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GAT211

    级别和纯度:
  • ≥99%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
G646624-5mg
5mg 期货 Stock Image
G646624-10mg
10mg 期货 Stock Image
G646624-25mg
25mg 期货 Stock Image
G646624-50mg
50mg 期货 Stock Image
G646624-100mg
100mg 期货 Stock Image

基本描述

规格或纯度 ≥99%
英文名称 GAT211
生化机理 GAT211 是一种大麻素 1 受体(CB1R)正异位调节剂(PAM)。GAT211 可激活 cAMP 和 β-arrestin2,其 EC 50 值分别为 260 nM 和 650 nM。GAT211 可抑制神经病理性疼痛和/或炎症性疼痛。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 激动剂
产品介绍


GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC 50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research

In Vitro

GAT211 is stable in both human- and rat-liver microsomal incubations, with t 1/2 of 28.4 min and 8.67 min, repsectively. GAT211 limits dopamine D2 receptor-mediated extracellular regulated kinase (ERK) phosphorylation in Neuro2a cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GAT211 potentiates the inhibition of electrically evoked vas deferens contraction in the same system (EC 50 =11 nM, E max =70). GAT211 (0.3 mg/kg, 1 mg/kg, 3 mg/kg; 5 mL/kg; ip; 2 doses with 5 min interval) dose-dependently reduced locomotor activity and the acoustic startle response.GAT211 is dissolved in a vehicle of ethanol, kolliphor, and saline at a ratio of 1:1:6 and injected at a volume of 5 mL/kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:CB1

纯度 ≥99%

关联靶点(人)

CNR1 Tclin 大麻素受体 1(Cannabinoid receptor 1) (3 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 未知
IIUPAC Name 3-(2-nitro-1-phenylethyl)-2-phenyl-1H-indole
INCHI 1S/C22H18N2O2/c25-24(26)15-19(16-9-3-1-4-10-16)21-18-13-7-8-14-20(18)23-22(21)17-11-5-2-6-12-17/h1-14,19,23H,15H2
InChi Key OHZDCJJHWPHZJD-UHFFFAOYSA-N
Smiles C1=CC=C(C=C1)C2=C(C3=CC=CC=C3N2)C(C[N+](=O)[O-])C4=CC=CC=C4
Isomeric SMILES C1=CC=C(C=C1)C2=C(C3=CC=CC=C3N2)C(C[N+](=O)[O-])C4=CC=CC=C4
PubChem CID 4402318
分子量 342.39

化学和物理性质

溶解性 DMSO : 100 mg/mL (292.06 mM; Need ultrasonic)
分子量 342.400 g/mol
XLogP3 5.200
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 2
可旋转键计数Rotatable Bond Count 4
精确质量Exact Mass 342.137 Da
单同位素质量Monoisotopic Mass 342.137 Da
拓扑极表面积Topological Polar Surface Area 61.600 Ų
重原子数Heavy Atom Count 26
形式电荷Formal Charge 0
复杂度Complexity 465.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 1
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性(GHS)

WGK Germany 3
RIDADR NONHforallmodesoftransport

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
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