AM630
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.
AM630是一种选择性的和竞争性的大麻素受体拮抗剂,作用于CB1受体和CB2受体,Ki值分别为5 μM和31.2 nM[1]。
在转染CB1的CHO细胞中,AM630显著抑制毛喉素刺激的cAMP的产生。在转染CB2的细胞中,AM630促进毛喉素刺激的cAMP的产生,EC50值为230.4 nM。AM630也抑制GTPγS与转染CB2细胞的细胞膜的结合。此外,在TG感觉神经元中,AM630可激活TRPA1通道,随后使TRPA1和TRPV1通道脱敏。而且,在WT小鼠中,AM630显著减弱辣椒素(CAP)诱导的热痛觉过敏[1,2]。
参考文献:
1. Ross R A, Brockie H C, Stevenson L A, et al. Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630. British journal of pharmacology, 1999, 126(3): 665-672.
2. Patil M, Patwardhan A, Salas M M, et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology, 2011, 61(4): 778-788.
- 1. Bin Zhang, Feng Zheng, et al. "Activation of CB2 receptor inhibits pyroptosis and subsequently ameliorates cecal ligation and puncture-induced sepsis." Int Immunopharmacol. 2021 Oct;99:108038. PMID:34364304
- 2. Zou G, Zuo X, et al. "Cannabinoids Rescue Cocaine-Induced Seizures by Restoring Brain Glycine Receptor Dysfunction." Cell Rep. 2020;30(12):4209-4219.e7. PMID:32209479
- 3. Liu AP, Yuan QH, et al. "Cannabinoid receptor 2 activation alleviates septic lung injury by promoting autophagy via inhibition of inflammatory mediator release." Cell Signal. 2020;69:109556. PMID:32027949
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 504.36 |
Cas No. | 164178-33-0 |
Formula | C23H25IN2O3 |
Synonyms | AM 630;AM-630 |
Solubility | ≥25.2 mg/mL in DMSO; insoluble in H2O; ≥2.53 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | [6-iodo-2-methyl-1-(2-morpholin-4-ylethyl)indol-3-yl]-(4-methoxyphenyl)methanone |
SDF | Download SDF |
Canonical SMILES | CC1=C(C2=C(N1CCN3CCOCC3)C=C(C=C2)I)C(=O)C4=CC=C(C=C4)OC |
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。 |
Cell experiment:[1] | |
Cell lines |
Trigeminal ganglia (TG) sensory neurons |
Reaction Conditions |
10 μM AM630 for 3 min incubation |
Applications |
The application of cannabinoid receptor antagonist AM630 (10 μM) activated a robust Ca2+ accumulation in a subset (35 ~ 40%) of TG neurons. The AM630-evoked Ca2+ influxes into TG sensory neurons were concentration-dependent, with an EC50 value being 15.6 μM. |
Animal experiment:[2] | |
Animal models |
Swiss ICR mice |
Dosage form |
1, 2 or 3 mg/kg Administered intraperitoneally twice a day for 7 days |
Applications |
Chronic AM630 treatment alleviated anxiety-like behaviors in the light-dark box and elevated plus maze tests. Meanwhile, chronic AM630 treatment increased gene and reduced protein expression of CB2 receptors, GABAAα2 and GABAAγ2 in cortex and amygdala. |
Note |
The technical data provided above is for reference only. |
References: 1. Patil M, Patwardhan A, Salas MM, et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology, 2011, 61(4): 778-788. 2. García-Gutiérrez MS, García-Bueno B, Zoppi S, et al. Chronic blockade of cannabinoid CB2 receptors induces anxiolytic-like actions associated with alterations in GABA(A) receptors. British Journal of Pharmacology, 2012, 165(4): 951-964. |
质量控制和MSDS
- 批次: