A-1165442

Name: A-1165442
Brand: TargetMol
SKU: T14067
Price: 48 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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

Catalog No. T14067Cas No. 1221443-94-2

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

Pack Size	Price	Availability
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

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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 Weight	431.86
Formula	C₂₂H₂₀ClF₂N₃O₂
Cas No.	1221443-94-2

Storage & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.3156 mL	11.5778 mL	23.1557 mL	115.7783 mL
5 mM	0.4631 mL	2.3156 mL	4.6311 mL	23.1557 mL
10 mM	0.2316 mL	1.1578 mL	2.3156 mL	11.5778 mL
20 mM	0.1158 mL	0.5789 mL	1.1578 mL	5.7889 mL
50 mM	0.0463 mL	0.2316 mL	0.4631 mL	2.3156 mL
100 mM	0.0232 mL	0.1158 mL	0.2316 mL	1.1578 mL

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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