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54

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T79577	CB2 PET Radioligand 1	Cannabinoid Receptor	GPCR/G Protein
	CB2PET Radioligand 1 (compound [18F]9) 作为hCB2靶向的PET Radioligand (Ki=7.7 nM)，采用Cu介导的18F-氟化方法制备，并在小鼠神经炎症模型中展现了高脑摄取率。
T21667	FAUC-365 FAUC-365 Benzo[b]thiophene-2-carboxylic acid {4-[4-(2,3-dichloro- phenyl)-piperazin-1-yl]-butyl}-amide,FAUC-365 Benzo[b]thiophene-2-carboxylic acid {4-[4-(2,3-dichloro- phenyl)-piperazin-1-yl]-butyl}-amide	Dopamine Receptor	GPCR/G Protein; Neuroscience
	FAUC-365 是一种高度选择性的多巴胺D3受体拮抗剂，能够作用于 D3 受体(Ki:0.5 nM)、D4.4 受体(Ki:340 nM)、D2short 受体(Ki:2600 nM)和 D2Long 受体(Ki:3600 nM)。它可用于研究帕金森病、精神分裂症等疾病。
T11894	Lusaperidone R107474	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Lusaperidone (R107474) 是一种有效的α2肾上腺素受体 (adrenergic receptor) 拮抗剂，是 α (2）-肾上腺素受体的潜在放射性配体，对 α2A和α2C 具有抑制作用， Ki 值分别为0.13和0.15 nM。
T16140	MRS 1754	Adenosine Receptor	GPCR/G Protein; Neuroscience
	MRS 1754 是A2B 腺苷受体选择性拮抗剂，对人和大鼠的 A1和 A3受体的亲和力非常低。
T38205	3-Aminopropylphosphonic Acid	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	3-Aminopropylphosphonic Acid 是与膦酸的磷相连的氢被3-氨基丙基取代的膦酸，是 GABAB 受体（GABABR）的部分激动剂和基础催乳素分泌拮抗剂。
T30140	Arotinolol hydrochloride Arotinolol HCl	5-HT Receptor; Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Arotinolol hydrochloride（Arotinolol HCl）是一种非选择性的 α/β-肾上腺素受体 (α/β-adrenergic receptor ) 阻滞剂。Arotinolol hydrochloride 对放射性配体 125I-ICYP 与 5HT1B-羟色胺受体能结合有抑制作用。Arotinolol hydrochloride 是一种抗高血压和抗肥胖试剂，可改善大鼠主动脉僵硬，研究肥胖相关疾病。
T16115	MLi-2	LRRK2	Autophagy
	MLi-2 是一种结构新颖、高效、选择性的 LRRK2 激酶抑制剂，具有中枢神经系统活性，IC50为 0.76 nM，有潜力用于帕金森氏病。
T26478	A-317920
	A-317920 is an inverse agonist radioligand.
T34243	R214127 R 214127,R-214127
	R214127 is a new type of mGlu1 receptor high-affinity radioligand.
T69100	A-349821
	A-349821 is an H3 receptor agonist radioligand.
T34626	Setoperone R-52245,R 52245,R52245
	Setoperone, as a sensitive radioligand, can be commonly used in position emission tomography (PET) imaging.
T70459	BMT-046091
	BMT-046091 is a potent and selective radioligand which inhibits adaptor-associated kinase 1 (AAK1).
T30253	AZD-2184 J2.698.897G,AZD2184
	AZD-2184 is a radioligand for detecting beta-amyloid deposits.
T34688	SP203 SP-203,SP 203
	SP203 is a radioligand for brain metabotropic glutamate receptor imaging.
T33277	Mefway F-18 18F-Mefway
	Mefway F-18 is a PET radioligand specific to serotonin-1A receptors.
T27494	GSK931145 GSK 931145,GSK-931145
	GSK931145 is a positron emission tomography (PET) radioligand, it is suitable for quantifying glycine transporter (GlyT1) availability in the living brain.
T39069	UCB-J
	UCB-J is a radioligand for the synaptic vesicle protein 2A (SV2A), utilized in positron emission tomography (PET)[4].
T10371	Arotinolol	5-HT Receptor	GPCR/G Protein; Neuroscience
	Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. It is an antihypertensive agent.
T34483	Sadopine
	Sadopine is an excellent high affinity, high specific activity radioligand to label selectively the DHP receptor of L-type Ca2+ channels in tissue sections as well as in membrane fragments.
T71186	ORM-13070
	ORM-13070 is a selective antagonist radioligand for the α2C adrenoceptor subtype. ORM-13070 C-11 is under investigation in clinical trial.
T29913	Altanserin R-53200,R53200,R 53200
	Altanserin can binds to the 5-HT2A receptor. Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) studies of the brain.
T70615	TAS-303
	TAS-303 is a selective norepinephrine reuptake inhibitor which displays significant norepinephrine transporter (NET) inhibitory activity toward serotonin or dopamine transporters. Radioligand-binding studies showed that TAS-303 selectively and potently inhibited [3H]norepinephrine binding to the human NET.
T38787	ER176
