Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8868 |
4BP-TQS
|
AChR | Neuroscience |
4BP-TQS 是 α7nAChR 变构激动剂。它利用变构跨膜位点激活 nAChRs。 | |||
T10573 |
BMT-145027
|
GluR | Neuroscience |
BMT-145027 是一种 mGluR5 的正变构调节剂,没有内在的激动剂活性 (EC50 = 47 nM)。 | |||
T3565 |
VU0155041
UV0155041,VU-0155041 |
GluR | Neuroscience |
VU0155041 是一种选择性的mGluR4正变构调节剂,有用于帕金森病的研究潜力,对人和大鼠 mGluR4 的EC50值分别为 798 和 693 nM。 | |||
T17300 |
(-)-(S)-B-973B
|
AChR | Neuroscience |
(-)-(S)-B-973B 是一种有效的别构激动剂和 α7 nAChR 的正向别构调节剂,可用于缓解疼痛的研究。 | |||
T1760 |
TBPB
|
AChR | Neuroscience |
TBPB 是变构 M1 mAChR 激动剂,EC50值为289nM,可在大鼠中调节淀粉样蛋白加工并产生抗精神病样活性。 | |||
T11458 |
GPR40/FFAR1 modulator 1
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
GPR40/FFAR1 modulator 1是一种针对Gq偶联的游离脂肪酸受体1 (GPR40/FFAR1) 的激动剂以及异构调节剂。 | |||
T3961 |
CYM-5541
CYM 5541,ML249,CID-17253208 |
S1P Receptor; LPL Receptor | GPCR/G Protein |
CYM-5541 (ML249) 是一种选择性的S1P3受体变构激动剂,EC50值在72至132 nM 之间。 | |||
T6575 |
LY2119620
|
AChR | Neuroscience |
LY2119620 是人 M2 和 M4 毒蕈碱乙酰胆碱受体的特异性变构激动剂。 | |||
T8403 |
Cinacalcet
西那卡塞,AMG 073 |
CaSR | GPCR/G Protein |
Cinacalcet (AMG 073) 是口服有活性的Ca receptor (CaR)激动剂,用于研究心血管疾病。 | |||
T12192 |
NCGC00229600
|
Others; TSH Receptor | GPCR/G Protein; Others |
NCGC00229600 是促甲状腺激素受体 (TSHR) 的变构反向激动剂。 NCGC00229600 抑制 TSH 和刺激 TSHR 的内源性激活抗体,可用于格雷夫斯病的研究。 | |||
T8642 |
4-CMTB
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
4-CMTB 是选择性的游离脂肪酸受体 2(FFA2/GPR43)的激动剂以及正变构调节剂 (pEC50=6.38)。 | |||
T22703 |
CYM-5520
CYM 5520 |
S1P Receptor; LPL Receptor | GPCR/G Protein |
CYM-5520 是一种选择性的变构鞘氨醇 1-磷酸受体 2 (S1PR2) 激动剂,EC50为 480 nM。它可以在 S1PR2 受体中与 S1P 结合,可用于骨质疏松症研究。 | |||
T2635 |
Org 27569
|
Cannabinoid Receptor | GPCR/G Protein |
Org 27569 是一种 CB1 receptor 别构调节剂,可以增加激动剂与 CB1 结合,能够抑制激动剂诱导的 CB1 信号通路。 | |||
T10814 |
Cinacalcet metabolite M4
3-三氟甲基苯丙胺,Rarechem AL BW 1078 |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Cinacalcet metabolite M4 (Rarechem AL BW 1078) 是 Cinacalcet 的代谢物。Cinacalcet 是具有活性的 Ca receptor 激动剂,可用于心血管疾病。 | |||
T8224 |
VU0119498
|
AChR | Neuroscience |
VU0119498 是泛 GqmAChR M1、M3和M5的正变构调节剂,具有抗糖尿病活性,EC50值分别为 6.04、6.38 和 4.08 µM。 | |||
T22301 |
L-838417 D9
CTP354,CTP354 (C-21191),C-21191 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
L-838417 D9 (C-21191) 是 L-838417 的氘代物。其中L-838417 是亚型选择性GABAA 正变构调节剂,在 α2, α3 和 α5 亚型中作为部分激动剂。 | |||
T7165 |
Basmisanil
RG1662,RO5186582,巴米沙尼 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Basmisanil (RG1662) 是高度选择性GABAAα5负调节剂,用于治疗与唐氏综合症相关的认知障碍。 | |||
T12165 |
nAChR agonist 1
DUN71755 |
AChR | Neuroscience |
nAChR agonist 1 (DUN71755) 是一种脑渗透性和口服有效的正变构 α7 烟碱乙酰胆碱受体 (α7 nAChR) 调节剂。它在 Ca2+中,对内源性表达 α7 nAChR 的人 IMR-32 神经母细胞瘤细胞的EC50为 0.32 μM。它可用于阿尔茨海默病的研究。 | |||
