A CB1 receptor agonist and PAM
Related Products
Isomer(s)
24485GAT228 24486GAT229
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GAT211

Item No. 24484

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(2-nitro-1-phenylethyl)-2-phenyl-1H-indole
CAS Number
102704-40-5
Molecular Formula
C22H18N2O2
Formula Weight
342.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
300 nm
SMILES
O=[N+](CC(C1=CC=CC=C1)C2=C(C3=CC=CC=C3)NC4=CC=CC=C42)[O-]
InChi Code
InChI=1S/C22H18N2O2/c25-24(26)15-19(16-9-3-1-4-10-16)21-18-13-7-8-14-20(18)23-22(21)17-11-5-2-6-12-17/h1-14,19,23H,15H2
InChi Key
OHZDCJJHWPHZJD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $190

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    Product Description

    GAT211 is an agonist and positive allosteric modulator (PAM) of cannabinoid receptor 1 (CB1) and a racemic mixture of GAT228 (Item No. 24485) and GAT229 (Item No. 24486), which have enantiomer-specific activities.1 GAT211 increases β-arrestin recruitment and cAMP inhibition in HEK293A cells expressing GFP-tagged human CB1 (hCB1-GFP) in a concentration-dependent manner. It also enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing hCB1, as well as the activity of 2-arachidonoyl glycerol (2-AG; Item No. 62160), arachidonoyl ethanolamide (AEA; Item No. 90050), and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. It inhibits excitatory postsynaptic currents (EPSCs) in a subset of CB1-expressing murine autaptic hippocampal neurons when used at a concentration of 1 µM.2 GAT211 also decreases mechanical hypersensitivity in wild-type (EC50 = 9.75 mg/kg), but not CB1 knockout, mice in a model of inflammatory pain induced by complete Freund’s adjuvant (CFA), and decreases mechanical and cold allodynia in a mouse model of paclitaxel-induced neuropathic pain when used at doses of 10 and 20 mg/kg per day.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Laprairie, R.B., Kulkarni, P.M., Deschamps, J.R., et al. Enantiospecific allosteric modulation of cannabinoid 1 receptor. ACS Chem Biol. 8(6), 1188-1203 (2017).

    2. Mitjavila, J., Yin, D., Kulkarni, P.M., et al. Enantiomer-specific positive allosteric modulation of CB1 signaling in autaptic hippocampal neurons. Pharmacol. Res. 129, 475-481 (2018).

    3. Slivicki, R.A., Xu, Z., Kulkarni, P.M., et al. Positive allosteric modulation of CB1 suppresses pathological pain without producing tolerance or dependence. Biol. Psychiatry 84(10), 722-733 (2018).