84
6
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T31976 |
Glymidine sodium
|
Others | Others |
Glymidine sodium 是口服有活性的抗糖尿病药物,也是肝脂肪分解的抑制剂。它通过抑制葡萄糖的形成,也对由于内源性脂质动员抑制而导致的丙酮酸氧化升高具有抑制作用。 | |||
T17250 |
W-54011
|
ROS; Complement System | Immunology/Inflammation |
W-54011 是口服有效的非肽 C5a 受体拮抗剂,抑制125I 标记的 C5a 与人嗜中性白细胞的结合,Ki 为 2.2 nM。它还抑制C5a 诱导的人嗜中性粒细胞的细胞内 Ca2+动员,趋化性和ROS 的生成,IC50分别为 3.1 nM、2.7 nM 和1.6 nM。 | |||
T16850 |
SB-265610
GSK-CXCR2 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
SB-265610 (GSK-CXCR2) 是竞争性非肽变构CXCR2选择性拮抗剂,可阻断大鼠 CINC-1 诱导的钙动员和中性粒细胞趋化性,IC50分别为 3.7 和 70 nM。 | |||
T28073 |
MLS1547
MLS000051547,MLS 1547,MLS-1547 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
MLS1547 (MLS000051547) 是一种高效的 G 蛋白偏向多巴胺 D2 受体激动剂,Ki 为 1.2 μM。 MLS1547 在钙动员试验中刺激 D2R G 蛋白介导的信号传导,EC50 为 0.37 μM。 | |||
T13325 |
VU 0365114
|
AChR | Neuroscience |
VU 0365114 是 mAChR M5 的正变构调节剂,可增加 ACh 诱导的钙动员,EC50为 2.7 μM。 | |||
T29135 |
VU0422288
VU-0422288,ML-396,ML396,VU 0422288,ML 396 |
GluR | Neuroscience |
VU0422288 (ML396) 是一种有效的 III 型 mGlu 受体 (mGlus) 正变构调节剂。VU0422288在钙动员试验中对 mGluR4、mGluR7 和 mGluR8 显示出抑制作用。VU0422288 可用于研究 Rett 综合症 (RTT)。 | |||
T9466 |
RTICBM-189
|
Others | Others |
RTICBM-189 是可透过血脑屏障的大麻素 1 型受体变构调节剂,在 Ca2+动员试验中pIC50为 7.54,对 hCB1和 mCB1的 pIC50分别为 5.29 和 6.25。 | |||
T23010 |
MNI 137
|
Others; GluR | Neuroscience; Others |
MNI 137 是 mGlu2 的负变构调节剂。 MNI 137 抑制谷氨酸诱导的钙动员,对人和大鼠的 IC50 分别为 8.3 和 12.6 nM。 | |||
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。 | |||
T2370 |
AC-55541
AOB2796 |
Proteasome; Protease-activated Receptor | GPCR/G Protein; Proteases/Proteasome; Ubiquitination |
AC-55541 (AOB2796) 是高选择性的蛋白酶激活受体 2(PAR2)激动剂,pEC50为6.7。它在 PI 水解测定和 Ca2+动态测定中的pEC50值为 5.9 和 6.6,在体内表现出伤害感受器活性。 | |||
T27753 |
KT-362 fumarate
KT 362,KT362,KT-362 |
Potassium Channel; Calcium Channel; Sodium Channel | Membrane transporter/Ion channel; Metabolism |
KT-362 fumarate 是一种新型化合物,可作为钙通道、钾通道和钠通道的拮抗剂.KT-362 fumarate 通过影响心房肌肉细胞内钙动员导致血管舒张。KT-362 fumarate 对兔子的股动脉和基底动脉条有放松作用。 | |||
TP1936L1 |
RFRP3(human) acetate(311309-27-0 free base)
|
Neuropeptide Y Receptor | GPCR/G Protein; Neuroscience |
RFRP3(human) acetate(311309-27-0 free base) 是一种人类 GnIH 肽同源物,是一种有效的促性腺激素分泌抑制剂,可抑制 Ca2+ 动员。它是一种 NPFF1 受体激动剂,它抑制毛喉素诱导的 cAMP 产生,IC50 为 0.7 nM。 | |||
T4674 |
SB297006
SB 297006 |
CCR | Immunology/Inflammation; Microbiology/Virology |
SB297006 是一种CCR3拮抗剂,IC50为39 nM。它能够显著抑制 CCL11 处理的神经祖细胞的增殖和神经球形成。 | |||
TP2106L |
Urantide acetate(669089-53-6 free base)
|
Neurotensin Receptor | GPCR/G Protein |
