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Search Results for " high-affinity ligand "

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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T13884	Shield-1	Others	Others
	Shield-1 是 FK506 结合蛋白 12 (FKBP) 的特异性、高亲和力和细胞渗透性配体，通过与突变的 FKBP (mtFKBP) 结合来逆转不稳定性，允许 mtFKBP 融合蛋白的条件表达。它可以稳定整个融合蛋白。
TP1704	Galanin Receptor Ligand M35 TFA	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	Galanin Receptor Ligand M35 TFA(142846-71-7 free base) 是一种高亲和力配体和甘丙肽受体拮抗剂 (Kd=0.1 nM)。
T7716	TNCA (S)-2,3,4,9-四氢-1H-吡啶[3,4-B]吲哚-3-羧酸,Lycoperodine-1	Others	Others
	TNCA (Lycoperodine-1) 是一种具有共激动剂活性的高亲和力 CaSR 配体 (CaSRL)。
T7021	ZM241385	Adenosine Receptor	GPCR/G Protein; Neuroscience
	ZM241385 是一种高亲和力的，选择性的腺苷A2AR 拮抗剂，Ki 值为 1.4 nM。
T11349	GABAA receptor agent 1	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	GABAA receptor agent 1 是GABAA 受体的高亲和力配体，有抗惊厥活性。
TP1496L	p5 Ligand for Dnak and DnaJ acetate p5 Ligand for Dnak and DnaJ acetate(209518-24-1 free base)	HSP	Cytoskeletal Signaling; Metabolism
	p5 Ligand for Dnak and DnaJ acetate(209518-24-1 free base) 是一种九肽。它是 DnaK（大肠杆菌 Hsp70）和 DnaJ（大肠杆菌 Hsp40）的高亲和力配体。
T22782	FGIN-1-27	Others	Others
	FGIN 1-27 是一种吲哚乙酰胺，是外周苯二氮卓受体的特异性的配体，Ki 为 5.0 nM。FGIN 1-27 可以透过血脑屏障。FGIN 1-27对异烟肼引起的抽搐发作具有抑制作用。
T16094	MK-3328	Others	Others
	MK-3328 是对β-淀粉样蛋白 (β-Amyloid)具有很高的亲和力(IC50 为 10.5 nM）,是一种可作为临床评估β-淀粉样斑块负荷的候选 PET 配体。MK-3328是治疗阿尔茨海默病的潜在药物。
TP1920L1	Acein acetate	RAAS	Endocrinology/Hormones
	Acein acetate 是高亲和力血管紧张素转换酶 (ACE) 配体 (Kd = 2.79 nM)。浓度高达 500 nM 时对 ACE 酶活性没有显着影响。增强 NMDA + D-丝氨酸诱导的多巴胺从体外纹状体切片和体内纹状体的释放。
T9542	NS3861	AChR	Neuroscience
	NS3861 是烟碱型乙酰胆碱受体的激动剂，对α3β4 nAChR 具有高亲和力。能够分别与α3β4 (Ki:0.62 nM)、α3β2 (Ki:25 nM)、α4β4 (Ki:7.8 nM)、α4β2 (Ki:55 nM) 结合。
T15162	DPA-714	Others	Others
	DPA-714 是高亲和力的移位蛋白配体 (Ki=7 nM)，它结构中有一个氟原子，能够被氟 -18 进行标记，并可通过正电子发射断层成像进行活体成像。它可在各种神经炎症模型及脑肿瘤模型中成功评估炎症的特异性成像。
T24334	L 687384 L687,384,L 687,384,L-687,384,L-687384,L687384
	L 687384 is a high-affinity ligand of sigma receptor.
T13745	KF21213	Histone Demethylase	Chromatin/Epigenetic
	KF21213 shows a high affinity for the adenosine A2A receptors (Ki=3.0 nM). KF21213 is a highly selective ligand for mapping CNS adenosine A2A receptors.
T30811	Cgp 12388 Cgp12388,Cgp-12388
	CGP 12388 is a radioactive ligand derived from a β-adrenergic receptor antagonist and is used for cardiac PET imaging due to its high hydrophilicity and affinity for β-adrenergic receptors.
T13672	EC0489	Others	Others
	EC0489, Small molecule-drug conjugate (SMDC) ,a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor.
T29030	U-101958 Maleate U101958,U-101958,U 101958
	U-101958 Maleate is a ligand of dopamine D4 receptor. U-101958 Maleate also binds to a large sigma1 receptor-like component in SK-N-MC neuroblastoma cells and human cerebellum with high affinity.
T16445	PD 144418	Sigma receptor	GPCR/G Protein
	PD 144418 displays potential antipsychotic activity. PD 144418 is a high affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki: 0.08 nM and 1377 nM for σ1 and σ2 respectively). It shows devoid of any significant affinity for other receptors, ion channels, and enzymes.
TP1767	Prolactin Releasing Peptide (12-31), human
	Prolactin Releasing Peptide (1-31), human is a high affinity GPR10 ligand that cause the release of the prolactin
TP1496	p5 Ligand for Dnak and DnaJ
	p5 Ligand for Dnak and DnaJ is a non-apeptide and correspond to the main binding sites of the 23 residues of the mitochondrial aspartate aminotransferase presequence.P5 ligand is a high affinity ligand for Dnak and DnaJ.
