(+)-Naloxone
(+)-Naloxone is a TLR4 inhibitor and the dextrorotatory enantiomer of the non-opioid Naloxone (HY-17417A) that lacks opioid receptor binding activity. (+)-Naloxone binds to MD2, preventing LPS from binding to TLR4, thereby inhibiting TLR4 signaling, downstream NFκB activation, and proinflammatory cytokine synthesis. (+)-Naloxone crosses the placenta. (+)-Naloxone is used in the research of preterm birth.
For research use only. We do not sell to patients.
- CAS No.: 65700-73-4
- Formula: C19H21NO4
- Molecular Weight:327.37
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Storage:
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
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- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
TLR4 |
MD2 |
NFκB |
In Vivo
(+)-Naloxone (i.p.; administered immediately after wound closure; followed by 3 additional doses at 12 h intervals) prevents E. coli-induced preterm birth (0/10 mice deliver before gd 18.0), attenuates the reduction in birth weight, and increases postpartum survival at 3 weeks to 56%[1].
(+)-Naloxone (i.p.; administered immediately after wound closure; followed by 3 additional doses at 12 h intervals) suppresses E. coli-induced proinflammatory cytokine expression in fetal membranes (Il1b, Il6, Tnf, Il10 reduced by 66-84%) and maternal uterine tissues, consistent with inhibition of TLR4 signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 (B6) (female, 8-12 weeks of age)[1]
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Dosage:60 mg/kg
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Administration:i.p.; within 5 min of LPS injection on gd 16.5, plus a further 3 equivalent doses at 12 h intervals on gd 17.0, 17.5 and 18.0
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Result:Completely abrogated preterm delivery (0/14 mice delivered before gd 18.0).
Reversed the low survival rate of fetuses in utero after LPS challenge, with the mean number of viable fetuses per dam not less than in the control PBS-treated group.
Exerted a positive impact on fetal weight.
Chemical Information
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CAS No. 65700-73-4
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Molecular Weight 327.37
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Formula C19H21NO4
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SMILES
O[C@@]12[C@]34C5=C(C[C@]2([H])N(CC4)CC=C)C=CC(O)=C5O[C@]3([H])C(CC1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(+)-Naloxone Related Classifications
HY-17417E Related Classifications
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