1. Membrane Transporter/Ion Channel
  2. TRP Channel
  3. AM-0902

AM-0902 

Cat. No.: HY-108329 Purity: 99.39%
Handling Instructions

AM-0902 is a potent, selective transient receptor potential A1 (TRPA1) antagonist with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively.

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

AM-0902 Chemical Structure

AM-0902 Chemical Structure

CAS No. : 1883711-97-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Estimated Time of Arrival: December 31
100 mg USD 960 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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  • Biological Activity

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  • References

Description

AM-0902 is a potent, selective transient receptor potential A1 (TRPA1) antagonist with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively.

IC50 & Target

IC50: 71 nM (rTRPA1), 131 nM (hTRPA1)[1]

In Vitro

AM-0902 is a potent, selective antagonist of TRPA1 with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively. AM-0902 is highly permeable (average Papp=44.5 μcm/s in MDCK cells), an unlikely substrate for P-gp (efflux ratio=1.3 in P-gp overexpressing MDCK cells), and demonstrates good solubility (PBS pH 7.4: 226 μM, SIF: 248 μM). AM-0902 shows good selectivity over other TRP channels, as no activity is observed against human TRPV1 or TRPV4, or rat TRPV1, TRPV3, or TRPM8, at concentrations up to 10 μM. AM-0902 inhibits 45Ca2+ flux upon activation of rat TRPA1 with methylglyoxal with an IC50 of 0.019 μM[1].

In Vivo

AM-0902 is a potent, selective antagonist of TRPA1 in vivo. AM-0902 has moderate terminal elimination half-life (t1/2=0.6 h and 2.8 h for rat (0.5 mg/kg, iv), rat (30 mg/kg, oral)). A dose-dependent reduction of allyl isothiocyanate (AITC)-induced flinching is observed for AM-0902, with a significant reduction in flinching observed postdosing of 10 and 30 mg/kg. The unbound plasma concentrations (Cu) at 1 h for the 1, 3, 10, and 30 mg/kg doses are 0.051±0.024 (n=8), 0.19±0.11 (n=8), 0.58±0.35 (n=8), and 2.2±0.40 (n=8) μM, covering the in vitro rat TRPA1 45Ca2+ IC50 at 0.72, 2.7, 8.2, and 30.3 fold, respectively. A good exposure-response relationship is observed in this target coverage model. An unbound in vivo IC50 of 0.35 μM, which is in good agreement with the in vitro rat TRPA1 45Ca2+ IC50, and unbound in vivo IC90 of 1.7 μM are determined. It is noteworthy that at a dose of 30 mg/kg, AM-0902 engages TRPA1 at concentrations that exceed the in vivo IC90, making it a useful tool for exploration of in vivo models of acute pain[1].

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 : 150 mg/mL (404.54 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6969 mL 13.4847 mL 26.9694 mL
5 mM 0.5394 mL 2.6969 mL 5.3939 mL
10 mM 0.2697 mL 1.3485 mL 2.6969 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 (6.74 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.74 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.74 mM); Clear solution

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

MDCK cells are generated and maintained for the TRPA1 calcium flux assays. On the day of assay, culture media is removed and cells are incubated for 10 min at room temperature (RT) with 50 μL of AM-0902 (compound 27) in AM-0902 dilution buffer [HBSS containing 1 mM HEPES+0.1 mg/mL BSA] at final concentrations (2.0 nM to 40 μM, 1:3 ratio), followed by another 3 min incubation at RT. The reaction mixture is aspirated, and cells are washed three times with phosphate buffer saline (PBS) containing 0.1 mg/mL BSA. Radioactivity is measured using a TopCount microplate scintillation counter. The activation of TRPA1 is measured by the cellular uptake of radioactive calcium[1].

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

Animal Administration
[1]

Rats[1]
Rats are dosed orally with either vehicle (2% HPMC/1% Tween-80) or AM-0902 at 1, 3, 10, or 30 mg/kg. After 1 h, one left ventral hind paw is injected with the TRPA1 agonist AITC (0.1%). AM-0902 is also given by an intravenous (IV) injection to rats (0.5 mg/kg)[1].

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

References
Molecular Weight

370.79

Formula

C₁₇H₁₅ClN₆O₂

CAS No.

1883711-97-4

SMILES

O=C1N(CC2=NC(CCC3=CC=C(Cl)C=C3)=NO2)C=NC4=C1N(C)C=N4

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
AM-0902
Cat. No.:
HY-108329
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AM-0902

Cat. No.: HY-108329