	ER176 is a novel PET radioligand utilized for the visualization of 18 kDa translocator protein (TSPO), a neuroinflammation biomarker, marking the advancement in imaging technology.
T29913L	Altanserin tartrate R-53,200
	Altanserin tartrate is a compound that binds to the 5-HT2A receptor. Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) studies of the brain.
T28335	PD 140376 PD-140376,PD140376
	PD 140376 is a highly selective antagonist radioligand for the cholecystokinin(B)-gastrin receptor in guinea pig gastric mucosa & cerebral cortex in the peripheral and central nervous systems.
T27455	GSK-215083 GSK215083
	GSK-215083 is a PET radioligand for the 5-HT6 receptor. GSK 215083 is a quinoline based compounds and acts by antagonising the 5-HT6 receptor. GSK-215083 binds to receptors 5-hydroxytrypamine-6 (5HT6) in the striatum and 5-hydroxytryptamine-2A (5HT2A) in
T19690	SB 224289 SB224289,SB-224289
	SB 224289 is a selective antagonist of 5-HT1B receptor with pKi of 8.2. It is a centrally active following oral administration in vivo. SB 224289 displays 60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand
T38162	STING18
	STING18 is a competitive ligand of stimulator of interferon genes (STING; IC50 = 0.068 μM in a radioligand binding assay).1 It inhibits cGAMP-induced IFN-β production (IC50 = 11 μM) but does not stimulate IFN-β production (EC50 = >30 μM) in THP-1 cells. \|1. Siu, T., Altman, M.D., Baltus, G.A., et al. Discovery of a novel cGAMP competitive ligand of the inactive form of STING. Med. Chem. Lett. 10(1), 92-97 (2019).
T38289	Leucomycin A13 Leucomycin A13
	Leucomycin A13 is a macrolide antibiotic and a component of the leucomycin complex originally isolated from S. kitasatoensis. It is active against B. subtilis, S. aureus, M. luteus, and E. coli with MIC values of 0.16, 0.16, 0.08 and >10 μg/ml, respectively. It binds to ribosomes with an IC50 value of 1.2 μM in a radioligand binding assay.
T29742	AH-9700 free base
	AH-9700 free base 用于治疗急迫性尿失禁和尿毒症。在一项放射性配体结合研究中，AH-9700 free base 对 sigma 受体表现出较高的亲和力，对膀胱功能正常的实验动物的排尿反射(即膀胱容量增加作用)有明显的抑制作用。
T75145	TRV-7019
	TRV-7019，一种能穿透血脑屏障的放射性配体，用于丁酰胆碱酯酶的脑成像，适用于淀粉样蛋白病、多发性硬化症、脑肿瘤或丁酰胆碱酯酶活性的诊断。
T38171	Ro 1138452 hydrochloride
	Selective prostacyclin IP receptor antagonist (pKi = 8.3). Exhibits no affinity at other prostanoid receptors (EP1-4, FP and TP) in a radioligand binding assay. Demonstrates analgesic activity in rats. Orally bioavailable. Clark et al (2004) Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg.Med.Chem.Lett. 14 1053 PMID:15013022 \|Jones et al (2006) Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel ...
T72999	PF-06455943
	PF-06455943, 作为一种LRRK2 (富含亮氨酸的重复激酶 2) 抑制剂，具有3 nM的IC50值，主要用于帕金森病（PD）的研究。
T35591	Guanfacine-13C,15N3 Guanfacine-13C,15N3
	Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacin...
T38223	N-(1-(3,4-Dihydroxyphenyl)propan-2-yl)oleamide
	N-(1-(3,4-Dihydroxyphenyl)propan-2-yl)oleamide binds to the cannabinoid 1 (CB1) receptor with a Ki value of 365 nM in a radioligand binding assay using rat brain homogenate. It has an EC50 value of 698 nM for the peroxisome proliferator-activated receptor α (PPARα) in a luciferase reporter assay and, in rats, it decreases food intake. It does not inhibit fatty acid amide hydrolase (FAAH).
T16547	PK14105	Others	Others
	PK14105 has been evaluated biologically as a potential radioligand for positron emission tomography (PET) studies targeting peripheral benzodiazepine binding sites (PBBS) receptors. When administered to rats with unilaterally lesioned striata, PK14105 was observed to quickly cross the blood-brain barrier, displaying significant radioactivity retention in the lesioned striatum, in contrast to the unlesioned striatum or cerebellar vermis. Additionally, PK14105 has the capability to inhibit recepto...
T62141	RBP4 ligand-1
