GNE-049
- Product Name
- GNE-049
- CAS No.
- 1936421-41-8
- Chemical Name
- GNE-049
- Synonyms
- GNE-049;GNE049;GNE 049;Ethanone, 1-[3-[7-(difluoromethyl)-3,4-dihydro-6-(1-methyl-1H-pyrazol-4-yl)-1(2H)-quinolinyl]-1,4,6,7-tetrahydro-1-(tetrahydro-2H-pyran-4-yl)-5H-pyrazolo[4,3-c]pyridin-5-yl]-
- CBNumber
- CB74667949
- Molecular Formula
- C27H32F2N6O2
- Formula Weight
- 510.58
- MOL File
- 1936421-41-8.mol
GNE-049 Property
- Boiling point:
- 788.2±60.0 °C(Predicted)
- Density
- 1.43±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 150 mg/mL (293.78 mM)
- form
- Solid
- pka
- 1.90±0.20(Predicted)
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- CS-0028645
- Product name
- GNE-049
- Purity
- 98.98%
- Packaging
- 5mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- orb611432
- Product name
- GNE-049
- Packaging
- 5mg
- Price
- $663
- Updated
- 2021/12/16
- Product number
- orb611432
- Product name
- GNE-049
- Packaging
- 10mg
- Price
- $805.8
- Updated
- 2021/12/16
- Product number
- CS-0028645
- Product name
- GNE-049
- Purity
- 98.98%
- Packaging
- 10mg
- Price
- $850
- Updated
- 2021/12/16
- Product number
- orb611432
- Product name
- GNE-049
- Packaging
- 25mg
- Price
- $1293.7
- Updated
- 2021/12/16
GNE-049 Chemical Properties,Usage,Production
Uses
GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively[1].
in vivo
GNE-049 demonstrates acceptable PK in mouse, rat, dog, and monkey. Determination of potency versus a selection of bromodomains revealed that GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1). GNE-049 is further evaluated in a rat single dose (30-250 mg/kg QD) toxicokinetic study. Adverse central nervous system (CNS)-related signs (e.g., marked hyperactivity and vocalization) are observed in several of the rats at the 250 mg/kg dose level. Furthermore, at the 250 mg/kg dose level, the ratio of the unbound drug concentration in brain to unbound drug concentration in plasma (Kp,uu) 3 h post dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity[1].
References
[1] Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem. 2017 Nov 22;60(22):9162-9183. DOI:10.1021/acs.jmedchem.7b00796
GNE-049 Preparation Products And Raw materials
Raw materials
Preparation Products
GNE-049 Suppliers
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- 021-65675885 18964387627
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- 021-65675885
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- China
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- United States
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- qq: 1050376806 mailbox : sales@nbpharmabridge.com
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- 18818260767
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- QQ 3610331285
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- China
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- 020-82000279 18988941452
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- QQ：3283937693
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- China
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