4A3-SC8 is a modular, ionizable cationic lipid (pKa ≈ 6.66) that functions as a degradable dendrimer. Structurally, it features a dendritic architecture with a central tertiary amine that is pH-responsive, protonated at endosomal pH to facilitate membrane disruption, while remaining neutral in the bloodstream to enhance circulation. The inclusion of hydrolytically degradable ester linkages in its structure and thioether bonds in its tails renders it biodegradable, improving its safety profile for in vivo use. This combination of structural features makes it a highly versatile and robust ionizable lipid for the formulation of LNPs.
4A3-SC8 is an extensively validated ionizable cationic lipid and dendrimer widely used for the systemic delivery of a broad range of nucleic acid cargos, including siRNA, mRNA, single-guide RNA (sgRNA), and single-stranded DNA (ssDNA). Due to its favorable pKa and degradable design, 4A3-SC8 demonstrates potent gene silencing activity. In vivo, LNPs formulated with 4A3-SC8 have shown efficient accumulation in the liver, enabling over 95% Factor VII knockdown in mice, and have been successfully applied in tumor imaging studies when co-encapsulated with a PEGylated BODIPY dye and an mRNA reporter. 4A3-SC8 has also been shown to enable small RNAs to extend survival in an aggressive liver cancer model.
Product Parameters
Parameter
Specification
Product Name
4A3-SC8
CAS Number
1857340-78-3
Molecular Formula
C₇₅H₁₃₉N₃O₁₆S₄
Molecular Weight
1467.18 g/mol
Appearance
Liquid
Purity (HPLC)
≥95%; ≥99% (Ultra-high purity)
pKa
9.329±0.50(predicted)
Solubility
≥40.1 mg/mL in DMSO; ≥43.2 mg/mL in EtOH; ≥33.5 mg/mL in H₂O
Why Cosperpharm? – Our Competitive Advantages
Advantage
Detail
Production Strength
GMP-certified campus spanning 100+ mu, 3 multi-purpose workshops, 6 D-grade clean zone production lines, and 150+ reactors (20L–5000L), supporting high/low temp, anaerobic & hydrogenation; kg to ton scale production.
Fast Delivery
R&D samples: one week; commercial orders: 1–2 months after payment. Express (DHL/FedEx) or air/sea freight available.
Global Partners
Trusted by 30+ pharmaceutical companies in USA, Europe, India, Brazil, and Southeast Asia; long-term cooperation with generic drug manufacturers, CROs, and impurity standard distributors.
Licensed Exporter
Valid drug import/export license — no compliance delays.
Dual Quality Grades
Both research/pharma grade(≥98%)and high-purity impurity grade(≥99%)available to meet diverse customer needs.
Product Advantages
1.Proven In Vivo Efficacy: LNPs containing 4A3-SC8 achieve >95% Factor VII knockdown in mice, demonstrating potent, clinically relevant gene silencing.
2.Multi-Cargo Versatility: Effectively encapsulates and delivers a wide array of nucleic acids including siRNA, mRNA, sgRNA, and ssDNA, making it a true multi-purpose tool for genetic medicine.
3.Optimized Ionizable pKa: With a pKa of 6.66, 4A3-SC8 remains neutral in the bloodstream (reducing toxicity and extending circulation) and becomes protonated in the acidic endosome, efficiently triggering membrane fusion and cytosolic release of its cargo.
4.Degradable Dendrimer Design: The modular, degradable structure of 4A3-SC8 allows for safe clearance after its delivery function is complete, reducing the risk of chronic toxicity and improving the therapeutic window.
5.Excellent Water Solubility: Uniquely, 4A3-SC8 exhibits high water solubility (≥33.5 mg/mL), a valuable property that simplifies formulation development and processing.
6. Therapeutic Applications: 4A3-SC8 has enabled small RNAs to extend survival in an aggressive liver cancer model and has been successfully used for tumor imaging.
FAQ
Q1: What is 4A3-SC8 used for?
A: 4A3-SC8 is an ionizable cationic lipid used to generate LNPs for the delivery of various nucleic acids, including siRNA, mRNA, and single-guide RNA, primarily for liver-targeted gene silencing and cancer research applications.
Q2: What is the pKa of 4A3-SC8 and why is it important?
A: The pKa of 4A3-SC8 is approximately 6.66. This value is critical because it allows the lipid to be neutrally charged at physiological pH (reducing toxicity and promoting circulation) but positively charged in the acidic endosome, facilitating membrane fusion and the release of the nucleic acid cargo into the cell‘s cytoplasm.
Contact Us
Sourcing a reliable ionizable lipid shouldn‘t slow your research down. Cosperpharm makes getting high-purity 4A3-SC8 simple and straightforward. Contact us today for pricing, a Certificate of Analysis, or to discuss your LNP formulation project. We‘re ready to support your next breakthrough.
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