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Cat. No. | Product Name | ||
---|---|---|---|
L1500 | GPCR靶点分子库 | 1940 compounds | |
1940 种与 G 蛋白及其耦联受体相关的生物活性小分子化合物,所有小分子都具有良好的生物和药理活性,部分是 FDA 批准的上市药物; | |||
L1580 | GPCR库Plus | 338 compounds | |
338 种GPCR 靶向、结构新颖的化合物; | |||
L2600 | 神经信号分子库 | 2540 compounds | |
2540 种CNS 相关的生物活性小分子化合物的特有集合,用于高通量、高内涵筛选; | |||
L7600 | 趋化因子抑制剂库 | 59 compounds | |
59 种趋化因子或其受体抑制剂的独特集合,可用于高通量筛选和高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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)。 | |||
T24850 |
Takeda103A
CMPD103A,Takeda-103A,Takeda-103-A,CMPD-103A,Takeda 103 A |
GRK | GPCR/G Protein |
Takeda103A (CMPD103A) 是 GRK2抑制剂。G 蛋白偶联受体是许多生理过程的核心。Takeda103A 对研究心力衰竭具有潜在的研究价值。 | |||
T50088 |
N-phenylthiophene-2-carboximidamide
|
Others | Others |
N-phenylthiophene-2-carboximidamide 是一种噻吩衍生物,可以作为蛋白酪氨酸激酶(PTKs)的抑制剂和 G 蛋白偶联受体(GPCR)的配体发挥作用。 | |||
T9146 |
ms48107
Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro- |
Others | Others |
MS48107 是 G 蛋白偶联受体 68 (GPR68) 的选择性正变构调节剂,对GPR68的选择性高于密切相关的神经递质转运蛋白,质子 GPCR 和 hERG 离子通道。它可以穿越过小鼠的血脑屏障。 | |||
T3306 |
PF-04418948
PF 04418948,PF04418948 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
PF-04418948 是一种可口服的,选择性的前列腺素EP2受体拮抗剂,IC50为16 nM。 | |||
T17243 |
VU0463271
N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide |
Potassium Channel | Membrane transporter/Ion channel |
VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) 是一种有效的、特异性的 KCC2 拮抗剂,其 IC50 为 61 nM,特异性是密切相关的 Na-K-2Cl 协同转运蛋白 1 (NKCC1) 的 100 倍以上,在更大的 GPCR、离子通道和转运蛋白面板中没有活性。 | |||
T3360 |
ZK 756326
ZK756326 2HCl |
CCR | Immunology/Inflammation; Microbiology/Virology |
ZK 756326 是一种选择性的非肽 CCR8 趋化因子受体激动剂(IC50:1.8 μM,在人体内;2.6 μM,在小鼠体内)。对 CCR4/5 和 CXCR3/4 没有活性,比其他 26 种 GPCR 的选择性高 28 倍(对 α2A 和 5-HT 受体的选择性较低)。诱导趋化性并抑制 Env 介导的 (HIV) 细胞-细胞融合。 | |||
T8720 |
PRX-07034 hydrochloride
PRX-07034 |
5-HT Receptor | GPCR/G Protein; Neuroscience |
PRX-07034 hydrochloride 是一种有效的高度选择性5-HT6受体拮抗剂,Ki 为 4-8 nM,IC50为 19 nM,可用于增强工作记忆和认知灵活性的研究。 | |||
T29120 |
VU0029767
VU 0029767,VU-0029767 |
Others | Others |
VU0029767 is a selective positive allosteric modulator of M1, a member of the muscarinic acetylcholine family of GPCRs (mAChRs). VU0029767 increases potency and efficacy of acetylcholine (ACh) at M1. | |||
T10281 |
Alimemazine
Trimeprazine |
Others | Others |
Alimemazine (Trimeprazine) is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist. Alimemazine also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. | |||
T39976 |
MS67
|
PROTACs | PROTAC |
MS67 is a potent and selective degrader of the WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM. It exhibits no activity against protein methyltransferases, kinases, G-protein-coupled receptors (GPCRs), ion channels, and transporters. Notably, MS67 demonstrates significant anticancer properties. | |||
TP2086 |
AdTx1
|
||
Selective, high affinity, non-competitive α1A adrenoceptor antagonist (Ki = 0.35 nM). Exhibits no significant activity against a range of other GPCRs, including α2A, β1 and β2 adrenoceptors. Antagonizes effects of phenylephrine on isolated rabbit prostate | |||
T41159 |
NCT 501 hydrochloride
|
Others | Others |
NCT 501 hydrochloride is a potent and selective ALDH1A1 inhibitor (IC50 = 40 nM). Exhibits >1000-fold selectivity for ALDH1A1 over ALDH3A1, ALDH1B1, ALDH2, HPGD and HSD17β4. Also selective over a panel of 168 GPCRs. Blood-brain barrier permeable. | |||
