2. Immunology/Inflammation Vitamin D Related/Nuclear Receptor
  3. Glucocorticoid Receptor Interleukin Related
  4. 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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Rofleponide 21-palmitate

Rofleponide 21-palmitate Chemical Structure

CAS No. : 144653-57-6

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Rofleponide 21-palmitate Related Antibodies

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Description

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[1][2].

In Vivo

Rofleponide 21-palmitate (Rofleponide 21-palmitate:mRNA weight ratios 1:1-1:30; fixed mRNA dose 0.3 mg/kg; s.c.; single dose) in DLin-MC3-DMA-based LNPs significantly reduces LNP-induced edema and plasma haptoglobin levels while increasing and prolonging mRNA 1 protein expression in female Crl:Cd1(ICR) 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 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.

Animal Model: Crl:Cd1(ICR) mice (female, ~12 weeks old)[1]
Dosage: Rofleponide 21-palmitate:mRNA weight ratios of 1:1, 1:10, 1:30; fixed mRNA dose of 0.3 mg/kg
Administration: s.c.; single dose
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.
Animal Model: Crl:Cd1(ICR) mice (female, ~12 weeks old)[1]
Dosage: Rofleponide 21-palmitate:mRNA weight ratio of 1:1; fixed mRNA dose of 0.3 mg/kg
Administration: s.c.; single dose
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.
Animal Model: Crl:Cd1(ICR) mice (female, ~12 weeks old)[1]
Dosage: Rofleponide 21-palmitate:mRNA weight ratio of ~1:1; fixed mRNA dose of 0.3 mg/kg
Administration: s.c.; single dose
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.
Molecular Weight

706.94

Formula

C41H64F2O7
CAS No.
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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Purity & Documentation
References
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Rofleponide 21-palmitate Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rofleponide 21-palmitate144653-57-6Glucocorticoid ReceptorInterleukin RelatedILplasma haptoglobinMCP-1single-crystal X-ray diffractionIP-10KCcorticosteroid prodrugCrl:Cd1(ICR) micesubcutaneous edemalipid nanoparticle formulationsIL-6Inhibitorinhibitorinhibit

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