| Bioactivity | AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain[1]. |
| Invitro | AZD6538 以浓度依赖性方式完全逆转了人类 mGluR5-GHEK 细胞中谷氨酸刺激的 (EC80, 80 μM) 磷脂酰肌醇水解，IC50 为 51 ± 3 nM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> AZD6538 相关抗体: |
| CAS | 453566-30-8 |
| Formula | C15H6FN5O |
| Molar Mass | 291.24 |
| Appearance | 固体 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Raboisson P, et al. Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6974-9. |