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TM-N1324 (Synonyms: Compound 1324, Cpd1324)

Catalog No.GC31074

TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.

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TM-N1324 Chemical Structure

Cas No.: 1144477-35-9

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10mM (in 1mL DMSO)
$98.00
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1mg
$46.00
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5mg
$111.00
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10mg
$213.00
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50mg
$853.00
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100mg
$1,622.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

Caco-2 cells are used as an in vitro model of the human intestinal epithelium and permit assessment of the intestinalpermeability of TM-N1324. TM-N1324 is added to either theapical or basolateral side of a confluent monolayer of Caco-2 cells and permeability is measured by monitoring the appearance of the TM-N1324 on the opposite side of the membrane using LC-MS/MS. TM-N1324 (3 µM) is incubated with pooled liver microsomes and incubated at 5 time points over the course of a 45 min experiment finally TM-N1324 is analyzed by LC-MS/MS. The intrinsic clearance (CLint) and t1/2 values for TM-N1324 in humanand mouse microsomes are reported[1].

References:

[1]. Frimurer TM, et al. Model-Based Discovery of Synthetic Agonists for the Zn2+-Sensing G-Protein-Coupled Receptor 39 (GPR39) Reveals Novel Biological Functions. J Med Chem. 2017 Feb 9;60(3):886-898.

Background

TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.

TM-N1324 activates human GPR39 with high efficacy and potencies of 280 nM and 9 nM in the absence and presence of Zn2+, respectively. TM-N1324 has similar potencies on murine GPR39, 180 nM and 5 nM. TM-N1324 is also found to have promising in vitro ADME properties. TM-N1324 has reasonably good aqueous solubility (65 μM at pH 7.0). Measurements of somatostatin confirms that the GPR39 agonist TM-N1324 increases somatostatin release by 53%[1].

[1]. Frimurer TM, et al. Model-Based Discovery of Synthetic Agonists for the Zn2+-Sensing G-Protein-Coupled Receptor 39 (GPR39) Reveals Novel Biological Functions. J Med Chem. 2017 Feb 9;60(3):886-898.

Chemical Properties

Cas No. 1144477-35-9 SDF
Synonyms Compound 1324, Cpd1324
Canonical SMILES O=C1CC(C2=CC=C(F)C=C2Cl)C3=C(N(C4=C5N=CNC5=NC=N4)N=C3C)N1
Formula C18H13ClFN7O M.Wt 397.79
Solubility DMSO : 6 mg/mL (15.08 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5139 mL 12.5694 mL 25.1389 mL
5 mM 0.5028 mL 2.5139 mL 5.0278 mL
10 mM 0.2514 mL 1.2569 mL 2.5139 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 11 reference(s) in Google Scholar.)

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