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A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $364 | 8-10 weeks | |
25 mg | $1,490 | 8-10 weeks | |
50 mg | $1,940 | 8-10 weeks | |
100 mg | $2,780 | 8-10 weeks |
Description | A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM. |
Targets&IC50 | TRPV1 (human):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]. |
Molecular Weight | 431.86 |
Formula | C22H20ClF2N3O2 |
Cas No. | 1221443-94-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (231.56 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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