Rofleponide 21-palmitate
Rofleponide 21-palmitate is a lipophilic Corticosteroid prodrug. Rofleponide 21-palmitate reduces subcutaneous edema, plasma haptoglobin levels, and plasma levels of IL-6, KC, IP-10, MCP-1. Rofleponide 21-palmitate increases and prolongs mRNA-encoded protein expression in lipid nanoparticle formulations.
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- CAS No.: 144653-57-6
- 화학식: C41H64F2O7
- 분자량:706.94
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
Rofleponide 21-palmitate (Rofleponide 21-palmitate:mRNA weight ratio 1:1; fixed mRNA dose 0.3 mg/kg; s.c.; single dose) in DLin-MC3-DMA-based LNPs eliminates LNP-induced edema, reduces plasma haptoglobin levels, prolongs mRNA 1 protein expression in mice[1].
Rofleponide 21-palmitate (Rofleponide 21-palmitate:mRNA weight ratio 1:1; fixed mRNA dose 0.3 mg/kg; s.c.; single dose) in Merck-32-based LNPs significantly reduces LNP-induced edema and plasma haptoglobin levels while increasing mRNA 1 protein expression in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Crl:Cd1(ICR) mice (female, ~12 weeks old)[1]
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Dosage:Rofleponide 21-palmitate:mRNA weight ratios of 1:1, 1:10, 1:30; fixed mRNA dose of 0.3 mg/kg
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Administration:s.c.; single dose
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Result:Significantly reduced edema scoring across all rofleponide 21-palmitate LNP groups compared to non-anti-inflammatory LNPs at 24 hours post-administration.
Significantly reduced plasma haptoglobin levels across all ratios compared to non-anti-inflammatory LNPs at 24 hours post-administration.
Increased and prolonged mRNA 1 protein expression over 0-24 hours compared to non-anti-inflammatory LNPs.
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Animal Model:Crl:Cd1(ICR) mice (female, ~12 weeks old)[1]
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Dosage:Rofleponide 21-palmitate:mRNA weight ratio of 1:1; fixed mRNA dose of 0.3 mg/kg
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Administration:s.c.; single dose
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Result:Achieved edema scoring of 0 at 24, 48, and 72 hours post-administration, compared to a score of 5 for rofleponide-containing LNPs at the same molar dose.
Significantly lowered plasma haptoglobin levels at 25, 50, and 75 hours post-administration compared to rofleponide-containing LNPs.
Increased and prolonged mRNA 1 protein expression.
Reached a rofleponide plasma concentration peak of ~6 nM at 2.5 hours post-administration, with a gradual decline over 24 hours, while Rofleponide-containing LNPs showed an initial peak of ~75 nM followed by a rapid drop to near 0 by 5 hours.\n
Reduced edema scoring at 24 hours post-administration compared to non-anti-inflammatory Merck-32 LNPs.
Significantly reduced plasma haptoglobin levels at 24 hours post-administration compared to non-anti-inflammatory Merck-32 LNPs.
Increased mRNA 1 protein expression over 0-24 hours.
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Animal Model:Crl:Cd1(ICR) mice (female, ~12 weeks old)[1]
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Dosage:Rofleponide 21-palmitate:mRNA weight ratio of ~1:1; fixed mRNA dose of 0.3 mg/kg
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Administration:s.c.; single dose
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Result:Reduced edema scoring to near 0 at 24 hours post-administration.
Significantly reduced plasma haptoglobin levels at 24 hours post-administration compared to non-anti-inflammatory LNPs.
Increased and prolonged mRNA 1 protein expression over 0-24 hours, reaching ~0.8 ng/mL at 24 hours compared to near 0 ng/mL for non-anti-inflammatory LNPs.
Chemical Information
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CAS No. 144653-57-6
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분자량 706.94
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화학식 C41H64F2O7
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SMILES
CCCCCCCCCCCCCCCC(OCC([C@]12[C@@]3([C@@]([C@@]4([H])[C@]([C@H](C3)O)([C@@]5(C([C@H](C4)F)=CC(CC5)=O)C)F)([H])C[C@@]1([H])O[C@H](O2)CCC)C)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Rofleponide 21-palmitate Related Classifications
HY-169801 Related Classifications
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