GAT211
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MedKoo CAT#: 571261

CAS#: 102704-40-5

Description: GAT211, aslo known as AZ-4, is a small molecule CB1 positive allosteric modulator. GAT211 suppresses allodynia and produces synergistic antiallodynic effects with fatty acid amide hydrolase and monoacylglycerol lipase inhibitors in paclitaxel-treated mice. Positive allosteric modulation of CB1-receptor signaling with GAT211shows promise as a safe and effective analgesic strategy that lacks tolerance, dependence, and abuse liability.

Chemical Structure

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GAT211
CAS# 102704-40-5
Instruction

Theoretical Analysis

MedKoo Cat#: 571261
Name: GAT211
CAS#: 102704-40-5
Chemical Formula: C22H18N2O2
Exact Mass: 342.14
Molecular Weight: 342.400
Elemental Analysis: C, 77.17; H, 5.30; N, 8.18; O, 9.35

Price and Availability

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5mg USD 295
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Synonym: GAT211; GAT 211; GAT-211; AZ-4; AZ4; AZ 4;

IUPAC/Chemical Name: 3-(2-nitro-1-phenylethyl)-2-phenyl-1H-indole

InChi Key: OHZDCJJHWPHZJD-UHFFFAOYSA-N

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

SMILES Code: O=[N+](CC(C1=C(C2=CC=CC=C2)NC3=C1C=CC=C3)C4=CC=CC=C4)[O-]

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 342.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Laprairie RB, Kulkarni PM, Deschamps JR, Kelly MEM, Janero DR, Cascio MG, Stevenson LA, Pertwee RG, Kenakin TP, Denovan-Wright EM, Thakur GA. Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor. ACS Chem Neurosci. 2017 Jun 21;8(6):1188-1203. doi: 10.1021/acschemneuro.6b00310. Epub 2017 Feb 7. PubMed PMID: 28103441.

2: Slivicki RA, Xu Z, Kulkarni PM, Pertwee RG, Mackie K, Thakur GA, Hohmann AG. Positive Allosteric Modulation of Cannabinoid Receptor Type 1 Suppresses Pathological Pain Without Producing Tolerance or Dependence. Biol Psychiatry. 2017 Jul 8. pii: S0006-3223(17)31761-4. doi: 10.1016/j.biopsych.2017.06.032. [Epub ahead of print] PubMed PMID: 28823711.

3: Nguyen T, German N, Decker AM, Langston TL, Gamage TF, Farquhar CE, Li JX, Wiley JL, Thomas BF, Zhang Y. Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. J Med Chem. 2017 Aug 18. doi: 10.1021/acs.jmedchem.7b00707. [Epub ahead of print] PubMed PMID: 28792219.