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Cat. No. Product Name Target Signaling Pathways
T2320 Indacaterol

Adrenergic Receptor GPCR/G Protein; Neuroscience
Indacaterol 是一种超长效β-肾上腺素受体激动剂。
T1239 Indacaterol maleate

马来酸茚达特罗,QAB149

Adrenergic Receptor GPCR/G Protein; Neuroscience
Indacaterol maleate (QAB149) 是一种超长效的 β-肾上腺素受体激动剂。
T13324 VUF11207 fumarate

CXCR; Arrestin Autophagy; GPCR/G Protein; Immunology/Inflammation
VUF11207 fumarate 是一种 CXCR7激动剂和高效CXCR7配体,pKi 为 8.1。它可诱导CXCR7的β-arrestin2募集和随后的内在化,pEC50分别为 8.8 和 7.9。
TP1923L1 ELA-14(human) acetate

ELA-14(human) acetate (1886973-05-2 free base)

Apelin receptor; Arrestin GPCR/G Protein
ELA-14(human) acetate 是 ELA 的一个片段,它与 APJ 结合,激活 Gαi1 和 β-arrestin-2 信号通路,并类似于其亲本内源性肽诱导受体内化。
T23583 58-G3

58G3

58-G3 is an agonist of methuselah (Mth)-specific that acts by inducing dose-dependent calcium elevation and membrane translocation of β-arrestin2.
T70403 VUF14480

VUF14480 is a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor. VUF14480 was shown to be a partial agonist of hH4 receptor-mediated G protein signalling and β-arrestin2 recruitment. VUF14480 bound covalently to the hH₄ receptor with submicromolar affinity. Serine substitution of C98(3.36) prevented this covalent interaction.
T79373 A3AR agonist 2

Adenosine Receptor GPCR/G Protein; Neuroscience
A3AR agonist 2 (Compound 19) 是高选择性A3AR激动剂,Ki为22.1 nM。本化合物有效促进β-arrestin2募集,展现出EC50为4.36 nM。A3AR agonist 2 主要用于研究炎症性疾病、缺血、癌症、神经性疼痛、肝脏病以及其他慢性病态。
T69513 (–)-IHCH7041

(–)-IHCH7041 is a optical rotation negative isomer of IHCH7041. (–)-IHCH7041 is a DRD2 partial agonist. (–)-IHCH7041 showed EC50 = 1.38 nM in Gαi1–γ9 dissociation and 2.75 nM in β-arrestin2 recruitment. (–)-IHCH7041 exhibited a inhibition constant (Ki) of 22.44 nM binding affinity at DRD2. (–)-IHCH7041 has antidepressant properties and reverses cognitive impairment.
T79372 A3AR agonist 1

Adenosine Receptor GPCR/G Protein; Neuroscience
A3AR拮抗剂1(化合物12)是一种选择性的A3AR激动剂,其Ki值为25.8 nM。该化合物能有效促进β-arrestin2的募集,表现出EC50为5.17 nM的高亲和力。A3AR拮抗剂1主要用于炎症性疾病、缺血、癌症、神经性疼痛和肝脏疾病等方面的科研。
T61180 GAT564

GAT564 (Compound 15d) is a highly effective allosteric modulator of cannabinoid 1 receptor (CB1R), having EC50 values of 87 nM and 320 nM for cAMP and β-arrestin2, respectively. It significantly enhances the binding of orthosteric ligands to hCB1R. Moreover, GAT564 exhibits remarkable efficacy as a topical agent, resulting in a significant reduction of intraocular pressure (IOP) in an ocular normotensive murine model of glaucoma [1].
T76223 NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)

NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) (化合物 39) 作为APJ激动剂表现出高亲和力,其Ki值为0.6 nM。该化合物能有效激活Gαi1,具有EC50值0.8 nM,并能募集β-arrestin2,相关EC50值为31 nM。同时,NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) 对心脏功能具有显著的延长作用。
T75801 TC14012 TFA

TC14012 TFA 是 T140 的血清稳定衍生物,是一种选择性的 CXCR4拮抗剂,IC50为 19.3 nM。TC14012 TFA 是有效的 CXCR7激动剂,可将 β-arrestin2 募集到 CXCR7,EC50为 350 nM。TC14012 TFA 具有抗 HIV 活性和抗癌活性。
T14498 Barbadin

Arrestin GPCR/G Protein
Barbadin 是一种新型且具有特异性的 β-arrestin/β2-adaptin 相互作用抑制剂,对β-arestin1 的 IC50 值为 19.1 μM,对β-arestin2 的 IC50 值为 15.6 μM。Barbadin 增强氯卡色林对 POMC 神经元和减肥的长期影响,可阻断激动剂促进的原型 β2-肾上腺素能、V2-血管加压素和血管紧张素-II-1 型受体的内吞,可用于研究肥胖。

化合物

Indacaterol
Cat.No: T2320
Synonym:
Target: Adrenergic Receptor
Indacaterol maleate
Cat.No: T1239
Synonym: 马来酸茚达特罗,QAB149
Target: Adrenergic Receptor
VUF11207 fumarate
Cat.No: T13324
Synonym:
Target: CXCR, Arrestin
ELA-14(human) acetate
Cat.No: TP1923L1
Synonym: ELA-14(human) acetate (1886973-05-2 free base)
Target: Apelin receptor, Arrestin
58-G3
Cat.No: T23583
Synonym: 58G3
Target:
VUF14480
Cat.No: T70403
Synonym:
Target:
A3AR agonist 2
Cat.No: T79373
Synonym:
Target: Adenosine Receptor
(–)-IHCH7041
Cat.No: T69513
Synonym:
Target:
A3AR agonist 1
Cat.No: T79372
Synonym:
Target: Adenosine Receptor
GAT564
Cat.No: T61180
Synonym:
Target:
NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)
Cat.No: T76223
Synonym:
Target:
TC14012 TFA
Cat.No: T75801
Synonym:
Target:
Barbadin
Cat.No: T14498
Synonym:
Target: Arrestin
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