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| Targets |
This compound does not have a specific protein target; it is a synthetic phospholipid that interacts with cell membranes and endosomal bilayers, promoting membrane destabilization and nucleic acid release into the cytoplasm.
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| ln Vitro |
In cell‑free assays, 9A1P9 shows higher membrane‑disruptive activity at acidic pH (pH 5.5) compared to neutral pH (pH 7.4). This property is characteristic of ionizable lipids that are neutral at physiological pH but become positively charged in the acidic endosomal environment, facilitating endosomal escape and release of nucleic acid payloads into the cytoplasm.
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| ln Vivo |
9A1P9 can efficiently deliver mRNA in mice when formulated into lipid nanoparticles. It has been used for organ‑selective mRNA delivery to the spleen and liver and for CRISPR‑Cas9 gene editing, demonstrating its utility as a delivery vehicle for nucleic acid‑based therapeutics.
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| Enzyme Assay |
A general cell‑free protocol for assessing pH‑dependent membrane destabilization: Large unilamellar vesicles (LUVs) composed of phosphatidylcholine (PC) and phosphatidylserine (PS) (1:1 molar ratio) are prepared by extrusion. The LUVs are loaded with a self‑quenching concentration of a fluorescent dye (e.g., calcein, 50 mM) and then the extraliposomal dye is removed by gel filtration. 9A1P9 (0.1‑100 ug/mL) is added to the LUVs at pH 7.4 and pH 5.5, and the increase in fluorescence due to dye release (dequenching) is monitored over 30 minutes. The percentage of membrane destabilization is calculated relative to complete lysis with 1% Triton X‑100.
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| Cell Assay |
A general cellular protocol for assessing nucleic acid delivery using 9A1P9: HEK293T or HeLa cells are seeded in 24‑well plates at 1×10⁵ cells/well. 9A1P9 is used to formulate lipid nanoparticles (LNPs) containing mRNA encoding firefly luciferase or EGFP (enhanced green fluorescent protein). LNPs are prepared by mixing 9A1P9 with helper lipids (e.g., DOPE, cholesterol, DMG‑PEG2000) and mRNA at an appropriate molar ratio (e.g., 9A1P9:DOPE:cholesterol:DMG‑PEG2000 = 25:30:30:1). The LNPs are added to the cells at concentrations of 0.1‑10 ug/mL mRNA equivalent. After 24‑48 hours, transfection efficiency is measured by luciferase assay (luminometer) or by flow cytometry for EGFP expression. Cytotoxicity is assessed by MTT assay.
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| Animal Protocol |
A general animal protocol for 9A1P9‑mediated mRNA delivery: Male C57BL/6J mice (6‑8 weeks old) are injected intravenously (tail vein) with 9A1P9‑formulated LNPs containing 0.1‑1 mg/kg mRNA encoding firefly luciferase or a reporter protein. At 4‑24 hours post‑injection, mice are imaged for luciferase expression using an IVIS imaging system after intraperitoneal injection of D‑luciferin (150 mg/kg). Tissues (liver, spleen, lung, kidney, heart) are harvested for ex vivo bioluminescence imaging and for analysis of protein expression by Western blot or ELISA. For CRISPR‑Cas9 gene editing, LNPs are co‑formulated with Cas9 mRNA and a single guide RNA (sgRNA) targeting a specific gene (e.g., PCSK9), and editing efficiency is assessed by T7E1 assay or by DNA sequencing of the target locus.
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| ADME/Pharmacokinetics |
General PK protocol for 9A1P9 in LNPs is not applicable; the PK of encapsulated mRNA is typically measured. For 9A1P9 itself, it is a lipid component of the LNP and is expected to be rapidly cleared from plasma and distributed to the liver (the primary site of LNP accumulation). Blood samples are collected after IV injection of LNPs, and 9A1P9 concentrations are quantified by LC‑MS/MS. The terminal half‑life is short (minutes to hours).
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| Toxicity/Toxicokinetics |
General toxicity protocol for 9A1P9 LNPs: A single‑dose toxicity study is performed in ICR mice. 9A1P9‑formulated LNPs are administered intravenously at doses of 0.5, 1, and 5 mg/kg (mRNA dose equivalent). Blood samples are collected 6 and 24 hours post‑injection for serum chemistry (ALT, AST, BUN, creatinine) and cytokine analysis (IL‑6, TNF‑alpha, IFN‑gamma) by ELISA. Animals are observed for 14 days for clinical signs and mortality. At the end of the study, gross necropsy and histopathology of the liver, spleen, lungs, and kidneys are performed.
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| References | |
| Additional Infomation |
9A1P9 has the molecular formula C2₇H₅₈NO4P and a molecular weight of 491.73 g/mol. The compound induces membrane destabilization and has been used for organ‑selective mRNA delivery to the spleen and liver and for CRISPR‑Cas9 gene editing in mice. It is a research tool for developing nucleic acid‑based therapeutics and gene editing technologies. The mechanism involves ionizable lipid properties that enable endosomal escape at acidic pH. The compound is typically stored as a solution in ethanol (20.34 mM) or as a powder at ‑20degC.
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| Molecular Formula |
C27H58NO4P
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| Molecular Weight |
491.73
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| CAS # |
2760467-57-8
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| Appearance |
Colorless to light yellow liquid
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| Density |
0.953±0.06 g/cm3(Predicted)
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| Boiling Point |
554.8±52.0 °C(Predicted)
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| LogP |
0
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0336 mL | 10.1682 mL | 20.3364 mL | |
| 5 mM | 0.4067 mL | 2.0336 mL | 4.0673 mL | |
| 10 mM | 0.2034 mL | 1.0168 mL | 2.0336 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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