ML-193
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.
IC50: 221 nM
ML-193 is a GPR55 antagonist.
GPR55 is a class A G protein-coupled receptor (GPCR) that has been implicated in inflammatory pain, neuropathic pain, metabolic disorder, bone development, and cancer. Initially deorphanized as a cannabinoid receptor, GPR55 has been shown to be activated by non-cannabinoid ligands such as l-α-lysophosphatidylinositol (LPI).
In vitro: Previous study found that for antagonist activity in the β-arrestin trafficking assay, ML193 and its two close analogs (ML191 and ML192) could inhibit trafficking induced by 10 μM LPI with IC50 values of 0.22 ± 0.03, 1.08 ± 0.03 and 0.70 ± 0.05μM, respectively.In addition, it was also found that ML193, ML191 and ML192 was able to inhibit trafficking induced by 1 μM ML186 with IC50 values of 0.12 ±0.02, 1.03 ± 0.03 and 0.29 ± 0.09 μM, respectively [1].
In vivo: Animal study showd that ML-193 was able to block the increases in intracellular calcium levels that was induced by lysophosphatidylinositol (LPI) in dissociated rat periaqueductal gray neurons and could also modulate pain perception in LPI-treated rats, suggesting that interfering with GPR55 signaling in the PAG might promote analgesia [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Kotsikorou, E. ,Sharir, H.,Shore, D.M., et al. Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry 52(52), 9456-9469 (2013).
[2] Deliu, E. ,Sperow, M.,Console-Bram, L., et al. The lysophosphatidylinositol receptor GPR55 modulates pain perception in the periaqueductal gray. Mol.Pharmacol. 88(2), 265-272 (2015).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 527.6 |
Cas No. | 713121-80-3 |
Formula | C28H25N5O4S |
Synonyms | CID-1261822 |
Solubility | ≤0.1mg/ml in ethanol;2mg/ml in DMSO;3mg/ml in dimethyl formamide |
Chemical Name | N-[4-[[(3,4-dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide |
SDF | Download SDF |
Canonical SMILES | O=C(C1=C(C=C(C)C=C2C)C2=NC(C3=CC=CC=N3)=C1)NC4=CC=C(S(NC5=C(C)C(C)=NO5)(=O)=O)C=C4 |
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。 |