42
4
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T40685L |
Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate
Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate (600171-70-8 Free base) |
Others | Others |
Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate (Orphan GPCR SP9155 agonist P550 ) 是具有促食欲作用的 RFamide 肽家族的成员。 | |||
T60074 |
GPCR agonist-2
4-(Cyclopropylamino)-3-nitrobenzoic acid |
GPR | Endocrinology/Hormones; GPCR/G Protein |
GPCR agonist-2 (4-(Cyclopropylamino)-3-nitrobenzoic acid) 是人源 GPCR GPR109B 的激动剂。 | |||
T40685 |
Orphan GPCR SP9155 agonist P550 (mouse, rat)
26RFa (mouse, rat),Orphan GPCR SP9155 agonist P550 (mouse, rat) |
||
Orphan GPCR SP9155 agonist P550 (mouse, rat) (26RFa (mouse, rat)) is an orphan GPCR with an orexigenic effect belonging to the RFamide peptide family. It acts as the cognate ligand for the mouse orphan receptor GPR103, which is also known as SP9155 or AQ27. | |||
T9407 |
Rasarfin
|
Others; Ras | GPCR/G Protein; MAPK; Others |
Rasarfin 是Ras 和ARF6双抑制剂。 | |||
T9357 |
Ro 5212773
Epptb |
Others | Others |
Ro 5212773 (Epptb) 是TAAR1的选择性拮抗剂(对于小鼠 TAAR1 的Ki= 0.9 nM),对其他 TAARs 没有显著影响。其中TAAR1 是一种 G 蛋白偶联受体 (GPCR),能够被内源性氨基酸代谢产物非选择性的激活。 | |||
T21874 |
CID 2745687
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
CID 2745687 是可逆的、特异性 GPR35竞争性拮抗剂(Ki:12.8 nM)。 | |||
T8329 |
AR 231453
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
AR 231453 是一种口服具有活性的、特异性的 GPR119激动剂。它能够刺激细胞增殖,改善胰岛 β 细胞的功能。 | |||
T15432 |
GSK256073
|
GPR; Others | Endocrinology/Hormones; GPCR/G Protein; Others |
GSK256073 是一种口服有活性的GPR109A 选择性激动剂,也是一种持久的人HCA2激动剂(pEC50:7.5) 。它能够减少脂降解,而显著改善葡萄糖稳态,对 2 型糖尿病和血脂异常具有潜在的研究价值。 | |||
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。 | |||
T2613 |
Almorexant
阿莫伦特,ACT 078573 |
OX Receptor | GPCR/G Protein; Neuroscience |
Almorexant (ACT 078573) 是一种有效的竞争性食欲素 1 受体 (OX1)/食欲素 2 受体 (OX2) 双重拮抗剂,OX1 和 OX2 的 Ki 值分别为 1.3 和 0.17 nM。 | |||
T6155 |
Almorexant hydrochloride
ACT-078573 hydrochloride,Almorexant HCl |
OX Receptor | GPCR/G Protein; Neuroscience |
Almorexant hydrochloride (ACT-078573 hydrochloride) 是一种有效的竞争性食欲素 1 受体(OX1)/食欲素 2 受体 (OX2) 双重拮抗剂,OX1 和 OX2 的 Ki 值分别为 1.3 和 0.17 nM。 | |||
T12684 |
Radioprotectin-1
5-chloro-2-[4-(1,3-dioxobenzo[de]isoquinolin-2-yl)butylsulfamoyl]benzoic acid |
LPA Receptor | GPCR/G Protein |
Radioprotectin-1 是特异性的 LPA2 激动剂,对小鼠 LPA2 GPCR 的 EC50 为 25 nM,具有辐射保护和辐射缓解作用。 | |||
T10363 |
Arazine
N-Acetyl-S-farnesyl-L-cysteine |
Others | Others |
Arazine (N-Acetyl-S-farnesyl-L-cysteine) 可以成为异戊二烯基半胱氨酸甲基转移酶的底物通过与异戊二烯化 G 蛋白或其受体位点竞争。 Arazine 是 G 蛋白和 GPCR 信号传导的细胞渗透性调节剂。 | |||
T9162 |
CID1231538
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
CID1231538 是一种苯并噻唑类似物,是 GPR35拮抗剂。其中 GPR35 是一种 G 蛋白偶联受体 (GPCR)。 | |||
T3433 |
TUG-891
TUG 891,TUG891 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
