1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. A-1165442

A-1165442 

Cat. No.: HY-12428 Purity: 99.70%
Handling Instructions

A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.

For research use only. We do not sell to patients.

A-1165442 Chemical Structure

A-1165442 Chemical Structure

CAS No. : 1221443-94-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 399 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 399 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 720 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2340 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3360 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.

IC50 & Target

IC50: 9 nM (human TRPV1)[1]

In Vitro

A-1165442 displays potent, competitive antagonism at recombinant human TRPV1 activated by capsaicin (IC50=9 nM) and incomplete blockade of acid-evoked response (62% block at 30 μM). A-1165442 possesses excellent selectivity (>100-fold) versus other members of the TRP family (TRPA1, TRPM8, TRPV2, TRPV3) and other receptors expressed in peripheral sensory neurons including P2X2/3, Cav2.2, Nav channels, and KCNQ2/3. A-1165442 shows minimal cross-reactivity upon evaluation (10 μM) in a broad screening panel (n=74, CEREP) of cell-surface receptors, ion channels, and enzymes[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

A-1165442 exhibits excellent pharmacological selectivity, has a favorable pharmacokinetic profile, and demonstrates good efficacy against osteoarthritis pain in rodents. Oral administration of A-1165442 prevents capsaicin-induced nocifensive behaviors in rats, with an ED50 of 9.5 μmol/kg corresponding to plasma concentration of 420 ng/mL (970 nM). A single dose of A-1165442 produces a robust effect on grip force, with an ED50 of 35 μmol/kg measured 1 h postdosing. Repeated dosing of A-1165442 results in an increase in potency relative to acute analgesic efficacy. No significant changes in core body temperature is observed in conscious rats dosed with A-1165442 and this temperature-neutral profile is maintained in conscious dogs[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

431.86

Formula

C₂₂H₂₀ClF₂N₃O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (231.56 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3156 mL 11.5778 mL 23.1557 mL
5 mM 0.4631 mL 2.3156 mL 4.6311 mL
10 mM 0.2316 mL 1.1578 mL 2.3156 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Dogs: Male beagle dogs are instrumented with telemetry transmitters capable of monitoring core body temperature and then allowed to recover. Dosing is initiated at time zero, with dogs receiving a single oral dose of vehicle, compound 1 at (30 μmol/kg), or A-1165442 (100 μmol/kg); n=4−6 per group. Measurements are recorded every 5 min for the duration of the study, then averaged to 15 min and 1 h intervals. Temperature signals are transmitted as radio signals by each implanted transmitter to a receiver placed on the cage and interfaced with a desktop personal computer[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
A-1165442
Cat. No.:
HY-12428
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