T15363 |
FzM1.8
|
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
FzM1.8 是变构 FZD4 激动剂,pEC50 为 6.4。 FzM1.8 与 FZD4 结合,在没有任何 WNT 配体的情况下促进 TCF/LEF 转录活性,并激活 WNT/β-catenin 通路[1]。 | |||
T9180 |
LUF6096
CF-602 |
Adenosine Receptor | GPCR/G Protein; Neuroscience |
LUF6096 (CF-602) 是一种有效的腺苷 A3 受体 (adenosine A3 receptor) 变构增强剂。LUF6096 对任何腺苷受体显示出低正构亲和力。LUF6096 在心肌缺血/再灌注损伤中显示出保护作用。 | |||
T21935L |
AMN082 free base
AMN082 |
GluR | Neuroscience |
AMN082 free base 是 mGluR7选择性激动剂,口服有活性,能够透过血脑屏障,可通过跨膜区的变构位点直接激活受体信号。在表达 mGluR7 的转染哺乳动物细胞上,它能够有效抑制 cAMP 积累并刺激 GTPγS 结合。它能够选择性针对 mGluR 的其他亚型及选择性离子型谷氨酸受体。具有抗抑郁活性。 | |||
T6764L |
ATI-2341 acetate(1337878-62-2 free base)
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
ATI-2341 acetate(1337878-62-2 free base) 是一种有效的 CXCR4 变构激动剂,它激活 Gα1 而不是 Gα13。 ATI-2341 acetate 激活抑制性异源三聚体 G 蛋白 (GI) 以促进对 cAMP 产生的抑制并诱导钙动员。 | |||
T16378 |
Ogerin
|
Others; 5-HT Receptor; Adenosine Receptor | GPCR/G Protein; Neuroscience; Others |
Ogerin 是选择性 GPR68正向别构调节剂(pEC50:6.83)。它能够抑制小鼠对恐惧记忆的回忆。它对 A2A 受体具有适中的拮抗作用(Ki:220 nM)。对 5-HT2B 受体的拮抗作用较弱(Ki:736 nM)。 | |||
TP1939L1 |
RVD-Hpα acetate(1193362-76-3 free base)
|
Cannabinoid Receptor | GPCR/G Protein |
RVD-Hpα acetate(1193362-76-3 free base) 是人血加压素的 N 末端延伸形式,可作为选择性 CB1 受体激动剂。增加体外表达 CB1 受体的细胞中的细胞内 Ca2+ 水平。也是高亲和力 CB2 正变构调节剂 (Ki = 50 nM)。 | |||
T15275 |
Fenobam
|
GluR | Neuroscience |
Fenobam 是可口服的、可穿过血脑屏障的 mGluR5拮抗剂,具有抗焦虑活性,在大鼠和人重组 mGlu5 受体上的 Kd 值分别 54 和 31 nM。它有反向激动剂活性,可阻断 mGlu5 受体活性,IC50为 84 nM。 | |||
T23507 |
VU0155041 sodium
VU 0155041 sodium salt |
Others | Others |
positive allosteric modulator/allosteric agonist of mGlu4 receptor | |||
T26541 | AC-42 | ||
AC-42 is an allosteric agonist of M1 muscarinic receptor. | |||
T29136 |
VU0424465
VU 0424465,ML273,ML-273,VU-0424465,ML 273 |
||
VU0424465 is a mGlu5-selective allosteric agonist. | |||
T24770 |
SCH-202676 HBr
SCH 202676 Hydrobromide,SCH202676 Hydrobromide,SCH-202676 Hydrobromide |
||
SCH-202676 HBr is an allosteric agonist. It also an GPCR antagonist. | |||
T28986 |
TMPPAA
|
||
TMPPAA is an allosteric agonist of 5-HT3 receptor. | |||
T68308 | GSK-1034702 HCl | ||
GSK-1034702 HCl is a potent M1 receptor allosteric agonist. | |||
T14092 |
AC260584
|
Others | Others |
AC260584 is an M1 muscarinic receptor allosteric agonist (pEC50: 7.6). | |||
T23934 |
D36
D 36,D-36 |
||
D36 is an androgen receptor allosteric antagonist. It also has inverse agonist properties. | |||
T13379 |
(Z)-Leukadherin-1
ADH-503 free base |
Complement System | Immunology/Inflammation |
(Z)-Leukadherin-1 (ADH-503 free base) 是 CD11b 的变构激动剂。 | |||
T11912 | LY3154207 | Others | Others |