T81999	K1 peptide TFA
	K1 peptide TFA为GABAA受体-相关蛋白(GABARAP)具有高亲和力的肽配体。
T25367	EM-800 EM800,EM 800
	EM-800 is a high affinity ligand for estrogen receptor-α (ERα), the prodrug of EM-652. EM-800 independently inhibited the growth of E1-stimulated ZR-75-1 xenograft tumors in nude mice.
T13813	PCSK9 ligand 1	Others	Others
	PCSK9 ligand 1 is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9(Ki of 107 nM).
T62879	OncoFAP
	OncoFAP 是一种超高亲和力的成纤维细胞激活蛋白（FAP）配体，具有潜在的肿瘤靶向作用。
TP1857	Adrenomedullin (AM) (13-52), human
	Adrenomedullin (13-52) is a 40 amino acid peptide with one intramolecular disulfide bridge, Adrenomedullin (13-52) is a high affinity ligand for the adrenomedullin receptor.
TP2102	WL 47 - dimer
	High affinity caveolin-1 (CAV1) ligand (Kd = 23 nM); disrupts caveolin-1 oligomers. Exhibits selectivity for CAV1 over BSA, casein and HEWL.
T35884	Sialyl-Lewis X
	Sialyl-Lewis X (sLeX), a sialylated fucosylated tetrasaccharide and endogenous antigen, serves as a high-affinity ligand for selectins (E-, P-, and L-selectin)[1]. It interacts with ELAM-1 and CD62, consequently inhibiting CD62-mediated neutrophil recruitment to inflammation sites[2].
T62528	Dopamine D3 receptor ligand-1
	Dopamine D 3 receptor ligand 是一种有效的、选择性的、高亲和力的多巴胺 D3受体配体，对 D3 (Ki: 8 nM) 的选择性是 D2 (Ki: 715 nM) 的89倍。
TP1920	Acein
	Acein is a High affinity angiotensin-converting enzyme (ACE) ligand (Kd = 2.79 nM). Exhibits no significant effect on ACE enzymatic activity up to 500 nM concentration. Potentiates NMDA + D-serine-induced dopamine release from striatal slices in vitro and the striatum in vivo.
T68059	Ebalzotan
	NAE-086 是一种高亲和力和选择性的5-HT(1A)受体配体，其K(i)值为4.5 nM。
T62312	Panamesine
	Panamesine (EMD 57445) 是一种高亲和力的 sigma 的受体配体 (IC50: 6 nM)，具有用于非典型抗精神病研究的潜力。
T29073	UR-2922 UR 2922
	UR-2922 is an oral antagonist of platelet GPIIb/IIIa. UR-2922 possessed a high affinity for the human platelet receptor (K(d) <1 nM) and a slow dissociation rate (k(off)= 90 min) in vitro. UR-2922 induced no ligand-induced binding sites (LIBS) expression
TP1940	Ac-RYYRIK-NH2
	High affinity ligand for the NOP site (Ki = 1.5 nM). Antagonizes nociceptin-stimulated GTP binding in rat brain and the chronotropic effect of nociceptin on rat cardiomyocytes. However, displays potent agonist properties in vivo, inhibiting locomotor acti
T37013	(+/-)-PPCC oxalate
	Selective sigma (σ) receptor ligand. Displays high affinity for σ1; also binds at σ2 sites (Ki = 1.5 nM and 50.8 nM respectively). Selective over a range of receptor types including dopaminergic and muscarinic receptors, DAT and SERT. Prezzavento et al (2007) Novel sigma receptor ligands: synthesis and biological profile. J.Med.Chem. 50 951 PMID:17328523 \|Prezzavento et al (2008) A new sigma ligand, (±)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effect. Life Sci. 82 549 PMI...
T37619	Leukotriene B4 Ethanolamide
	The effects of Leukotriene B4 (LTB4) are mediated by two known receptors, BLT1 and BLT2. LTB4 is a high affinity ligand for BLT1, and many of its pro-inflammatory effects are believed to be transduced through this receptor. The BLT2 is more enigmatic, in that LTB4 is not a high-affinity ligand, nor is it clear that BLT2 activation promotes inflammation. LTB4 ethanolamide (LTB4-EA) is a theoretical 5-LO metabolite of arachidonoyl ethanolamide (AEA). In CHO cells transfected with human BLTR1, LTB4...
T76740	Carlumab
	Carlumab (CNTO 888) 是一种具有高亲和力的人源化抗 CCL2(趋化因子配体 2) 抗体。Carlumab 可用于癌症，尤其是前列腺癌的研究。
T74143	AZD4694 Precursor
