Tadalafil (CAS No.: 171596-29-5) - Long-Acting PDE5 Inhibitor for Erectile Dysfunction & Pulmonary Arterial Hypertension
As a professional supplier of pharmaceutical-grade active pharmaceutical ingredients (APIs), we provide high-purity Tadalafil that strictly complies with global pharmacopoeia standards (USP, EP, BP, CP). A selective and long-acting phosphodiesterase type 5 (PDE5) inhibitor, it is clinically approved for treating erectile dysfunction (ED), benign prostatic hyperplasia (BPH), and pulmonary arterial hypertension (PAH). Its unique pharmacokinetic profile-with a half-life of ~17.5 hours-enables flexible dosing (on-demand or daily low-dose) and extended therapeutic effects, making it a preferred choice in men's health and cardiovascular care.
Product Basic Information
| Item | Details |
|---|---|
| Product Name | Tadalafil |
| CAS No. | 171596-29-5 |
| Synonyms | (6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione; Cialis® (brand name for ED/BPH formulations); Adcirca® (brand name for PAH formulations) |
| Molecular Formula | C₂₂H₁₉N₃O₄ |
| Molecular Weight | 389.40 |
| Appearance | White to off-white crystalline powder; Odorless |
| Specification | - Pharmaceutical Grade: Purity ≥99.0% (HPLC); Assay 98.0%–102.0% (anhydrous basis); Loss on drying ≤0.5%; Residue on ignition ≤0.1%; Heavy metals (Pb≤1ppm, Hg≤0.1ppm, Cd≤0.1ppm); Residual solvents (methanol ≤300ppm, acetonitrile ≤410ppm, ethyl acetate ≤500ppm); Optical purity (ee) ≥99.5% |
| Melting Point | 302–305°C (with decomposition) |
| Solubility | Practically insoluble in water (≈0.02 mg/mL at 25°C); Slightly soluble in ethanol (≈0.8 mg/mL) and methanol; Soluble in dimethyl sulfoxide (DMSO) and dilute acids (e.g., 0.1M HCl) |
| Storage Conditions | Store in a cool (2–8°C), dry, light-protected container; Sealed under nitrogen to prevent oxidation and moisture absorption; Avoid contact with strong acids/bases and oxidizing agents; Shelf life: 36 months for pharmaceutical grade |
Core Functions & Mechanism of Action
Tadalafil exerts its therapeutic effects by selectively inhibiting PDE5-an enzyme that breaks down cyclic guanosine monophosphate (cGMP), a key signaling molecule in smooth muscle relaxation:
1. For Erectile Dysfunction (ED)
Physiological Trigger: Sexual stimulation causes the release of nitric oxide (NO) in the corpus cavernosum of the penis.
cGMP Accumulation: NO activates guanylate cyclase, which increases cGMP production. Tadalafil inhibits PDE5, preventing cGMP degradation and allowing its levels to rise.
Smooth Muscle Relaxation: Elevated cGMP relaxes the smooth muscles of penile blood vessels, increasing blood flow into the corpus cavernosum-resulting in an erection.
Key Advantage: Unlike shorter-acting PDE5 inhibitors (e.g., sildenafil), CAS#171596-29-5 long half-life allows for erections to occur spontaneously within 24–36 hours of dosing (no need for precise timing relative to sexual activity).
2. For Benign Prostatic Hyperplasia (BPH)
Pathology Link: BPH involves enlarged prostate tissue compressing the urethra, causing urinary symptoms (e.g., frequent urination, weak stream). PDE5 is also expressed in the prostate and bladder neck smooth muscle.
Relaxation Effect: is inhibits PDE5 in the prostate and bladder, relaxing smooth muscle, reducing urethral obstruction, and improving urinary flow. It is often used in patients with both ED and BPH (dual indication).
Core Applications (Pharmaceutical Field)
Tadalafil CAS#171596-29-5 is administered orally (tablets, orally disintegrating tablets) and is strictly prescription-only due to potential cardiovascular risks. Dosing varies by indication:
1. Erectile Dysfunction (ED)
On-Demand Dosing: 10 mg taken at least 30 minutes before sexual activity; may be adjusted to 5 mg (for mild ED or elderly patients) or 20 mg (for severe ED), with a maximum frequency of once daily.
Daily Low-Dose Dosing: 2.5 mg or 5 mg taken once daily (regardless of sexual activity), ideal for patients seeking spontaneous sexual function or those with BPH comorbidity.
