NNC 0640

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Cat.No. 6807 - NNC 0640 | C29H31N7O4S | CAS No. 307986-98-7
Description: Negative allosteric modulator of glucagon and GLP-1 receptors
Chemical Name: 4-[[(4-Cyclohexylphenyl)[[[3-(methylsulfonyl)phenyl]amino]carbonyl]amino]methyl]-N-2H-tetrazol-5-ylbenzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity

Negative allosteric modulator of glucagon receptors (pKi = 7.4). Binds to external surface of the transmembrane domain. Also negative allosteric modulator of glucagon-like peptide 1 (GLP-1) receptor. Inhibits GLP-1-mediated cAMP accumulation in vitro.

Technical Data

M. Wt 573.67
Formula C29H31N7O4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 307986-98-7
PubChem ID 23549991
InChI Key PPTKULJUDJWTSA-UHFFFAOYSA-N
Smiles CS(=O)(C1=CC=CC(NC(N(C2=CC=C(C3CCCCC3)C=C2)CC4=CC=C(C(NC5=NN=NN5)=O)C=C4)=O)=C1)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 57.37 100

Preparing Stock Solutions

The following data is based on the product molecular weight 573.67. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.74 mL 8.72 mL 17.43 mL
5 mM 0.35 mL 1.74 mL 3.49 mL
10 mM 0.17 mL 0.87 mL 1.74 mL
50 mM 0.03 mL 0.17 mL 0.35 mL

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References

References are publications that support the biological activity of the product.

Zhang et al (2017) Structure of the full-length glucagon class B g-protein-coupled receptor. Nature. 546 259 PMID: 28514451

Jazayeri et al (2016) Extra-helical binding site of a glucagon receptor antagonist. Nature. 533 274 PMID: 27111510

Song et al (2017) Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators. Nature. 546 213 PMID: 28514449


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Keywords: NNC 0640, NNC 0640 supplier, NNC0640, glucagon, receptor, glucagon-like, peptide, 1, GLP-1, GLP-1R, negative, allosteric, modulators, modulates, NAMs, GCGR, Glucagon, Receptor, Glucagon-Like, Peptide, Receptors, 6807, Tocris Bioscience

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Literature in this Area

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