NNC0640
- Product Name
- NNC0640
- CAS No.
- 307986-98-7
- Chemical Name
- NNC0640
- Synonyms
- NNC0640;NNC-0640, 10 mM in DMSO;NNC-0640,Glucagon Receptor,NNC0640,GCGR,inhibit,Inhibitor,NNC 0640;4-((1-(4-Cyclohexylphenyl)-3-(3-(methylsulfonyl)phenyl)ureido)methyl)-N-(1H-tetrazol-5-yl)benzamide;Benzamide, 4-[[(4-cyclohexylphenyl)[[[3-(methylsulfonyl)phenyl]amino]carbonyl]amino]methyl]-N-2H-tetrazol-5-yl-
- CBNumber
- CB54718643
- Molecular Formula
- C29H31N7O4S
- Formula Weight
- 573.67
- MOL File
- 307986-98-7.mol
NNC0640 Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:57.37(Max Conc. mg/mL);100.0(Max Conc. mM)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 6807
- Product name
- NNC0640
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $215
- Updated
- 2021/12/16
- Product number
- 6807
- Product name
- NNC0640
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $905
- Updated
- 2021/12/16
- Product number
- CS-0087150
- Product name
- NNC-0640
- Purity
- 98.48%
- Packaging
- 5mg
- Price
- $390
- Updated
- 2021/12/16
NNC0640 Chemical Properties,Usage,Production
Description
NNC0640 is a negative allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R).
in vitro
Crystal structures of the human GLP-1R transmembrane domain in complex with two different negative allosteric modulators, PF-06372222 and NNC0640, at 2.7 and 3.0 ? resolution, respectively were reported. The structures reveal a common binding pocket for negative allosteric modulators, present in both GLP-1R and GCGR and located outside helices V-VII near the intracellular half of the receptor. The receptor is in an inactive conformation with compounds that restrict movement of the intracellular tip of helix VI, a movement that is generally associated with activation mechanisms in class A GPCRs. Molecular modelling and mutagenesis studies indicate that agonist positive allosteric modulators target the same general region, but in a distinct sub-pocket at the interface between helices V and VI, which may facilitate the formation of an intracellular binding site that enhances G-protein coupling._x000D_ _x000D_ Reference: Song G, Yang D, Wang Y, de Graaf C, Zhou Q, Jiang S, Liu K, Cai X, Dai A, Lin G, Liu D, Wu F, Wu Y, Zhao S, Ye L, Han GW, Lau J, Wu B, Hanson MA, Liu ZJ, Wang MW, Stevens RC. Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators. Nature. 2017 Jun 8;546(7657):312-315. doi: 10.1038/nature22378. Epub 2017 May 17. PMID: 28514449.
target
Glucagon receptors (pKi = 7.4).
storage
Store at -20°C
NNC0640 Preparation Products And Raw materials
Raw materials
Preparation Products
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