T35804 |
C16 Lactosylceramide (d18:1/16:0)
|
Others | Others |
C16 Lactosylceramide is an endogenous bioactive sphingolipid. It forms membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs), suggesting a role in cell signaling. Plasma levels of C16 lactosylceramide are elevated in insulin-resistant cattle. C16 Lactosylceramide is also upregulated in a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder. | |||
T37131 |
MS 15203
|
Others | Others |
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... | |||
T37907 |
DL 175
|
Others | Others |
Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bone marrow-derived macrophages (BMDMs) in a cellular impedance assay, and promotes phagocytosis by M1 polarized U937 cells. Induces migration of primary human monocytes, but has no effect on macrophage chemotaxis. | |||
T77789 |
Oleoyl-L-alpha-lysophosphatidic acid sodium salt
LPA sodium salt |
Others | Others |
Oleoyl-L-alpha-lysophosphatidic acid sodium salt为必需的细胞膜生物合成代谢物,可通过与G蛋白偶联受体(GPCR)(即LPA受体)相互作用来介导信号传导,是LPA1和LPA2受体的内源性激动剂。 | |||
T75708 |
Argipressin diacetate
|
||
Argipressin (diacetate) (AVP (diacetate),又称antidiuretic hormone (ADH)) 是一种由垂体后叶分泌的含9个氨基酸的神经肽。通过作用于三种G蛋白偶联受体(GPCRs),Avpr1a (V1a)、Avpr1b (V1b) 及Avpr2 (V2),它调控体液平衡、渗透压及心血管系统的生理功能,并可能对中枢代谢过程产生重要影响。 | |||
T31995 |
GRC-17536
GRC17536,GRC 17536 |
Others | Others |
GRC-17536 is an orally available, potent, and selective transient receptor potential anchor protein 1 (TRPA1) inhibitor that has been shown to be highly effective in the treatment of inflammation and neuropathic pain in animal models. The selectivity of G | |||
T37283 |
1-Palmitoyl Lysophosphatidic Acid (sodium salt)
|
Others | Others |
1-Palmitoyl lysophosphatidic acid (1-Palmitoyl LPA) is a LPA analog containing palmitic acid at the sn-1 position. LPA binds to one of five different G protein-coupled receptors (GPCRs) to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell motility. In addition to playing a role in the aforementioned biological responses, 1-palmitoyl LPA enhances the action of β-lactam antibiotics (ampicillin, pipe... | |||
T68356 |
AM-3189
|
Others | Others |
AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good oral bioavai... | |||
T70039 |
BIM-46174
|
Others | Others |
BIM-46174 is a New Inhibitor of the Heterotrimeric Gα/Gβγ Protein Complex. BIM-46174 acts as a selective inhibitor of heterotrimeric G-protein complex. BIM-46174 prevents the heterotrimeric G-protein signaling linked to several GPCRs mediating (a) cyclic AMP generation (Gαs), (b) calcium release (Gαq), and (c) cancer cell invasion by Wnt-2 frizzled receptors and high-affinity neurotensin receptors (Gαo/i and Gαq). BIM-46174 inhibits the growth of a large panel of human cancer cell lines, includ... | |||
T36578 |
Boc-Lys(Ac)-AMC
|
Others | Others |
Commendamide (N-acyl-3-hydroxypalmitoyl-glycine) is a newly discovered GPCR G2A/GPR132 agonist (EC50=11.8 μM) that isolated from Bacteroides vulgatus. [1] G2A/GPR132 belongs to the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily. GPR132/G2A is first reported to be a transcriptional target for BCR-ABL tyrosine kinase attenuating B-cell expansion in vitro and arresting cells at G2 during mitosis. It has been involved in autoimmune disease and atherosclerosis. [1]... | |||