TUG-891 是一种选择性的长链游离脂肪酸受体 4 (FFA4/GPR120) 的激动剂。 | |||
T3119 |
JNJ-63533054
JNJ 63533054 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
JNJ-63533054 是一种选择性的,具有口服活性的GPR139激动剂,对人GPR139的EC50为 16 nM。它可穿过血脑屏障,对 GPR139 的选择性高于其他 GPCR、离子通道和转运蛋白。 | |||
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。 | |||
T8423 |
ML417
|
Dopamine Receptor; Arrestin | GPCR/G Protein; Neuroscience |
ML417 是选择性的,可透过血脑屏障的 D3 多巴胺受体激动剂,EC50=38 nM。它能够促进 D3R 介导的 β-arrestin 易位、G 蛋白介导的信号传导和 pERK 磷酸化,对其他 GPCR 介导的信号传导影响小。它对毒素诱导的多巴胺能神经元变性具有神经保护活性。 | |||
T10843 |
CMF019
|
Apelin receptor | GPCR/G Protein |
CMF019 是一种有效的小分子 Apelin receptor (APJ) 激动剂,具有 G protein 偏向性。 CMF019 在人,大鼠和小鼠中与 APJ 结合的 pKi 值分别为 8.58、8.49 和 8.71。CMF-019 在啮齿动物中的有益于心血管。 Apelin 受体 (APJ) 是由内源性肽 apelin 激活的 G 蛋白偶联受体(GPCR)。 | |||
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。 | |||
T24770 |
SCH-202676 HBr
SCH 202676 Hydrobromide,SCH202676 Hydrobromide,SCH-202676 Hydrobromide |
||
SCH-202676 HBr is an allosteric agonist. It also an GPCR antagonist. | |||
T69774 | VUF14738 | ||
VUF14738 is a robust and fatigue-resistant photoswitchable GPCR antagonist. | |||
T26962 |
CBP-307
CBP307 |
||
CBP-307 is a selective second generation S1P1 (a G-protein coupled receptor -GPCR) modulator. | |||
T83743 |
VPM-p15 TFA
T1V/F3Phe(4-Me) |
||
VPM-p15是一种合成多肽激动剂,针对粘附G蛋白偶联受体(GPCR) G2 (ADGRG2)而设计,ADGRG2是一种孤儿GPCR,与男性不育有关。在表达人类ADGRG2的HEK293细胞中,它能诱导cAMP积累(EC50 = 1.41 µM)。 | |||
T69775 |
VUF14862
|
||
VUF14862 is a robust and fatigue-resistant photoswitchable GPCR antagonist. | |||
T27428 |
GP-1681
GP 1681,GP1681 |
||
GP-1681, a G-protein coupled receptor (GPCR) agonist, is used potentially for the treatment of influenza infection. | |||
TP1279 |
Neurokinin B (TFA)
神经激肽 B 三氟乙酸盐,Neurokinin B TFA |
||
Neurokinin B TFA belongs to the tachykinin family.Neurokinin B binds to a series of GPCR, including neurokinin receptors 1 (NK1R), NK2R, and nk3r, to modulate their biological effects | |||
T73005 |
PF-07054894
|
||
PF-07054894 是一种有效的 CCR6拮抗剂。 PF-07054894 靶向 G 蛋白偶联受体 (GPCR)。 PF-07054894 可用于炎症性肠病的研究。 | |||
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]... | |||
T69953 | MK-8666 Tris | ||
MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects. | |||
T63340 |
CCG-273220
|
||
CCG-273220 是 G 蛋白偶联受体 (GPCR) 激酶 5 (GRK5) 共价抑制剂 (IC50: 220 nM)。CCG-273220 可以共价结合GRK5亚家族特异性残基 Cys474 ,而对GRK5的选择性比 GRK2 高。 | |||
T70468 | MK-8666 | ||
MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects. | |||
T81683 |
Neuromedin S (human)
|
||
Neuromedin S (human) 是包含33个氨基酸的神经肽,作为G 蛋白偶联受体 (GPCR) FM-4/TGR-1的内源性配体,在大脑中被鉴定,并对神经调节素 U (NMU) 受体 2 (NMUR2)调节体重稳态具有调控作用。 | |||
T4186 |
AC-264613
AC264613 |
Protease-activated Receptor | GPCR/G Protein |
AC-264613 是一种选择性蛋白酶激活受体 (PAR-2) 激动剂,pEC50为 7.5。 | |||
TP1946 |
QWF
|
||
