(R)-DOTMA
(R)-DOTMA is a cationic lipid that can be used to construct lipid nanoparticles and lipoplexes. (R)-DOTMA binds nucleic acid molecules such as mRNA through electrostatic interactions, facilitating nucleic acid encapsulation and cellular delivery. (R)-DOTMA can form lipid systems with DOPE (HY-112005) or cholesterol (HY-N0322). (R)-DOTMA is applicable to mRNA delivery, vaccine development, cancer immunotherapy and gene editing research.
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- CAS 番号: 2101981-60-4
- 分子式: C42H84ClNO2
- 分子量:670.59
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
(R)-DOTMA (2.75-4.32 mM; charge ratios 1.3:2.0, 4.0:1.0; 1 h, overnight) positively charged (4.0:1.0) (R)-DOTMA/DOPE and (R)-DOTMA/cholesterol lipoplexes have mean zeta potentials of +9.5 mV and mean particle sizes of 284 nm and 337 nm, respectively, while negatively charged (1.3:2.0) formulations have negative zeta potentials and smaller mean particle sizes of 212 nm ((R)-DOTMA/DOPE) and 235 nm ((R)-DOTMA/cholesterol)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
(R)-DOTMA (20 µg mRNA; retro-orbital injection; single dose) efficiently delivers Cre mRNA activity to all lung lobes (proximal and distal airways) via cationic DOTMA/cholesterol lipoplexes in ROSA26 lacZ Cre reporter mice, while cationic DOTMA/DOPE lipoplexes only target proximal lung areas and pulmonary vessel cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:White NMRI mice[1]
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Dosage:20 µg mRNA (delivered in 200 µl isotonic lipoplex mixture); cationic DOTMA/DOPE (charge ratio 4.0:1.0); anionic DOTMA/DOPE (charge ratio 1.3:2.0); cationic DOTMA/cholesterol (charge ratio 4.0:1.0); anionic DOTMA/cholesterol (charge ratio 1.3:2.0)
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Administration:retro-orbital injection; single dose
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Result:Produced strong luciferase activity primarily in lungs with cationic formulations.
Produced strong luciferase activity primarily in spleen with anionic formulations.
Achieved highest luciferase expression in lungs with cationic DOTMA/cholesterol formulation.
Achieved highest luciferase expression in spleen with anionic DOTMA/DOPE formulation.
Showed no detectable luciferase activity in liver, except weak signal in heart with cationic DOTMA/cholesterol lipoplexes.
Accumulated predominantly in lungs, spleen, and liver, with no detectable levels in heart and kidneys via LC-MS analysis.
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Animal Model:ROSA26 lacZ Cre reporter mice (FVB.129S4(B6)-Gt(ROSA)26Sortm1Sor/J)[1]
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Dosage:20 µg mRNA (delivered in 200 µl isotonic lipoplex mixture); cationic DOTMA/DOPE (charge ratio 4.0:1.0); cationic DOTMA/cholesterol (charge ratio 4.0:1.0)
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Administration:retro-orbital injection; single dose
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Result:Targeted Cre mRNA activity to central areas of left, right cranial, middle, and caudal lung lobes, with no activity in right post caval lobe and no delivery to distal airways via cationic DOTMA/DOPE lipoplexes.
Delivered Cre mRNA activity only to proximal lung areas and pulmonary vessel cells via cationic DOTMA/DOPE lipoplexes.
Targeted all five lung lobes (both proximal and distal airways) with uniform staining of endothelial cells in small lung vessels via cationic DOTMA/cholesterol lipoplexes.
Showed no delivery of Cre mRNA activity to large airway cells with either formulation.
Showed no background X-Gal staining in control mice not injected with Cre mRNA.
化学情報
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CAS 番号 2101981-60-4
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分子量 670.59
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分子式 C42H84ClNO2
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SMILES
[C@@H](COCCCCCCCC/C=C\CCCCCCCC)(OCCCCCCCC/C=C\CCCCCCCC)C[N+](C)(C)C.[Cl-]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Rosigkeit S, et al. Monitoring Translation Activity of mRNA-Loaded Nanoparticles in Mice. Molecular pharmaceutics. 2018 Sep 04;15(9):3909-3919. [Content Brief]
[2]. Graewert MA, et al. Quantitative size-resolved characterization of mRNA nanoparticles by in-line coupling of asymmetrical-flow field-flow fractionation with small angle X-ray scattering. Scientific reports. 2023 Sep 22;13(1):15764. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)