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A-1165442

Catalog No. T14067Cas No. 1221443-94-2

A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM.

A-1165442

A-1165442

Catalog No. T14067Cas No. 1221443-94-2
A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM.
Pack SizePriceAvailabilityQuantity
5 mg$3648-10 weeks
25 mg$1,4908-10 weeks
50 mg$1,9408-10 weeks
100 mg$2,7808-10 weeks
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight431.86
FormulaC22H20ClF2N3O2
Cas No.1221443-94-2
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.3156 mL11.5778 mL23.1557 mL115.7783 mL
5 mM0.4631 mL2.3156 mL4.6311 mL23.1557 mL
10 mM0.2316 mL1.1578 mL2.3156 mL11.5778 mL
20 mM0.1158 mL0.5789 mL1.1578 mL5.7889 mL
50 mM0.0463 mL0.2316 mL0.4631 mL2.3156 mL
100 mM0.0232 mL0.1158 mL0.2316 mL1.1578 mL

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