Lu AF21934
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EC50为500 nM。
Lu AF21934是mGlu4受体的一种正向变构调节剂。
III组mGlu的mGlu4受体亚型主要是突触前自或异受体。其刺激导致对谷氨酸能或GABA能传递和释放的抑制
体外：Lu AF21934已被鉴定为mGlu4受体的一种脑通透性正向变构调节剂。在广泛的体外筛选中，Lu AF21934可以增强mGlu4受体的谷氨酸反应，Emax = 120％且谷氨酸酯折叠移位FS = 5。10 μM的Lu AF21934未对70个GPCRs显示出任何显著亲和力，但是作为mGlu6受体的弱正性变构调节剂，以及腺苷A2A和5-HT2B受体的拮抗剂[1]。
体内：在大鼠中，harmaline引发震颤，表现为9-15Hz频带内的功率和震颤指数增加。 Harmaline还诱导对流动性的双相作用，最初抑制大鼠的探索性运动活动，随后增加其基本活性。Lu AF21934在0.5-5 mg/kg sc不影响震颤，但是在0.5和2.5 mg/kg的剂量下逆转harmaline诱导的多动症。MGlu4 mRNA表达在小脑皮层中较高，而在下橄榄中较低[1]。
临床试验：到目前为止，Lu AF21934仍处于临床前研究阶段。
参考文献：
[1] Ossowska K,Wardas J,Berghauzen-Maciejewska K,et al. Lu AF21934, a positive allosteric modulator of mGlu4 receptors, reduces the harmaline-induced hyperactivity but not tremor in rats. Neuropharmacology.2014 Aug;83:28-35.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 315.2 |
| Cas No. | 1445605-23-1 |
| Formula | C14H16Cl2N2O2 |
| Solubility | ≥31.5 mg/mL in DMSO; insoluble in H2O; ≥5.03 mg/mL in EtOH with ultrasonic |
| Chemical Name | (1R,2S)-2-((3,4-dichlorophenyl)carbamoyl)cyclohexanecarbimidic acid |
| SDF | Download SDF |
| Canonical SMILES | ClC1=C(C=C(C=C1)NC([C@]2(CCCC[C@]2(C(O)=N)[H])[H])=O)Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
