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| 25mg |
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Purity: ≥98%
TC-G-1008, formerly known as GPR39-C3, is a GPR39 (zinc receptor) agonist (EC50 are 0.4 and 0.8 nM for rat and human receptors respectively).
| Targets |
GPR39 ( IC50 = 0.4 nM ); GPR39 ( IC50 = 0.8 nM )
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|---|---|
| ln Vitro |
TC-G-1008 demonstrates selectivity towards a range of kinases (IC50s>10 μM) and lacks significant binding affinity towards the associated ghrelin and neurotensin-1 receptors (IC50s>30 μM)[1]. GPR39-C3, a positive allosteric modulator, stimulates the production of cAMP (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment in HEK293-GPR39 cells. By introducing the compound again, GPR39-C3 causes a dose- and time-dependent loss of response in the synthesis of cAMP[2].
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| ln Vivo |
For TC-G-1008, the measured levels of rat and mouse plasma protein binding are 99.3% and 99.1%, respectively. In mice, TC-G-1008 is orally bioavailable and effectively raises acute GLP-1 levels. After taking 10, 30, and 100 mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80 orally, TC-G-1008 reaches maximal exposures of 1.4, 6.1, and 25.3 μM in 1 to 1.5 hours, respectively[1].
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| Enzyme Assay |
HEK293-GPR39 cells are plated and grown in the growth medium for an entire night at 37°C with 5% CO2 in white, 384-well plates coated with poly-d-lysine (4000 cells/well). The culture medium is removed before the cells are stimulated with GPR39 ligands in assay buffer for the specified amount of time at 37°C. This is done for pretreatment of the cells with GPR39 ligands (TC-G-1008) or vehicle control (DMSO). After that, the compound solution is taken out and twice cleaned using PBS that has 0.1% BSA added. The cells are stimulated with drugs in stimulation buffer for 30 minutes at 37°C in order to measure the amount of intracellular cAMP. The HTRF cAMP dynamic 2 kit is used to measure the intracellular cAMP level[2].
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| Animal Protocol |
Mice: Single oral doses of TC-G-1008 at 10, 30, and 100 mg/kg are administered to mice[1].
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| References |
| Molecular Formula |
C18H19CLN6O2S
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|---|---|
| Molecular Weight |
418.9
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| Exact Mass |
418.1
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| Elemental Analysis |
C, 51.61; H, 4.57; Cl, 8.46; N, 20.06; O, 7.64; S, 7.65
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| CAS # |
1621175-65-2
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| Related CAS # |
1621175-65-2
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| Appearance |
Solid powder
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| SMILES |
CNC1=NC(=CC(=N1)NCC2=C(C=C(C=C2)NS(=O)(=O)C)Cl)C3=CC=CC=N3
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| InChi Key |
DRSZMILOMUPIBJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H19ClN6O2S/c1-20-18-23-16(15-5-3-4-8-21-15)10-17(24-18)22-11-12-6-7-13(9-14(12)19)25-28(2,26)27/h3-10,25H,11H2,1-2H3,(H2,20,22,23,24)
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| Chemical Name |
N-[3-chloro-4-[[[2-(methylamino)-6-pyridin-2-ylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide
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| Synonyms |
GPR39-C3; GPR39C3; GPR39 C3; TC-G-1008; TC-G1008; TC-G 1008; TCG-1008; TCG1008; TCG 1008
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~84 mg/mL (~200.5 mM)
Ethanol: ~2 mg/mL |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3872 mL | 11.9360 mL | 23.8720 mL | |
| 5 mM | 0.4774 mL | 2.3872 mL | 4.7744 mL | |
| 10 mM | 0.2387 mL | 1.1936 mL | 2.3872 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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