WrFr-OCH3
WrFr-OCH3 is a competitive nAChR inhibitor, with IC50 values of 291.9 nM, 25.3 nM, 477.5 nM and 36.5 nM against hα1β1εδ nAChR, hα9α10 nAChR, hα7 nAChR and hα9 nAChR, respectively. WrFr-OCH3 exhibits analgesic and muscle relaxant effects, reduces forelimb grip strength in rats, and alleviates Oxaliplatin (HY-17371)-induced cold allodynia in rats. WrFr-OCH3 can be used in studies related to cold allodynia.
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- Formule: C33H47N11O5
- Masse moléculaire:677.80
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
WrFr-OCH3 (100 pM-30 μM) potently and competitively inhibits adult muscle-type hα1β1εδ nAChR heterologously expressed in Xenopus oocytes, with an IC50 of 291.9 nM[1].
WrFr-OCH3 (30 pM-10 μM) potently and competitively inhibits the heterologously expressed neuronal hα9α10 nAChR in Xenopus oocytes, with an IC50 of 25.3 nM[1].
WrFr-OCH3 (100 pM-30 μM) moderately inhibits the heterologously expressed neuronal hα7 nAChR in Xenopus oocytes, with an IC50 value of 477.5 nM[1].
WrFr-OCH3 (30 pM-10 μM) inhibits the heterologously expressed neuronal hα9 nAChR in Xenopus oocytes, with an IC50 of 36.5 nM, and its potency is weaker than that on hα9α10 nAChR[1].
WrFr-OCH3 (1 mg/mL; 0-24 h) exhibits good stability in serum, with a half-life of 14.20 h, and its degradation occurs primarily via C-terminal ester hydrolysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
WrFr-OCH3 (60 μg/kg-600 μg/kg; intramuscular injection; single administration) produces a dose-dependent muscle relaxant effect in healthy rats. At a dose of 600 μg/kg, it exerts a long-lasting effect with a duration of over 120 min and a delayed peak onset time, compared with Rocuronium (HY-17033)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 180-200 g, oxaliplatin-induced cold allodynia model)[1]
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Dosage:500 μg/kg; 800 μg/kg; 1 mg/kg
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Administration:i.v.; single dose
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Result:Significantly reduced cold allodynia scores within 12 h at 1 mg/kg, with effects waning by 24 h.
Produced comparable antinociceptive effects to 50 mg/kg gabapentin in the first 3 h postadministration, with significantly lower acetone response scores than gabapentin after 3 h at 1 mg/kg.
Decreased acetone response scores within 12 h at 800 μg/kg.
Exhibited antinociceptive effect lasting only 1 h at 500 μg/kg.
Did not impair rat muscle strength at 1 mg/kg.
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Animal Model:Sprague-Dawley[1]
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Dosage:60 μg/kg; 600 μg/kg
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Administration:i.m.; single dose
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Result:Induced only mild muscle relaxation lasting approximately 30 min at 60 μg/kg.
Significantly reduced forelimb grip strength, with a slower onset of action (peak relaxation at ~20 min postinjection) and a muscle relaxant effect persisting for over 120 min at 600 μg/kg, which is longer than the duration of action of 600 μg/kg rocuronium.
Chemical Information
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Masse moléculaire 677.80
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Formule C33H47N11O5
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Sequence
Trp-d{Arg}-Phe-d{Arg}-OCH3
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Sequence Shortening
W-d{Arg}-F-d{Arg}-OCH3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WrFr-OCH3 Related Classifications
HY-P11860 Related Classifications
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