Size | Price | Stock |
---|---|---|
5mg | $120 | In-stock |
10mg | $204 | In-stock |
25mg | $408 | In-stock |
50mg | $696 | In-stock |
100mg | $1176 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
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Cat. No. : | HY-103007 |
M.Wt: | 418.90 |
Formula: | C18H19ClN6O2S |
Purity: | >98 % |
Solubility: | DMSO : ≥ 100 mg/mL (238.72 mM) |
TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively. IC50 & Target: IC50: 0.4 nM (GPR39), 0.8 nM (GPR39)[1] 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)[1]. 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[2]. 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[1].
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