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A-1165442

Catalog No. T14067 CAS 1221443-94-2

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

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A-1165442, CAS 1221443-94-2

Pack Size	Availability	Price/USD
5 mg	8-10 weeks	$ 364.00
25 mg	8-10 weeks	$ 1,490.00
50 mg	8-10 weeks	$ 1,940.00
100 mg	8-10 weeks	$ 2,780.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Storage & Solubility Information

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

Solubility Information

DMSO: 100 mg/mL (231.56 mM)

References and Literature

1. Voight EA, et al. Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy. J Med Chem. 2014 Sep 11;57(17):7412-24.

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Keywords

A-1165442 1221443-94-2 Membrane transporter/Ion channel TRP/TRPV Channel A1165442 A 1165442 inhibitor inhibit

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