| Name | A-1165442 |
| Description | A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM. |
| In vitro | A-1165442 is a potent, competitive antagonist of recombinant human TRPV1, evidenced by its IC50 value of 9 nM when activated by capsaicin and achieves a 62% block at 30 μM in acid-evoked responses, indicating incomplete blockade. It demonstrates exceptional selectivity, exceeding 100-fold over related TRP family members (TRPA1, TRPM8, TRPV2, TRPV3) and shows minimal cross-reactivity with other receptors and channels prevalent in peripheral sensory neurons, such as P2X2/3, Cav2.2, Nav channels, and KCNQ2/3. Furthermore, A-1165442 maintains limited cross-reactivity across a broad panel of 74 cell-surface receptors, ion channels, and enzymes at 10 μM, as assessed in a comprehensive screen (CEREP)[1]. |
| In vivo | A-1165442 demonstrates exceptional pharmacological selectivity, a favorable pharmacokinetic profile, and robust efficacy in mitigating osteoarthritis pain in rodents. Its oral administration effectively inhibits capsaicin-induced nocifensive behaviors in rats, achieving an ED50 of 9.5 μmol/kg, which corresponds to a plasma concentration of 420 ng/mL (970 nM). Furthermore, a single dose markedly enhances grip strength, with an ED50 of 35 μmol/kg observed one hour after administration. Notably, its analgesic potency increases with repeated doses. Importantly, administration of A-1165442 does not significantly alter core body temperature in conscious rats, maintaining this temperature-neutral effect in conscious dogs[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (231.56 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (7.64 mM), Sonication is recommended.
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| Keywords | TRPVChannel | TRPV Channel | TRPChannel | TRP Channel | human TRPV1 | A-1165442 | A1165442 | A 1165442 |
| Inhibitors Related | (+)-Camphor | Rosiglitazone | Caffeic Acid | Oleoyl Serotonin | (-)-Menthol | Camphor | Probenecid | Pregnenolone | Nonivamide | 1,4-Cineole | trans-Cinnamaldehyde | Methyl salicylate |
United States
