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GPR39-C3

Cat. No. M6150
GPR39-C3 Structure
Synonym:

TC-G-1008

Size Price Availability Quantity
5mg USD 110 In stock
10mg USD 185 In stock
25mg USD 400 In stock
50mg USD 680 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Rat
Formulation 0.5% methylcellulose/0.1% Tween 80
Dosages 10, 30, and 100 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 418.9
Formula C18H19ClN6O2S
CAS Number 1621175-65-2
Purity >99%
Solubility 100 mg/mL in DMSO
Storage at -20°C
References

Rho kinase-dependent desensitization of GPR39; a unique mechanism of GPCR downregulation.
Shimizu Y, et al. Biochem Pharmacol. 2017 Sep 15;140:105-114. PMID: 28619258.

Discovery and Characterization of Novel GPR39 Agonists Allosterically Modulated by Zinc.
Sato S, et al. Mol Pharmacol. 2016 Dec;90(6):726-737. PMID: 27754899.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GPR39-C3, TC-G-1008 supplier, inhibitors

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