	RBP4 ligand-1 是一种视黄醇结合蛋白 4 (RBP4) 的非视黄醇配体。RBP4 ligand-1 在放射配体结合检测和 FRET 检测中对 hRBP4SPAIC50 和 RBP4–TTR FRET IC50值分别为 0.23±0.11 和 0.13±0.12 μM。
T73711	Atomoxetine-d3 hydrochloride
	Atomoxetine-d3 hydrochloride 是氘代标记的Atomoxetine hydrochloride。Atomoxetine hydrochloride 是去甲肾上腺素重吸收抑制剂，与人NET，SERT 和DAT 的放射性配体结合的 Ki 分别为5，77和1451 nM。
T37131	MS 15203
	Potent and selective GPR171 partial agonist (EC50 = 90 nM; 28% inhibition of forskolin activated adenylyl cyclase activity in rat hypothalamic memebranes). Exhibits minimal binding to a panel of ~70 GPCRs and 10 other receptors (<22% of radioligand displaced from the target receptors). Increases neuronal activity in the paraventricular nucleus. Increases food intake and body weight in mice. Wardman et al (2016) Identification of a small-molecule ligand that activates the neuropeptide receptor GP...
T78927	PSMA-IN-3
	PSMA-IN-3（compound 17）是一种高亲和力的新型PSMA抑制剂，IC50为13 nM。该化合物可作为开发18F标记的放射性配体的基础，用于前列腺癌PSMA的PET成像。
T16443	PCS1055 dihydrochloride	Others	Others
	PCS1055 dihydrochloride is an effective, selective, and competitive muscarinic M4 receptor antagonist (IC50: 18.1 nM and a Kd: 5.72 nM). PCS1055 dihydrochloride is also a potent AChE inhibitor (IC50 s: 22 nM and 120 nM for electric eel and human AChE, res
T36204	Methylatropine (nitrate)
	Methylatropine is an antagonist of muscarinic acetylcholine receptors (IC50= <0.1 nM in a radioligand binding assay using isolated porcine brain membranes) and a derivative of atropine .1,2It reduces acetylcholine-induced decreases in blood pressure in rats when administered intravenously with an ED50value of 5.5 μg/kg.2Methylatropine reduces salivation, induces mydriasis, and increases heart rate in dogs.3 1.Schmeller, T., Sporer, F., Sauerwein, M., et al.Binding of tropane alkaloids to nicotin...
T37167	Reduced Haloperidol
	Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing ...
T37212	5-hydroxy-Nω-methyl Tryptamine (oxalate)
	5-hydroxy-Nω-methyl Tryptamine is a metabolite of serotonin in humans that has also been found in plants. It is an agonist of the 5-HT receptor subtype 5-HT7 (IC50 = 23 pM in a radioligand binding assay). 5-hydroxy-Nω-methyl Tryptamine increases intracellular cyclic AMP production in HEK293 cells expressing 5-HT7 (EC50 = 22 nM). It inhibits serotonin uptake in HEK293 cells expressing human serotonin transporters (IC50 = 490 nM). Elevated levels of urinary 5-hydroxy-Nω-methyl tryptamine have been...
T31828	AZD4694 Flutafuranol,AZD 4694,NAV-4694,AZD-4694,NAV 4694,NAV4694
	Flutafuranol, also known as AZD 4694 and NAV4694, is a bio-active chemical. AZD4694 shows high affinity for beta-amyloid fibrils in vitro (K(d) = 2.3 +/- 0.3 nM). The fluorine-18 labeled AZD4694 may have potential for PET-visualization of cerebral beta-am
T37492	11-trans Leukotriene C4 11-trans Leukotriene C4
	11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum ...
T83957	CELT-211
	CELT-211是一种强效且选择性的h5HT2B血清素受体荧光配体。它对h5HT2B显示出完全选择性，与h5HT2A、h5HT2C相比，其在放射配体结合测定中针对h5HT2B受体的Ki值为56.3 nM。激发和发射峰值（λ）分别为589和616 nm。这些波长与CoraFlor 1 TR-FRET供体一起使用作为TR-FRET测定中的受体染料是兼容的。
T35772	Emestrin
	Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities.1,2,3,4,5 It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg/ml, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestr...
T69383	NBI-42902
	NBI-42902 is a potent inhibitor of peptide radioligand binding to the human GnRH receptor (K(i) = 0.56 nm). Tritiated NBI-42902 binds with high affinity (K(d) = 0.19 nm) to a single class of binding sites and can be displaced by a range of peptide and nonpeptide GnRH receptor ligands. In vitro experiments demonstrate that NBI-42902 is a potent functional, competitive antagonist of GnRH stimulated IP accumulation, Ca(2+) flux, and ERK1/2 activation. It did not stimulate histamine release from rat...
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...