LY3154207 is a subtype selective, potent, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM). | |||
T28261 |
Org27759
Org-27759,Org 27759 |
||
Org27759, an allosteric modulator of the CB1 receptor, significantly increases the binding of the CB1 receptor agonist. | |||
T28262 | Org-29647 | ||
Org-29647, an allosteric modulator of the CB1 receptor, significantly increases the binding of the CB1 receptor agonist. | |||
T70301 |
GAT100
|
||
GAT100 is a potent and covalent negative allosteric modulator (NAM). GAT-100 behaved as a robust positive allosteric modulator of binding of orthosteric agonist CP55,940. This novel covalent probe can serve as a useful tool for characterizing CB1R allosteric ligand-binding motifs. | |||
T27446 |
GSK-1034702
GSK-1034702 HCl,GSK 1034702 |
||
GSK-1034702 is a selective M(1) receptor allosteric agonist, it may have therapeutic benefits in disorders of impaired learning including Alzheimer's disease. | |||
T39140 | SCO-267 | ||
SCO-267 is a potent allosteric full agonist of the GPR40 receptor, making it a valuable tool in studying chronic diseases like diabetes. | |||
T13550 |
AP5
|
Others | Others |
AP5 is a potent and selective agonist for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49 nM against the GPR40 receptor. | |||
T61775 |
mGlu4 receptor agonist 1
|
||
mGlu4 receptor agonist 1 (compound 62) is a highly effective positive allosteric modulator of mGlu4 receptors, displaying an EC 50 of 308 nM. Additionally, it exhibits noteworthy anxiolytic and antipsychotic properties [1]. | |||
T28928 |
TASP0433864
|
||
TASP0433864 is a positive allosteric modulator of metabotropic glutamate 2 receptor with EC50 values of 199 and 206 nM at human and rat mGlu2 receptors, respectively, without exerting agonist activity at rat mGlu2 receptor. | |||
T37896 |
AZ 1729
|
||
FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel... | |||
T60497 | MRGPRX1 agonist 3 | ||
MRGPRX1 agonist 3 (compound 1f) 是一种有效的正向变构调节剂,对Mas 相关 G 蛋白偶联受体 X1 (MRGPRX1)的EC50值为 0.22 μM,可用于研究神经性疼痛。 | |||
TP1939 |
RVD-Hpα
|
||
N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2 positive allosteric modulator (Ki = 50 nM). | |||
T80489 |
MmTx1 toxin
Micrurotoxin 1 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
MmTx1毒素是一种调节变构性GABAA受体活性的化合物,它能够提升GABAA受体对激动剂的反应性。 | |||
T72835 |
FSHR agonist 1
|
||
FSHR agonist 1是一种对卵泡刺激素(FSH)受体(FSHR)具有高亲和力并能引起变构的激动剂,具有pEC50值为7.72。它通过与TMD广泛相互作用直接激活FSHR。 | |||
T78090 |
CVN636
|
||
CVN636,作为口服有效的选择性mGluR7变构激动剂,其对humGluR7的EC50为7 nM,并显示出良好的中枢神经系统(CNS)通透性。 | |||
T60466 |
MRGPRX1 agonist 2
|
||
MRGPRX1 agonist 2 (compound 1a) 是有效的Mas 相关 G 蛋白偶联受体 X1 (MRGPRX1)的正变构调节剂(EC50 = 0.48 μM)。MRGPRX1 agonist 2 具有用于神经性疼痛的研究潜力。 |