1. GPCR/G Protein
  2. GHSR

TM-N1324 

Cat. No.: HY-108699 Purity: 98.91%
Handling Instructions

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.

For research use only. We do not sell to patients.

TM-N1324 Chemical Structure

TM-N1324 Chemical Structure

CAS No. : 1144477-35-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 289 In-stock
Estimated Time of Arrival: December 31
1 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 330 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target

EC50: 280 nM (human GPR39 without Zn2+), 9 nM (human GPR39 with Zn2+), 180 nM (murine GPR39 without Zn2+), 5 nM (murine GPR39 with Zn2+)[1]

In Vitro

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].

Solvent & Solubility
In Vitro: 

DMSO : 6 mg/mL (15.08 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay

Caco-2 cells are used as an in vitro model of the human intestinal epithelium and permit assessment of the intestinal permeability of TM-N1324. TM-N1324 is added to either the apical 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 human and mouse microsomes are reported[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

397.79

Formula

C₁₈H₁₃ClFN₇O

CAS No.

1144477-35-9

SMILES

O=C1CC(C2=CC=C(F)C=C2Cl)C3=C(N(C4=C5N=CNC5=NC=N4)N=C3C)N1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
TM-N1324
Cat. No.:
HY-108699
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TM-N1324

Cat. No.: HY-108699