2. Benign Prostatic Hyperplasia (BPH)
Monotherapy: 5 mg once daily (improves urinary symptoms within 1–2 weeks).
Combination Therapy: 5 mg once daily with alpha-blockers (e.g., tamsulosin) for severe BPH (avoids additive hypotension due to is minimal effect on blood pressure at low doses).
3. Pulmonary Arterial Hypertension (PAH)
Branded Formulation (Adcirca®): 40 mg once daily (higher dose than ED/BPH, as PAH requires greater PDE5 inhibition in pulmonary vasculature).
Indication: Approved for PAH (WHO Group 1) to improve exercise capacity and delay clinical worsening.
Quality & Safety Assurance
As a critical prescription API, CAS#171596-29-5 requires rigorous quality control to ensure purity, potency, and safety-especially given its potential for drug interactions and cardiovascular side effects:
1. Manufacturing & Purity Control
Synthesis: Produced via multi-step chemical synthesis (starting from 1,3-benzodioxole derivatives), with key steps including cyclization, chiral resolution (to ensure optical purity), and crystallization. The process ensures:
Minimal impurities (e.g., synthetic intermediates, degradation products) ≤0.1% (single impurity) and ≤0.5% (total impurities);
High optical purity (ee ≥99.5%), as the (R,R)-enantiomer is the active form (other enantiomers have no PDE5 inhibitory activity).
GMP Compliance: Manufactured in Grade B/C cleanrooms (per ICH Q7 guidelines) with strict environmental monitoring (airborne particles, microbial counts) to prevent contamination.
2. Comprehensive Testing Protocol
| Test Item | Method | Acceptance Criterion |
|---|---|---|
| Purity & Assay | HPLC (C18 column, 230 nm detection) | Purity ≥99.0%; Assay 98.0%–102.0% |
| Optical Purity | Chiral HPLC (cellulose-based column) | Enantiomeric excess (ee) ≥99.5% |
| Related Substances | HPLC (gradient elution) | Single impurity ≤0.1%; Total impurities ≤0.5% |
| Heavy Metals | ICP-MS (Inductively Coupled Plasma-Mass Spectrometry) | Pb≤1ppm, Hg≤0.1ppm, Cd≤0.1ppm |
| Residual Solvents | GC (headspace sampling, FID detector) | Class 2 solvents ≤500ppm; Class 1 solvents not detected |
| Loss on Drying | Gravimetric method (105°C for 2 hours) | ≤0.5% |
| Residue on Ignition | Ashing at 600°C | ≤0.1% |
3. Safety Reminders
Contraindications:
Hypersensitivity to Tadalafil or PDE5 inhibitors.
Concurrent use of nitrates (e.g., nitroglycerin, isosorbide dinitrate)-risk of life-threatening hypotension.
Severe cardiovascular disease (e.g., recent myocardial infarction/stroke, unstable angina, uncontrolled hypertension).
Severe hepatic impairment (Child-Pugh Class C) or end-stage renal disease (ESRD, CrCl <30 mL/min).
Adverse Effects:
Common (mild, transient): Headache, dyspepsia (heartburn), back pain, muscle aches, and flushing.
Rare but serious: Priapism (erection lasting >4 hours-requires emergency treatment to avoid tissue damage), sudden vision loss (non-arteritic anterior ischemic optic neuropathy, NAION), or sudden hearing loss.
Cooperation & Contact
We supply pharmaceutical-grade Tadalafil in forms tailored to drug formulation:
Pharmaceutical Grade: Fine powder (1kg–100kg per order, double-layered aluminum foil bags with desiccants, packed in sealed fiber drums) for tablet, capsule, or orally disintegrating tablet (ODT) production.
Value-added services include:
Providing DMF (Drug Master File) (Type II) and CEP (Certificate of Suitability) to support regulatory filings (ANDA, NDA, MAA) in global markets (U.S., EU, APAC).
Supplying batch-specific COA (Certificate of Analysis) with full testing results (purity, optical purity, impurities) for compliance.
Technical support for formulation development (e.g., solubility enhancement for oral dosage forms, stability testing protocols).
If you are a pharmaceutical manufacturer, generic drug company, or contract development and manufacturing organization (CDMO), please contact us for detailed cooperation:
Contact Information:
Email: sales@huarongpharma.com
Phone/WhatsApp: +86 13751168070
We adhere to the principles of "prescription-grade quality, regulatory compliance, and patient safety" and look forward to partnering with global pharmaceutical industries in men's health and cardiovascular care!
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