Free shipping on all orders over $ 500

AM-0902

Cat. No. M6250
AM-0902 Structure
Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 720 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity > 99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 370.79
Formula C17H15ClN6O2
CAS Number 1883711-97-4
Purity > 99%
Solubility 150 mg/mL in DMSO
Storage at -20°C
References

Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.
Schenkel LB, et al. J Med Chem. 2016 Mar 24;59(6):2794-809. PMID: 26942860.

Related Products
Ceforanide

Ceforanide is a new cephalosporin with antibacterial activity and has a longer elimination half-life than any currently available cephalosporin.

Inositol Nicotinate

Inositol Nicotinate is a formulation of niacin, which is also called vitamin B3, an essential human nutrient.

ND-630

ND-630 is an ACC inhibitor of human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.

D-Luciferin potassium salt

D-Luciferin potassium salt is the substrate of luciferases that catalyze the production of light in bioluminescent insects.

ZD 7114 hydrochloride

ZD 7114 is a selective β3 adrenergic receptor agonist.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AM-0902 supplier, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.