	AZD4694 Precursor (AZ13040214) 为[18F] AZD4694合成前体，专用于[18F] AZD4694的合成。该前体作为淀粉样蛋白-β成像配体，展现对淀粉样蛋白-β斑块的高亲和性。
T78248	Nesvacumab
	Nesvacumab为全人源IgG1型单克隆抗体，具有高亲和力，可特异性结合并灭活Tie2受体配体Angiopoietin-2（Ang2），与Ang1无结合作用。
T61434	Mirogabalin besylate
	Mirogabalin besylate is a potent and orally active ligand that selectively targets the α2δ subunit of voltage-gated calcium channels. It displays high affinity (K d ) values, namely 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM, for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
T61836	Pioglitazone potassium
	Pioglitazone potassium (U 72107) is an orally active and selective agonist of peroxisome proliferator-activated receptor gamma (PPARγ). It demonstrates high affinity binding to the ligand-binding domain of PPARγ, with an EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium has applications in diabetes research [2] [3] [4].
TP1769	Prolactin Releasing Peptide (1-31), human
	Prolactin Releasing Peptide (1-31), human is a high affinity GPR10 ligand that cause the release of the prolactin. Human and rat Prolactin Releasing Peptide (1-31) binds to GPR10 with Kis of 1.03 and 0.33 nM, respectively.Prolactin-releasing peptide is a
TP2005	Kisspeptin-54(human) Metastin (human)
	Potent endogenous ligand of the kisspeptin receptor (KISS1, GPR54). Binds with high affinity to rat and human KISS1 receptors with Ki values of 1.80 and 1.45 nM respectively. Inhibits chemotaxis, invasion and metastasis of human melanomas and breast carci
T76820	Namilumab
	Namilumab (AMG203) 是一种人的IgG4单克隆抗体，与GM-CSF 配体高亲和力结合，有效地中和GM-CSF。Namilumab 可用于类风湿关节炎的研究。
T37029	PtdIns-(3,4,5)-P3-biotin (sodium salt) PtdIns-(3,4,5)-P3-biotin (sodium salt)
	The PtdIn phosphates play an important role in the generation and transduction of intracellular signals. PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
T41173	FAM-DEALAHypYIPMDDDFQLRSF
	FAM-DEALAHypYIPMDDDFQLRSF is a 5,6-carboxyfluorescein (FAM) labeled HIF-1α peptide. It binds with high affinity to von Hippel-Lindau (VHL) protein (KD= 3 nM). Can be used to assess ligand binding to VHL in a direct fluorescence polarization (FP) displacement assay. Excitation/emission maxima (λ) = 485/520 nm. This product is a longer peptide version of FAM-DEALA-Hyp-YIPD.
T82417	FAP Ligand 1
	FAPLigand 1（FL）为高亲和力小分子FAP配体，专用于将药物导向表达FAP的成纤维细胞，适用于癌症放射成像研究的靶向。
T10522	BET-IN-6	Epigenetic Reader Domain	Chromatin/Epigenetic
	BET-IN-6 是一种有效且高亲和力的BRD2/BRD4抑制剂。BET-IN-6 是靶蛋白 BRD2/4 的配体，可用于合成 PROTAC BRD2/BRD4 degrader-1 。
T69740	AMG-315
	AMG-315 is a Potent Endocannabinoid Ligand with Stability to Metabolizing Enzymes. AMG-315 is a chiral arachidonoyl ethanolamide (AEA) analogue or (13S,1′R)-dimethylanandamide. AMG-315 is a high affinity ligand for the CB1 receptor (Ki of 7.8 ± 1.4 nM) that behaves as a potent CB1 agonist in vitro (EC50 = 0.6 ± 0.2 nM). AMG-315 is the first potent AEA analogue with significant stability for all endocannabinoid hydrolyzing enzymes as well as the oxidative enzymes COX-2. AMG-315 will serve as a ...
TP1662	Galanin Receptor Ligand M35
	The chimeric peptide M35 [galanin (1-13)-bradykinin(2-9) amide] is a high-affinity galanin receptor ligand acting as a galanin receptor antagonist in the rat spinal cord, rat hippocampus and isolated mouse pancreatic islets. The radiolabelled M35 and perf
T60543	THK-523
	THK-523 在体内外都显示出对tau 的选择性和高亲和力。18F-THK-523 是一种有效的 tau 成像放射性示踪剂，它是用于研究阿尔茨海默病的有效体内 tau 成像配体。
T75845	[Ala17]-MCH TFA
	[Ala17]-MCH TFA 是一种 MCH 的类似物，是 MCHR1的配体 (Ki=0.16 nM) 选择性优于对 MCHR2的 (Ki=34 nM)。Eu3+螯合标记 [Ala17]-MCH 对 MCHR1(Kd=0.37 nM) 亲和性高，而对 MCHR2的亲和性低。