T74142 |
Angiotensin II human TFA
|
||
Angiotensin II human (Angiotensin II) TFA 作为肾素/血管紧张素系统中关键的生物活性肽,扮演着血管收缩剂的角色并在调节人体血压中发挥中心作用。其主要通过与 G 蛋白偶联受体 (GPCRs)、血管紧张素 II 1型受体 (AT1R) 和血管紧张素 II 2型受体 (AT2R) 的相互作用来介导效应,包括刺激交感神经系统、增加醛固酮的生物合成和肾脏功能。此外,Angiotensin II human TFA 促进血管平滑肌细胞的生长和 I 型及 III 型胶原在成纤维细胞中的合成,导致血管壁与心肌增厚及纤维化,并诱导细胞凋亡。还通过LOX-1依赖的氧化还原敏感路径诱导内皮细胞中的毛细血管形成。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-01422 |
GNAS Protein, Human, Recombinant (His & SUMO)
Guanine nucleotide-binding protein G(s) subunit alpha isofor... |
Human | E. coli |
Guanine nucleotide-binding proteins (G proteins) function as transducers in numerous signaling pathways controlled by G protein-coupled receptors (GPCRs). Signaling involves the activation of adenylyl cyclases, resulting in increased levels of the signaling molecule cAMP. GNAS functions downstream of several GPCRs, including beta-adrenergic receptors. Stimulates the Ras signaling pathway via RAPGEF2. GNAS Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6... | |||
TMPY-04270 |
GPR133 Protein, Human, Recombinant (His)
PGR25,GPR133 |
Human | HEK293 Cells |
ADGRD1 (Adhesion G Protein-Coupled Receptor D1, also known as GPR133) is a Protein Coding gene. 4 alternatively spliced human isoforms have been reported. ADGRD1, an orphan member of the adhesion family of G-protein-coupled receptors, is a critical regulator of the response to hypoxia and tumor growth in Glioblastoma (GBM). ADGRD1 represents a novel molecular target in GBM and possibly other malignancies where hypoxia is fundamental to pathogenesis. Variations in the ADGRD1 locus are linked with... | |||
TMPK-00895 |
Tubby Protein, Human, Recombinant (His)
TUB,RD5,RDOB |
Human | E. coli |
Tubby is the founding member of the tubby-like family of proteins. Tubby-like proteins (TLPs) possess a highly conserved closed β barrel tubby domain at C-terminal and N-terminal F-box.Tubby plays a critical role in trafficking select GPCRs to the cilia. | |||
TMPY-02837 |
GPR114 Protein, Human, Recombinant (hFc)
PGR27,GPR114 |
Human | HEK293 Cells |
GPR114 belongs to the G-protein coupled receptor 2 family. Members of this family share a common molecular architecture which consists of seven transmembrane domains, three extracellular loops, three intracellular loops, an amino-terminal extracellular domain, and an intracellular carboxyl terminus. It is thought that light acts as the activating stimulus of a G-protein-coupled receptor (GPCR). GPCRs are expected to have a molecular function (G-protein coupled receptor activity) and to localize ... | |||
TMPY-04058 |
RGS5 Protein, Human, Recombinant (His)
MST106,MSTP032,MST092,regulator of G-protein signaling 5,MST... |
Human | E. coli |
RGS5 is a member of the RGS superfamily and acts as a negative regulator of heterotrimeric G protein-mediated signalling through G protein-coupled receptors (GPCRs). The regulator of G-protein signaling (RGS) proteins have recently been identified as signal transduction molecules which have structural homology to SST2 of Saccharomyces cerevisiae and EGL-10 of Caenorhabditis elegans. The messenger RNA of hRGS5 was abundantly expressed in heart, lung, skeletal muscle, and small intestine, and at l... |