Triptorelin Acetate 2mg/Vial – Pharmaceutical Grade GnRH Analog Peptide
Brand: ACDC | CAS No.: 140194-24-7 | Purity: ≥99%
Triptorelin Acetate is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH, also referred to as luteinizing hormone-releasing hormone, LHRH), formulated as an acetate salt to boost water solubility and chemical stability. A potent, long-acting GnRH agonist, it is a staple in clinical practice for managing hormone-dependent diseases and a critical research tool in reproductive medicine. Its free base has a molecular weight of approximately 1311.5 Da, with the amino acid sequence pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH₂—featuring a pyroglutamic acid N-terminus and amidated glycine C-terminus. The substitution of L-tryptophan with D-tryptophan at position 6 is a key structural modification, drastically enhancing enzymatic degradation resistance and GnRH receptor binding affinity, and extending its in vivo half-life compared to endogenous GnRH.
Core Product Characteristics
Form & Appearance
Supplied as a sterile filtered white lyophilized (freeze-dried) powder in 2mg/vial packaging (10 vials/box), designed for subcutaneous or intramuscular administration upon reconstitution. Long-acting depot formulations (e.g., microsphere-encapsulated preparations) are also a clinical standard for less frequent dosing.
Solubility Guidelines
Reconstitute the lyophilized powder in sterile 18M-cm H₂O at a minimum concentration of 100 ug/ml; the stock solution can then be further diluted into other aqueous solutions for research or clinical use. Prepare fresh solutions immediately before administration for optimal stability and efficacy.
Purity & Quality Assurance
ACDC Triptorelin Acetate meets a pharmaceutical grade purity standard of ≥99%, verified through two gold-standard analytical methods:
Reverse-Phase High-Performance Liquid Chromatography (RP-HPLC)
Sodium Dodecyl Sulfate-Polyacrylamide Gel Electrophoresis (SDS-PAGE)
Storage & Stability Protocols
Proper storage is critical to preserving peptide integrity—follow these guidelines for maximum stability:
Lyophilized powder (unreconstituted): Stable at room temperature for 3 weeks; for long-term storage, keep desiccated at below -18°C away from light. Avoid repeated freeze-thaw cycles at all times.
Reconstituted solution: Store at 4°C for 2–7 days for immediate use; for future use, freeze at below -18°C and add a carrier protein (0.1% HSA or BSA) to extend shelf life.
Short-term clinical storage (non-lyophilized formulations): 2–8°C, protected from light.
Mechanism of Action
Triptorelin Acetate exerts its biological effects via a biphasic interaction with GnRH receptors on pituitary gonadotroph cells, driving the hormone-modulating activity that underpins its clinical and research use:
Initial Stimulatory Phase (1–2 weeks post-administration): Binds to GnRH receptors to stimulate pituitary secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), causing a temporary rise in serum testosterone (males) and estrogen (females) levels.
Sustained Desensitization Phase (prolonged exposure): Continuous agonist binding leads to GnRH receptor downregulation and desensitization, resulting in a significant reduction in LH and FSH secretion. This subsequent suppression of gonadal steroid hormone synthesis creates a state of “medical castration”—the primary mechanism for its therapeutic applications in hormone-dependent conditions.
Key Clinical Applications & Research Value
As a highly effective GnRH analog, Triptorelin Acetate has broad utility in clinical care and endocrinology/reproductive medicine research, with established use in the following areas:
Hormone-Dependent Cancers
Prostate Cancer: First-line treatment for advanced disease; lowers testosterone to castration-resistant levels to inhibit tumor growth.
Breast Cancer: Used for estrogen receptor-positive metastatic breast cancer in premenopausal women.
Gynecological Malignancies: Indicated for endometrial and ovarian cancers sensitive to hormone suppression.
Benign Gynecological Disorders
Endometriosis: Relieves pelvic pain and dysmenorrhea, and reduces the size of endometrial lesions by suppressing estrogen production.
Uterine Fibroids: Shrinks fibroid volume and reduces abnormal uterine bleeding; often used as preoperative preparation to minimize surgical trauma.
Reproductive Medicine & Pediatric Care
Assisted Reproductive Technology (ART): Regulates follicular development and controls ovulation timing in ovarian hyperstimulation protocols.
Central Precocious Puberty (CPP): Inhibits premature activation of the hypothalamic-pituitary-gonadal (HPG) axis, delaying puberty progression and improving final adult height in affected children.
Research Applications
A vital tool in endocrinology research for studying HPG axis function; also used to develop next-generation GnRH analogs with improved pharmacokinetic properties (e.g., longer half-lives, enhanced receptor affinity).
Dosage & Administration (Clinical Reference)
Dosing is tailored to the specific condition, with both daily subcutaneous and long-acting intramuscular depot formulations available (clinical reference only—adjust for research use as needed):
Advanced Prostate Cancer: 3.75 mg intramuscular (long-acting depot) every 4 weeks, or 0.1 mg subcutaneous daily.
Endometriosis/Uterine Fibroids: 3.75 mg intramuscular (long-acting depot) every 4 weeks for 3–6 months.
Central Precocious Puberty: Weight-adjusted dose, typically 0.1–0.3 mg subcutaneous every 4 weeks.
Triptorelin Acetate injection (extended-release suspension) is administered by a healthcare provider in a clinical setting; dosage frequency is determined by the treating physician, with close monitoring for hormone level changes during the initial stimulatory phase.
Safety Profile (Clinical Reference)
Common Adverse Reactions
Initial Flare Reaction: Transient worsening of tumor-related symptoms (e.g., prostate cancer bone pain) or menstrual irregularities in the first week; mitigated by concurrent antiandrogen/antiestrogen use.
Hypogonadism-Related Symptoms: Hot flashes, decreased libido, erectile dysfunction (males), vaginal dryness (females), and bone loss (long-term use may require calcium/vitamin D supplementation).
Mild Local/Systemic Reactions: Injection-site pain/redness/itching, headache, fatigue, and gastrointestinal disturbances—most are self-limiting and resolve with continued use.
Contraindications & Precautions
Contraindicated in: Pregnant/lactating women, individuals with hypersensitivity to Triptorelin Acetate or its excipients, and patients with untreated hormone-independent tumors.
Use with caution in: Patients with osteoporosis, cardiovascular disease, liver/kidney dysfunction, long QT syndrome, diabetes, urinary obstruction, or a history of seizures/strokes/brain tumors.
Fertility Note: May impair fertility in males; not for use in women of childbearing potential unless strict contraception is in place, as it can cause fetal harm.
ACDC Product Advantages
Pharmaceutical Grade Purity: ≥99% purity verified by RP-HPLC and SDS-PAGE, ensuring consistent biological activity for clinical and research use.
Stable Formulation: Acetate salt form for enhanced water solubility and chemical stability; sterile lyophilized powder preserves integrity during storage and transit.
Standardized Packaging: 2mg/vial (10 vials/box) – a widely used clinical/research 规格，with secure, light-protected vials to prevent degradation.
Global Shipping Capability: Shipped from Guangzhou, China—with professional documentation for smooth customs clearance and compliant international transit.
Port of Shipment: Guangzhou, China | Place of Origin: China | MOQ: 1 Box (10 vials)