Product Details
| Product Name:
TC-G-1008 |
CAS No.:
1621175-65-2 |
| Purity:
99% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | TC-G-1008 |
| Description | TC-G-1008 (GPR39-C3) is a zinc receptor agonist with EC50 values of 0.4 nM for rat GPR39 and 0.8 nM for human GPR39. |
| Kinase Assay | HEK293-GPR39 cells are plated and cultured in poly-d-lysine-coated, white, 384-well plates (4000 cells/well) in the growth medium overnight at 37°C in the presence of 5% CO2. For pretreatment of the cells with GPR39 ligands (TCG-1008) or vehicle control (DMSO), the culture medium is removed and the cells are stimulated with GPR39 ligands in assay buffer for the indicated time at 37°C. Then, the compound solution is removed and washed twice with PBS containing 0.1% BSA. For measurement of intracellular cAMP, the cells are stimulated with drugs in stimulation buffer for 30 min at 37°C. The intracellular cAMP level is determined by using HTRF cAMP dynamic 2 kit[2] . |
| Animal Research | Mice: Mice are given single oral doses of 10, 30, and 100 mg/kg of TC-G-1008[1] . |
| In vitro | TC-G-1008 demonstrates selectivity over a panel of kinases (IC50s>10 μM) and lacks significant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30 μM)[1]. GPR39-C3 acts as a positive allosteric modulator in HEK293-GPR39 cells, activating cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment, and induces dose- and time-dependent loss of response in cAMP production upon second challenge[2]. |
| In vivo | Rat and mouse plasma protein binding for TC-G-1008 is 99.3% and 99.1%, respectively. TC-G-1008 is the first potent GPR39 agonist (EC50s ≤ 1 nM for human and rat receptor) that is orally bioavailable in mice and significantly induces acute GLP-1 levels. Following 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 maximal exposures of 1.4, 6.1, and 25.3 μM, respectively, between 1 and 1.5 hours[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (131.3 mM)
|
| Keywords | inhibit | GHSR | TC-G 1008 | Inhibitor | TC-G-1008 | TC-G1008 | Growth hormone secretagogue receptor | TC G 1008 | TCG1008 |
| Inhibitors Related | Ibutamoren Mesylate | Capromorelin Tartrate | AnaMorelin hydrochloride | YIL 781 | Anamorelin | CJC-1295 acetate(863288-34-0 free base) | hGPR91 antagonist 1 | L-692429 | NF-56-EJ40 hydrochloride | TM-N1324 | Obestatin (rat) acetate | Cortistatin-8 acetate |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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