LASSBio-1135

Research use only, not for human use.

LASSBio-1135 is an orally effective antagonist of TRPV1 and inhibitor of TNF-α production.Oral administration of 100 mol x Kg(-1) LASSBio-1135 markedly reduced thermal hyperalgesia induced by carrageenan.

LASSBio-1135 is an orally effective antagonist of TRPV1 and inhibitor of TNF-α production.Oral administration of 100 mol x Kg(-1) LASSBio-1135 markedly reduced thermal hyperalgesia induced by carrageenan, however at 10 mol x Kg(-1) only a partial reduction was observed at the 4th h. Neutrophil recruitment and TNF-α production after carrageenan stimulus was also inhibited by the treatment with LASSBio-1135. Modulating TRPV1 and TNF-α production, two key therapeutic targets of neuropathic pain, 100 mol x Kg(-1) LASSBio-1135 was orally efficacious in reversing thermal hyperalgesia and mechanical allodynia produced by partial sciatic ligation 7-11 days after surgery without provoking hyperthermia, a common side effect of TRPV1 antagonists.

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Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRPV1|TNF-α

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852453-71-5

286.33

C18H14N4

>98% (HPLC)

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N(c1c(nc2ccccn12)-c1ccccn1)c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years