Tripeptide substance P (SP) antagonist (IC50 = 90 μM). Also inhibits binding of SP to Mas-related GPCR (MRGPR) X2. Inhibits SP-induced IgE-independent degranulation of mast cells in vitro. Inhibits compound 48/80-induced MRGPRX2 activation and scratching | |||
T83926 |
S-Geranylgeranyl-L-glutathione
GGG |
||
S-Geranylgeranyl-L-glutathione是孤儿G蛋白偶联受体(GPCR)P2RY8的配体。该化合物在100 nM浓度下,选择性地诱导P2RY8而非鞘氨醇-1-磷酸受体2(S1P2)、GPR55、半胱氨酸白三烯受体1(CysLT1 receptor)以及CysLT2 receptor的内吞作用。在10 nM浓度下,S-Geranylgeranyl-L-glutathione抑制了表达P2RY8的WEHI-231 B细胞淋巴瘤细胞和分离的人扁桃体生发中心B细胞由趋化因子(C-X-C motif)配体12(CXCL12)诱导的迁移。 | |||
T35562 |
Nat-20(S)-yne
|
||
Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors. 20(S)-hydroxy Cholesterol (20(S)-OHC) is an oxysterol which binds SMO and activates hedgehog signaling (EC50 = 3 μM), and this activation is selective for the nat-20(S)-OHC enantiomer. Nat-20(S)-OHC synergizes with the SMO agonist SAG, suggesting an allosteric effect. Nat-20(S)-yne is a form of nat-20(S)-OHC with a terminal alkyne group, whi... | |||
T36550 |
CAY10535
|
||
TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for ... | |||
T83959 | CELT-426 | ||
CELT-426是一种高效且部分选择性的荧光hD2多巴胺受体拮抗剂,其Kivalue分别针对D2、D3和D4多巴胺受体,在放射配体结合实验中分别为89.3 nM、194.8 nM和263.6 nM。CELT-426可作为荧光多巴胺受体探针,在荧光结合实验、活细胞成像、流式细胞术及荧光偏振实验中使用。它是GPCR放射性标记配体的理想替代品。激发和发射峰值(λ)分别为560 nm和571 nm。这些波长适合作为TR-FRET实验中的受体染料,与CoraFluor1 TR-FRET供体一起使用。 | |||
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。 | |||
T83958 | CELT-327 | ||
CELT-327是一种高效且选择性的荧光hA2B/A3腺苷受体拮抗剂,其Kivalues在A2B和A3受体上分别为35.6 nM和45.7 nM。在表达A2B腺苷受体的HCT116细胞中,CELT-327表现出剂量依赖性的膜荧光标记,荧光信号快速扩散并在细胞单层中均匀分布。在活的HCT116紧凑球体中,CELT-327展现出整个球体直径上的均匀染色,可达到球体深层区域。CELT-327可作为荧光腺苷受体探针用于荧光结合分析、活细胞成像、流式细胞术和荧光偏振分析。它是GPCR放射标记配体的合适替代品。激发和发射最大值(λ)分别为589 nm和616 nm。这些波长与作为TR-FRET分析中接受体染料使用兼容,与CoraFluor1 TR-FRET供体一同使用。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T0853 |
Adenosine
腺苷,D-Adenosine,Adenine riboside |
Apoptosis; Nucleoside Antimetabolite/Analog; Endogenous Metabolite; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
Adenosine (D-Adenosine) 是一种核糖核苷,由与核糖结合的腺嘌呤组成,具有血管扩张、抗心律失常和镇痛作用。 | |||
T14063 |
7α,25-Dihydroxycholesterol
7α,25-OHC |
EBI2/GPR183; Endogenous Metabolite | GPCR/G Protein; Metabolism |
7α,25-Dihydroxycholesterol 是一种孤儿 GPCR 受体EBI2 (GPR183)的内源性配体和有效选择性激动剂。它对激活 EBI2 有很强的作用 (EC50=140 pM;Kd=450 pM)。它能够作为一种趋化因子,指导 B 细胞、T 细胞和树突状细胞的迁移。 | |||
TQ0194 |
trans-Vaccenic acid
TVA,(11E)-octadec-11-enoic acid,11E)-octadec-11-enoic acid |
Endogenous Metabolite | Metabolism |
Trans-Vaccenic acid(TVA)是一种天然存在的反式脂肪酸,存在于反刍动物的脂肪和乳制品中,可通过 GPCR-CREB 通路调控 CD8+ T 细胞增殖,具有抗肿瘤活性。Trans-Vaccenic acid 可在瘤胃中合成饱和脂肪酸,在组织水平合成共轭亚油酸。 | |||
TN5580 | Rediocide A | ||
Rediocide A, an insecticide, can inhibit calcium mobilization in Drosophila G-protein- coupled receptors (GPCR)s other than methuselah, it can induce GPCR desensitization and internalization, and such effects are mediated by the activation of conventional |