Free shipping on all orders over $ 500

GW842166X

Cat. No. M3282
GW842166X Structure
Size Price Availability
5mg USD 90 Out of stock
10mg USD 140 Out of stock
25mg USD 220 Out of stock
Bulk Inquiry?

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

GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63nM, respectively. GW842166X exhibits full agonist potency with an EC50 of 133 nM and Emax of 101% in cyclase assays. GW842166X exhibits weak agonist potency with an EC50 of 7.780 μM and Emax of 84% in FLIPR assays.GW842166X has an oral bioavailability of 58% and a half-life of 3 h when dosed orally in the rat. GW842166X has extremely high potency with an oral ED50 of 0.1 mg/kg and shows full reversal of hyperalgesia at 0.3 mg/kg in the FCAa model of inflammatory pain. GW842166X orally administrated at a dose of 15 mg/kg for 8 days produced a significant reversal of the CCI induced decrease in paw withdrawal threshold in a rat model of neuropathic pain.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models rat model of neuropathic pain
Formulation saline
Dosages 15 mg/kg
Administration Orally administrated once daily for 8 days
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 449.25
Formula C18H17Cl2F3N4O2
CAS Number 666260-75-9
Purity >99%
Solubility DMSO 10 mg/mL
Storage at -20°C
Related Cannabinoid Products
WIN 55212-2 mesylate

WIN 55212-2 is a potent nanomolar affinity cannabinoid receptor agonist with Ki of 62.3 and 3.3 nM at the human cloned CB1 and CB2 receptors respectively.

CP 945598

CP 945598 (Otenabant) is a selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.

BML-190

BML-190 is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.

AM-2201

AM-2201 is a potent synthetic cannabinoid (CB) with Ki values of 1.0 and 2.6 nM for the CB1 and CB2 receptors, respectively.

CP 945598 hydrochloride

CP 945598 hydrochloride is a selective and high affinity CB1 antagonist (Ki values are 0.7 and 0.12 nM in binding and functional assays respectively).

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GW842166X supplier, Cannabinoid, 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.