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Product details

名称

GAT211

分子类型

未知

英文名称

GAT211

货号

G646624-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

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

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。

CAS号

102704-40-5

分子式

C22H18N2O2

分子量

342.39 g/mol

PubChem编号

4402318

Isomeric SMILES

C1=CC=C(C=C1)C2=C(C3=CC=CC=C3N2)C(C[N+](=O)[O-])C4=CC=CC=C4

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

PubChem CID

4402318

溶解性

DMSO : 100 mg/mL (292.06 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

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 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

465.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

5.200

RIDADR

NONHforallmodesoftransport

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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