化合物

Cat.No: T13884

Target: Others

Galanin Receptor Ligand M35 TFA

Cat.No: TP1704

Target: Neuropeptide Y Receptor

Cat.No: T7716

Synonym: (S)-2,3,4,9-四氢-1H-吡啶[3,4-B]吲哚-3-羧酸,Lycoperodine-1

Target: Others

Cat.No: T7021

Target: Adenosine Receptor

GABAA receptor agent 1

Cat.No: T11349

Target: GABA Receptor

p5 Ligand for Dnak and DnaJ acetate

Cat.No: TP1496L

Synonym: p5 Ligand for Dnak and DnaJ acetate(209518-24-1 free base)

Target: HSP

Cat.No: T22782

Target: Others

Cat.No: T16094

Target: Others

Cat.No: TP1920L1

Target: RAAS

Cat.No: T9542

Target: AChR

Cat.No: T15162

Target: Others

Cat.No: T24334

Synonym: L687,384,L 687,384,L-687,384,L-687384,L687384

Cat.No: T13745

Target: Histone Demethylase

Cat.No: T30811

Synonym: Cgp12388,Cgp-12388

Cat.No: T13672

Target: Others

U-101958 Maleate

Cat.No: T29030

Synonym: U101958,U-101958,U 101958

Cat.No: T16445

Target: Sigma receptor

Prolactin Releasing Peptide (12-31), human

Cat.No: TP1767

p5 Ligand for Dnak and DnaJ

Cat.No: TP1496

Cat.No: T81999

Cat.No: T25367

Synonym: EM800,EM 800

PCSK9 ligand 1

Cat.No: T13813

Target: Others

Cat.No: T62879

Adrenomedullin (AM) (13-52), human

Cat.No: TP1857

Cat.No: TP2102

Cat.No: T35884

Dopamine D3 receptor ligand-1

Cat.No: T62528

Cat.No: TP1920

Cat.No: T68059

Cat.No: T62312

Cat.No: T29073

Synonym: UR 2922

Cat.No: TP1940

(+/-)-PPCC oxalate

Cat.No: T37013

Leukotriene B4 Ethanolamide

Cat.No: T37619

Cat.No: T76740

AZD4694 Precursor

Cat.No: T74143

Cat.No: T78248

Mirogabalin besylate

Cat.No: T61434

Pioglitazone potassium

Cat.No: T61836

Prolactin Releasing Peptide (1-31), human

Cat.No: TP1769

Kisspeptin-54(human)

Cat.No: TP2005

Synonym: Metastin (human)

Cat.No: T76820

PtdIns-(3,4,5)-P3-biotin (sodium salt)

Cat.No: T37029

Synonym: PtdIns-(3,4,5)-P3-biotin (sodium salt)

FAM-DEALAHypYIPMDDDFQLRSF

Cat.No: T41173

Cat.No: T82417

Cat.No: T10522

Target: Epigenetic Reader Domain

Cat.No: T69740

Galanin Receptor Ligand M35

Cat.No: TP1662

Cat.No: T60543

[Ala17]-MCH TFA

Cat.No: T75845

Cat. No.	Product Name	Target	Signaling Pathways
TP1232L	Amylin, amide, rat acetate(124447-81-0,free base)	Amylin Receptor	GPCR/G Protein
	Amylin, amide, rat acetate(124447-81-0,free base) 是 AMY1 和 AMY3 受体以及 AMY2 受体的强效和高亲和力配体。

天然产物

Amylin, amide, rat acetate(124447-81-0,free base)

Cat.No: TP1232L

Target: Amylin Receptor

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