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Submit ReviewVU 0650991
说明： Non-competitive GLP-1 antagonist; orally bioavailable and brain penetrant
化学名： 7-(4-Chlorophenyl)-5,8-dihydro-1,3-dimethyl-5,5-bis(trifluoromethyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione
纯度： ≥98% (HPLC)
生物活性 for VU 0650991
VU 0650991 is a noncompetitive glucagon-like peptide-1 (GLP-1) receptor antagonist (IC50 = 0.65 - 0.69 μM). Displays >40-fold selectivity for GLP-1 receptor over glucagon receptors. Blocks activity of Exendin-4 (Cat. No. 1933) in potentiating insulin secretion from primary mouse pancreatic islets in vitro. Decreases blood insulin and increases blood glucose levels in vivo. Brain penetrant and orally bioavailable.
技术数据 for VU 0650991
| 分子量 | 440.73 |
| 公式 | C16H11ClF6N4O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 488097-06-9 |
| PubChem ID | 1941609 |
| InChI Key | MFEIZMHODFOWAT-UHFFFAOYSA-N |
| Smiles | CN1C(N(C2=C(C(C(F)(F)F)(C(F)(F)F)N=C(C3=CC=C(C=C3)Cl)N2)C1=O)C)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for VU 0650991
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 44.07 | 100 |
制备储备液 for VU 0650991
以下数据基于产品分子量 440.73。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.27 mL | 11.34 mL | 22.69 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.27 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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产品说明书 for VU 0650991
参考文献 for VU 0650991
参考文献是支持产品生物活性的出版物。
Nance et al (2017) Discovery of a novel series of orally bioavailable and CNS penetrant GLP-1R noncompetitive 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. 60 1611 PMID: 28103022
If you know of a relevant reference for VU 0650991, please let us know.
关键词: VU 0650991, VU 0650991 supplier, VU0650991, GLP1, glucagon, like, peptide, 1, receptor, antagonism, antagonists, brain, penetrant, orally, bioavailable, Glucagon-Like, Peptide, Receptors, 6355, Tocris Bioscience
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