TC-G-1008( GPR39-C3, GPR39 C3, TC-G-1008, TCG1008, TCG 1008 )

Catalog No. M18094 CAS No. 1621175-65-2

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Datasheet

HNMR

HPLC

MSDS

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Product Name

TC-G-1008
Note

Research use only, not for human use.
Brief Description

TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).
Description

TC-G-1008, also known as GPR39-C3, is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).
In Vitro

TC-G-1008 shows selectivity over a panel of kinases (IC50s>10 μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30 μM). In HEK293-GPR39 cells, GPR39-C3, which is a positive allosteric modulator, activates cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment. GPR39-C3 induces dose- and time-dependent loss of response in cAMP production by second challenge of the compound.
In Vivo

Rat and mouse plasma protein binding for TC-G-1008 is measured as 99.3% and 99.1%, respectively. TC-G-1008 is orally bioavailable in mice and robustly induces acute GLP-1 levels. Upon single oral doses of 10, 30, and 100 mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80, TC-G-1008 achieves, between 1 and 1.5 h, maximal exposures of 1.4, 6.1, and 25.3 μM, respectively.
Synonyms

GPR39-C3, GPR39 C3, TC-G-1008, TCG1008, TCG 1008
Pathway

Others
Target

Other Targets
Recptor

rat GPR39| human GPR39
Research Area

——
Indication

——

CAS Number

1621175-65-2
Formula Weight

418.9
Molecular Formula

C18H19ClN6O2S
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 100 mg/mL; 238.72 mM
SMILES

CNc2nc(cc(NCc1ccc(NS(C)(=O)=O)cc1Cl)n2)c3ccccn3
Chemical Name

N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide

1.Peukert S, et al. Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists. ACS Med Chem Lett. 2014 Aug 4;5(10):1114-8.

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