SML2784
CMPD101 hydrochloride
≥98% (HPLC)
동의어(들):
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
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모든 사진(1)
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5 MG
₩207,263
25 MG
₩834,127
About This Item
실험식(Hill 표기법):
C24H21N6OF3 · HCl
CAS Number:
Molecular Weight:
502.92
UNSPSC 코드:
12352200
NACRES:
NA.77
추천 제품
![1,2,3,4-Tetrahydro-9H-pyrido[3,4-b]indole 98%](/deepweb/assets/sigmaaldrich/product/structures/181/460/3d58bc34-1b5c-4295-bbac-3b52085670e8/640/3d58bc34-1b5c-4295-bbac-3b52085670e8.png)
Quality Level
분석
≥98% (HPLC)
양식
powder
저장 조건
desiccated
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
2-8°C
SMILES string
CN1C(CNC2=CC=CC(C(NCC3=CC=CC=C3C(F)(F)F)=O)=C2)=NN=C1C4=CC=NC=C4.Cl
InChI key
QBLGBXYDINNUFE-UHFFFAOYSA-N
생화학적/생리학적 작용
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.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
시험 성적서(COA)
Lot/Batch Number
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
Yuji Shimizu et al.
Biochemical pharmacology, 140, 105-114 (2017-06-18)
GPR39, a G-protein-coupled receptor activated by zinc, reportedly activates multiple intracellular signaling pathways via Gs, Gq, G12/13, and β-arrestin, but little is known about downregulation of the receptor upon its activation. To our knowledge, this is the first report on
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
활성 필터
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