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。 | |||
T27405 |
GAT211
AZ4,GAT-211,AZ 4,GAT 211,AZ-4 |
cAMP; Cannabinoid Receptor; Arrestin | GPCR/G Protein |
GAT211 (AZ-4) 是一种具有选择性和高效性的大麻素 1 受体 (CB1R) 正变构调节剂 (PAM),对 cAMP 和 β-arrestin2 具有较高的亲和力。GAT211 具有降眼压和抗精神病的作用,可用于研究癫痫。 | |||
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。 | |||
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。 | |||
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 |
Others | Others |
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
|
Others | Others |
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
|
Others | Others |
(–)-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. | |||
T61180 |
GAT564
|
Others | Others |
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]. | |||
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。 | |||
T76223 |
NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)
|
Others | Others |
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。 |