化合物

CB2 PET Radioligand 1

Cat.No: T79577

Target: Cannabinoid Receptor

Cat.No: T21667

Synonym: FAUC-365 Benzo[b]thiophene-2-carboxylic acid {4-[4-(2,3-dichloro- phenyl)-piperazin-1-yl]-butyl}-amide,FAUC-365 Benzo[b]thiophene-2-carboxylic acid {4-[4-(2,3-dichloro- phenyl)-piperazin-1-yl]-butyl}-amide

Target: Dopamine Receptor

Cat.No: T11894

Synonym: R107474

Target: Adrenergic Receptor

Cat.No: T16140

Target: Adenosine Receptor

3-Aminopropylphosphonic Acid

Cat.No: T38205

Target: GABA Receptor

Arotinolol hydrochloride

Cat.No: T30140

Synonym: Arotinolol HCl

Target: 5-HT Receptor, Adrenergic Receptor

Cat.No: T16115

Target: LRRK2

Cat.No: T26478

Cat.No: T34243

Synonym: R 214127,R-214127

Cat.No: T69100

Cat.No: T34626

Synonym: R-52245,R 52245,R52245

Cat.No: T70459

Cat.No: T30253

Synonym: J2.698.897G,AZD2184

Cat.No: T34688

Synonym: SP-203,SP 203

Cat.No: T33277

Synonym: 18F-Mefway

Cat.No: T27494

Synonym: GSK 931145,GSK-931145

Cat.No: T39069

Cat.No: T10371

Target: 5-HT Receptor

Cat.No: T34483

Cat.No: T71186

Cat.No: T29913

Synonym: R-53200,R53200,R 53200

Cat.No: T70615

Cat.No: T38787

Altanserin tartrate

Cat.No: T29913L

Synonym: R-53,200

Cat.No: T28335

Synonym: PD-140376,PD140376

Cat.No: T27455

Synonym: GSK215083

Cat.No: T19690

Synonym: SB224289,SB-224289

Cat.No: T38162

Cat.No: T38289

Synonym: Leucomycin A13

AH-9700 free base

Cat.No: T29742

Cat.No: T75145

Ro 1138452 hydrochloride

Cat.No: T38171

Cat.No: T72999

Guanfacine-13C,15N3

Cat.No: T35591

Synonym: Guanfacine-13C,15N3

N-(1-(3,4-Dihydroxyphenyl)propan-2-yl)oleamide

Cat.No: T38223

Cat.No: T16547

Target: Others

Cat.No: T62141

Atomoxetine-d3 hydrochloride

Cat.No: T73711

Cat.No: T37131

Cat.No: T78927

PCS1055 dihydrochloride

Cat.No: T16443

Target: Others

Methylatropine (nitrate)

Cat.No: T36204

Reduced Haloperidol

Cat.No: T37167

5-hydroxy-Nω-methyl Tryptamine (oxalate)

Cat.No: T37212

Cat.No: T31828

Synonym: Flutafuranol,AZD 4694,NAV-4694,AZD-4694,NAV 4694,NAV4694

11-trans Leukotriene C4

Cat.No: T37492

Synonym: 11-trans Leukotriene C4

Cat.No: T83957

Cat.No: T35772

Cat.No: T69383

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

Cat. No.	Product Name	Target	Signaling Pathways
T4727	Taurolithocholic acid sodium salt 牛磺石胆酸钠,Sodium taurolithocholate	Others; Calcium Channel	Membrane transporter/Ion channel; Metabolism; Others
	Taurolithocholic acid sodium salt (Sodium taurolithocholate) 是抑胆剂和 Ca2+激动剂，可抑制放射性配体与毒蕈碱 M1 结合。
T37714	Fuscin
	Fuscin is a quinonoid fungal metabolite originally isolated from O. fuscum that has diverse biological activities. It inhibits binding of the ADP/ATP translocase inhibitor atractyloside to rat liver mitochondria in an ADP-dependent manner when used at a concentration of 50 μM in a radioligand binding assay. Fuscin (20 μM) reduces the glutathione content of rat liver mitochondria to 28% of controls and inhibits NADH oxidation in sonicated pigeon heart mitochondria preparations in a concentration-...

天然产物

Taurolithocholic acid sodium salt

Cat.No: T4727

Synonym: 牛磺石胆酸钠,Sodium taurolithocholate

Target: Others, Calcium Channel

Cat.No: T37714

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