICH Q3C limits |
| Heavy Metals (Total) | ≤10 ppm |
| Grade | Research Grade (RUO) |
| Applications | ED pharmacology, PDE isozyme selectivity, cGMP/NO signaling, analytical reference standard |
| Certifications | ISO 9001, cGMP, FDA facility registration |
| Packaging | 1 g / 5 g / 10 g / 50 g sealed vials |
| Storage | 2–8°C, protected from light and moisture |
| Shipping | Ambient with desiccant; 2–8°C cold chain available |
| Shelf Life | 3 years |
| Disclaimer | Research Use Only (RUO) — not for human diagnostic or therapeutic use |
Key Benefits — Avanafil Research Grade
Highly Selective PDE5 Inhibition — IC50 5.2 nM
Avanafil inhibits PDE5 at an IC50 of 5.2 nM, selectively preventing cGMP hydrolysis and potentiating NO-mediated relaxation. Its high-affinity, selective blockade makes it a potent, well-characterized reference compound for PDE5 mechanism-of-action studies.
IC50 5.2 nM>121-Fold PDE Isoform Selectivity
Avanafil discriminates PDE5 from other PDE isozymes by >121-fold, sparing PDE6 (retinal) and PDE11 (testicular). This selectivity margin reduces off-target effects and makes avanafil a clean comparator for isozyme-specificity research.
>121-Fold SelectiveFast-Onset cGMP Potentiation Profile
Rapid absorption with a short Tmax delivers a fast-onset cGMP potentiation profile. This second-generation kinetic characteristic is central to onset-kinetics and dose-timing studies in urology pharmacology.
Fast Onset≥98% HPLC Purity Reference Standard
Supplied at ≥98% HPLC purity as a documented single (S) enantiomer, with COA, MSDS, HPLC chromatogram, and heavy-metals data. A reliable analytical reference standard for method development and QC across research batches.
Reference StandardApplications
Erectile Dysfunction (ED) Pharmacology Research
Avanafil supports ED mechanism studies — PDE5 inhibition, corpus-cavernosum relaxation, and erectile response models. A key RUO reference compound for second-generation PDE5-inhibitor pharmacology.
PDE Isozyme Selectivity Assays
Its >121-fold PDE5 selectivity makes avanafil a clean tool for isozyme-discrimination assays, comparing PDE5 affinity against PDE6, PDE11, and other family members.
cGMP/NO Signaling Pathway Studies
Avanafil potentiates the NO–cGMP signaling axis by blocking cGMP hydrolysis, supporting studies of nitric-oxide-mediated relaxation and intracellular second-messenger dynamics.
Corpus Cavernosum Tissue Models
Ex-vivo smooth-muscle strips and tissue bath models use avanafil to characterize NO-mediated relaxation kinetics and functional erectile response in isolated preparations.
Urology & Cardiovascular Pharmacology
Research extends into pulmonary and cardiovascular pharmacology, where PDE5 inhibition and cGMP potentiation are investigated across vascular smooth-muscle systems.
Analytical Reference Standard & Method Development
At ≥98% HPLC purity, avanafil serves as a calibration standard for HPLC/LC-MS method development, impurity profiling, and stability-indicating assay validation.
Frequently Asked Questions
Avanafil (CAS 330784-47-9) is a highly selective, orally available PDE5 inhibitor — a pyrimidine-carboxamide small molecule (referenced as Stendra/Spedra, framed here strictly as an RUO reference standard). It works by selectively inhibiting phosphodiesterase-5 at an IC50 of 5.2 nM, preventing the breakdown of cGMP in corpus-cavernosum smooth muscle. This potentiates nitric-oxide (NO)-mediated relaxation and supports the erectile response. Its >121-fold selectivity over other PDE isozymes minimizes off-target activity in reference studies.
Avanafil is a second-generation PDE5 inhibitor with several reference-study differentiators versus sildenafil: faster onset of action (rapid absorption, shorter Tmax), >121-fold PDE5 selectivity, and markedly less PDE6 cross-reactivity. PDE6 inhibition is associated with sildenafil’s transient visual side effects (cyanopsia); avanafil’s high PDE5/PDE6 discrimination substantially reduces this in comparative assays. This makes avanafil a preferred comparator in PDE5-inhibitor selectivity and onset-kinetics research.
Avanafil is used in erectile dysfunction (ED) pharmacology research, PDE isozyme selectivity assays, cGMP/NO signaling pathway studies, corpus cavernosum tissue models, and urology and cardiovascular pharmacology. As a ≥98% HPLC reference standard with documented single-enantiomer stereochemistry, it also supports analytical method development and QC. Strictly Research Use Only (RUO) — not for human diagnostic or therapeutic use.
Store at 2–8°C, protected from light and moisture. Prepare DMSO stock solutions (DMSO solubility ≥50 mg/mL) for assay work and avoid repeated freeze-thaw cycles of diluted stocks. Handle with standard laboratory PPE under a fume hood where appropriate. Every lot ships with COA, MSDS, and stability data for the intended RUO research application.
Every shipment includes COA (HPLC purity ≥98.0%, related substances, heavy metals ≤10 ppm), MSDS, HPLC chromatogram, stability data, and complete lot traceability. Manufacturing facilities hold ISO 9001, cGMP, and FDA facility registration. Avanafil is supplied as Research Grade (RUO) — not for human diagnostic or therapeutic use — in 1/5/10/50 g packaging.