TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.

Product information

CAS Number: 1144477-35-9

Molecular Weight: 397.79

Formula: C18H13ClFN7O

Chemical Name: 4-(2-chloro-4-fluorophenyl)-3-methyl-1-(9H-purin-6-yl)-1H,4H,5H,6H,7H-pyrazolo[3,4-b]pyridin-6-one

Smiles: CC1=NN(C2=NC=NC3NC=NC=32)C2NC(=O)CC(C=21)C1=CC=C(F)C=C1Cl

InChiKey: CYQNVXRIWKKWQG-UHFFFAOYSA-N

InChi: InChI=1S/C18H13ClFN7O/c1-8-14-11(10-3-2-9(20)4-12(10)19)5-13(28)25-17(14)27(26-8)18-15-16(22-6-21-15)23-7-24-18/h2-4,6-7,11H,5H2,1H3,(H,25,28)(H,21,22,23,24)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 12.22 mg/mL (30.72 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

TM-N1324 activates human GPR39 with high efficacy and potencies of 280 nM and 9 nM in the absence and presence of Zn2+, respectively. TM-N1324 has similar potencies on murine GPR39, 180 nM and 5 nM. TM-N1324 is also found to have promising in vitro ADME properties. TM-N1324 has reasonably good aqueous solubility (65 μM at pH 7.0). Measurements of somatostatin confirms that the GPR39 agonist TM-N1324 increases somatostatin release by 53%.

Products are for research use only. Not for human use.