7-(4-chlorophenyl)-1,3-dimethyl-5,5-bis(trifluoromethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4-dione
- Product Name
- 7-(4-chlorophenyl)-1,3-dimethyl-5,5-bis(trifluoromethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4-dione
- CAS No.
- 488097-06-9
- Chemical Name
- 7-(4-chlorophenyl)-1,3-dimethyl-5,5-bis(trifluoromethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4-dione
- Synonyms
- VU 0650991;GLP-1R Antagonist 1;GLP-1R Antagonist 1, 10 mM in DMSO;GLP 1R Antagonist 1,GLP1R Antagonist 1;7-(4-chlorophenyl)-1,3-dimethyl-5,5-bis(trifluoromethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4-dione;Pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione, 7-(4-chlorophenyl)-5,8-dihydro-1,3-dimethyl-5,5-bis(trifluoromethyl)-
- CBNumber
- CB44599881
- Molecular Formula
- C16H11ClF6N4O2
- Formula Weight
- 440.7275592
- MOL File
- 488097-06-9.mol
7-(4-chlorophenyl)-1,3-dimethyl-5,5-bis(trifluoromethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4-dione Property
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- color
- White to light yellow
N-Bromosuccinimide Price
- Product number
- 6355
- Product name
- VU0650991
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $224
- Updated
- 2021/12/16
- Product number
- CS-0020879
- Product name
- GLP-1RAntagonist1
- Purity
- 99.48%
- Packaging
- 25mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0020879
- Product name
- GLP-1RAntagonist1
- Purity
- 99.48%
- Packaging
- 50mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0020879
- Product name
- GLP-1RAntagonist1
- Purity
- 99.48%
- Packaging
- 100mg
- Price
- $850
- Updated
- 2021/12/16
- Product number
- CS-0020879
- Product name
- GLP-1RAntagonist1
- Purity
- 99.48%
- Packaging
- 5mg
- Price
- $110
- Updated
- 2021/12/16
7-(4-chlorophenyl)-1,3-dimethyl-5,5-bis(trifluoromethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4-dione Chemical Properties,Usage,Production
Description
VU 0650991 is a non-competitive GLP-1 antagonist that is orally bioavailable and acts as a brain penetrant.
Uses
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM[1].
in vivo
GLP-1R Antagonist 1 (compound 5d) (10 mg/kg, p.o.) increases the levels of blood glucose and decreases the levels of blood insulin in male Sprague-Dawley rats[1].
Pharmacokinetic Analysis in MC38 Syngeneic Model[1]
| Route | Dose (mg/kg) | CLp (mL/min/kg) | t1/2 (min) | Vss (L/kg) | %F |
| i.v., p.o. | 1, 3 | 4.79 | 587 | 3.57 | 50 |
storage
Store at -20°C
References
[1] Kellie D. Nance, et al. Discovery of a novel series of orally bioavailable and CNS penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) non-competitive antagonists based on a 1,3-disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione core. J. Med. Chem. 19 Jan 2017. DOI:10.1021/acs.jmedchem.6b01706
7-(4-chlorophenyl)-1,3-dimethyl-5,5-bis(trifluoromethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4-dione Preparation Products And Raw materials
Raw materials
Preparation Products
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