首页工具

登录

搜索结果

Search Results for " gpcrs "

如果没找到您满意的产品或者您对产品有其他要求，可以联系我们专业顾问为您提供针对性的合理建议。 QQ咨询网站留言咨询

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。
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。
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。
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。
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。
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
	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.
T39976	MS67
	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.
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.
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
T37907	DL 175
	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.
T37131	MS 15203
	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...
T41159	NCT 501 hydrochloride
	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.
T77789	Oleoyl-L-alpha-lysophosphatidic acid sodium salt LPA sodium salt
	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。
T35804	C16 Lactosylceramide (d18:1/16:0)
	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.
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
	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
T68356	AM-3189
	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
	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...
T37283	1-Palmitoyl Lysophosphatidic Acid (sodium salt)
	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...
T36578	Boc-Lys(Ac)-AMC
	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。

化合物

Cat.No: T8642

Target: GPR

Cat.No: T24850

Synonym: CMPD103A,Takeda-103A,Takeda-103-A,CMPD-103A,Takeda 103 A

Target: GRK

N-phenylthiophene-2-carboximidamide

Cat.No: T50088

Target: Others

Cat.No: T3306

Synonym: PF 04418948,PF04418948

Target: Prostaglandin Receptor

Cat.No: T9146

Synonym: Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-

Target: Others

Cat.No: T3360

Synonym: ZK756326 2HCl

Target: CCR

Cat.No: T17243

Synonym: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide

Target: Potassium Channel

PRX-07034 hydrochloride

Cat.No: T8720

Synonym: PRX-07034

Target: 5-HT Receptor

Cat.No: T29120

Synonym: VU 0029767,VU-0029767

Cat.No: T39976

Cat.No: T10281

Synonym: Trimeprazine

Target: Others

Cat.No: TP2086

Cat.No: T37907

Cat.No: T37131

NCT 501 hydrochloride

Cat.No: T41159

Oleoyl-L-alpha-lysophosphatidic acid sodium salt

Cat.No: T77789

Synonym: LPA sodium salt

C16 Lactosylceramide (d18:1/16:0)

Cat.No: T35804

Argipressin diacetate

Cat.No: T75708

Cat.No: T31995

Synonym: GRC17536,GRC 17536

Cat.No: T68356

Cat.No: T70039

1-Palmitoyl Lysophosphatidic Acid (sodium salt)

Cat.No: T37283

Boc-Lys(Ac)-AMC

Cat.No: T36578

Angiotensin II human TFA

Cat.No: T74142

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Copyright © 2015-2024 TargetMol Chemicals Inc. All rights reserved. 沪ICP备20019793号-4

沪公网安备 31010602006700号

沪公网安备 31010602006700号

TargetMol Loading

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