SML2784
CMPD101 hydrochloride
≥98% (HPLC)
别名:
3-((4-Methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methylamino)-N-(2-(trifluoromethyl)benzyl)benzamide, 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide hydrochloride, Compound 101 hydrochloride, Cpd101 hydrochloride, Takeda101 hydrochloride
产品名称
CMPD101 hydrochloride, ≥98% (HPLC)
InChI key
QBLGBXYDINNUFE-UHFFFAOYSA-N
SMILES string
CN1C(CNC2=CC=CC(C(NCC3=CC=CC=C3C(F)(F)F)=O)=C2)=NN=C1C4=CC=NC=C4.Cl
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Active site-targeting, potent and subtype-selective G protein-coupled receptor kinase GRK2/3 inhibitor with no inhibitory potency against GRK1/5.
CMPD101 is an active site-targeting, potent and subtype-selective G protein-coupled receptor kinase GRK2 & GRK3 inhibitor (human GRK2/3 IC50 = 54/32 nM with 3 μM ATP and tubulin dimer as substrate; bovine GRK2 IC50 = 290 nM with 0.5 mM ATP and bROS as substrate; no GRK1/5 inhibition at 125 μM). CMPD101 selectively inhibits GPR39 agonist-induced β-arrestin recruitment (by 94% at 10 μM against 30 μM GPR39-C3/50 μM ZnCl2), but not cAMP pathway desensitization in cultures and prevents β-arrestin2-biased D2R ligand UNC9994(1 μg/side bilateral local injection) from blocking NMDAR antagonist PCP (6 mg/kg i.p.)-induced locomotion (60%/12% blockage without/with 0.5 μg CMPD101 co-injection) in mice in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
David M Thal et al.
Molecular pharmacology, 80(2), 294-303 (2011-05-21)
G protein-coupled receptors (GPCRs) are key regulators of cell physiology and control processes ranging from glucose homeostasis to contractility of the heart. A major mechanism for the desensitization of activated GPCRs is their phosphorylation by GPCR kinases (GRKs). Overexpression of
Anika Mann et al.
Science signaling, 12(574) (2019-03-28)
Agonists of the nociceptin/orphanin FQ opioid peptide (NOP) receptor, a member of the opioid receptor family, are under active investigation as novel analgesics, but their modes of signaling are less well characterized than those of other members of the opioid
Alessandro Martini et al.
Neuropharmacology, 155, 76-88 (2019-05-28)
Neurotensin (NT) is a 13-amino acid peptide acting as a neuromodulator in the CNS. NT immunoreactive cell bodies, synaptic terminals and receptors (NTS) are intimately associated with the dopaminergic system. In fact, NT exerts a stimulatory action on the dopaminergic
Arisbel B Gondin et al.
Frontiers in molecular neuroscience, 12, 104-104 (2019-05-24)
Differential regulation of the μ-opioid receptor (MOP) has been linked to the development of opioid tolerance and dependence which both limit the clinical use of opioid analgesics. At a cellular level, MOP regulation occurs via receptor phosphorylation, desensitization, plasma membrane
Seung-Ryoung Jung et al.
The Journal of general physiology, 147(3), 255-271 (2016-03-02)
Activated Gq protein-coupled receptors (GqPCRs) can be desensitized by phosphorylation and β-arrestin binding. The kinetics and individual contributions of these two mechanisms to receptor desensitization have not been fully distinguished. Here, we describe the shut off of protease-activated receptor 2
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