GPR39-C3

Synonym(s):N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide;TC G-1008;TC-G-1008

CAS NO.：1621175-65-2
Empirical Formula: C18H19ClN6O2S
Molecular Weight: 418.9
MDL number: MFCD30182283
Update Date: 2025-12-04 16:42:01

What is GPR39-C3?

Description

GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC₅₀ values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively. It is selective for GPR39 over a panel of kinases (IC₅₀s = >10 μM), ghrelin and neurotensin-1 receptors (IC₅₀s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; ) in STC-1 mouse enteroendocrine cells (EC₅₀ = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC₅₀ = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.

The Uses of GPR39-C3

TC-G 1008 is the first potent, selective, and orally bioavailable GPR39 agonist.

Storage

Store at +4°C

Properties of GPR39-C3

Boiling point:	662.1±65.0 °C(Predicted)
Density	1.462±0.06 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMSO:63.97(Max Conc. mg/mL);152.72(Max Conc. mM) DMSO:PBS (pH 7.2) (1:5):0.16(Max Conc. mg/mL);0.38(Max Conc. mM) Ethanol:2.0(Max Conc. mg/mL);4.77(Max Conc. mM)
form	A crystalline solid
pka	7.43±0.10(Predicted)
color	White to off-white

Safety information for GPR39-C3

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for GPR39-C3

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