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TC-G-1008

SKU: orb1222634

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).

Images & Validation

Key Properties

CAS Number1621175-65-2
MW418.9
Purity>98% (HPLC)
FormulaC18H19ClN6O2S
SMILESCNc2nc(cc(NCc1ccc(NS(C)(=O)=O)cc1Cl)n2)c3ccccn3
Targetrat GPR39| human GPR39
SolubilityDMSO : ≥ 100 mg/mL; 238.72 mM

Bioactivity

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.
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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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

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Protocol Information

TC-G-1008 (orb1222634)

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(Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO +
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% Tween 80 +
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Available Sizes

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2 mg
¥ 1,430.00
5 mg
¥ 1,950.00
10 mg
¥ 3,120.00
25 mg
¥ 5,980.00
50 mg
¥ 10,010.00
100 mg
¥ 14,170.00
500 mg
¥ 28,210.00