Urantide acetate(669089-53-6 free base) 是一种选择性和竞争性的 urotensin-II (UT) 受体拮抗剂 (pKB = 8.3)。体外阻断 hU-II 诱导的胸主动脉收缩。对去甲肾上腺素或内皮素 1 诱导的收缩或乙酰胆碱诱导的松弛没有影响。在钙动员测定(在表达 hUT 受体的 CHO 细胞中)中表现为部分激动剂。 | |||
T22794 |
G36
G-36 |
Estrogen Receptor/ERR | Endocrinology/Hormones |
G36是一种细胞可渗透的G 蛋白偶联雌激素受体(GPER/GPR30)的非甾体拮抗剂。G36抑制17β-雌二醇或GPER 选择性激动剂G-1的激活(IC50分别为112和165 nM)。G36对ERα或ERβ均无可检测的结合活性。G36通过GPER 阻断由雌激素触发的PI3K 的激活或钙动员,并且它通过雌激素或G-1而不是通过EGF 抑制ERK 的激活。 | |||
T37312 |
Isotachysterol 3
|
||
Isotachysterol 3, an analog of 1,25-dihydroxy Vitamin D3, was found to enhance intestinal calcium transport and stimulate bone calcium mobilization in anephric rats[1]. | |||
T40948 | KMG-104 | ||
KMG-104 is a fluorescent magnesium (Mg2+) probe known for its exceptional selectivity. It has been extensively utilized to investigate the mobilization of Mg2+ in the cytoplasm across different cell types. | |||
T12331L |
OT-R antagonist 1
Oxytocin receptor antagonist 1 |
Others | Others |
OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). OT-R antagonist 1 is a new effective and selective nonpeptide low molecular weight OT-R antagonist. | |||
T62660 |
MLN3126
|
||
MLN3126 是一种口服具有活力的强效 CCR9 拮抗剂。 MLN3126 抑制 CCL25 诱导的钙动员 (calcium mobilization) 和小鼠初级胸腺细胞趋化 (chemotaxis) (IC50: 6.3 nM)。 | |||
T63661 |
HF51116
|
||
HF51116 是 XCR4 的有效拮抗剂。HF51116 能够显著拮抗 SDF-1α 诱导的细胞迁移、钙动员和 CXCR4 内化,并利用 CXCR4 抑制 HIV-1 感染。HF51116 对HIV-1感染、造血干细胞动员和癌症转移表现出研究潜力。 | |||
T28169 |
NIBR-0213
NIBR 0213 |
LPL Receptor | GPCR/G Protein |
NIBR-0213 是S1P1选择性拮抗剂,有抗实验性自身免疫性脑脊髓炎的作用。在 GTPγ35S 试验中,它作用于人和大鼠S1P1的IC50分别为 2.0 nM 和 2.3 nM。 | |||
T35922 |
NAADP (sodium salt)
|
||
Nicotinic acid adenine dinucleotide phosphate (NAADP) is a secondary messenger that induces calcium mobilization. It induces calcium release from endosomes and lysosomes via two-pore channel 2 (TPC2) and TPC1, which then stimulates large-scale calcium release from granules and the endoplasmic reticulum mediated by type 1 ryanodine receptors (RyR2s), RyR3s, and inositol-(1,4,5)-triphosphate receptors (IP3Rs). NAADP induces calcium mobilization in sea urchin and starfish eggs post fertilization to... | |||
T16034 |
Meclinertant
SR 48692 |
Others | Others |
Meclinertant is an effective, selective, nonpeptide, and orally active neurotensin receptor 1 (NTS1) antagonist. Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization (pA2 : 8.13), in human colon carcinoma (HT-29) cell | |||
T69385 | Baicalein monohydrate | ||
Baicalein monohydrate is an inhibitor of 12-lipoxygenase, leukotriene biosynthesis and release of lysosomal enzymes. It also inhibits cellular Ca2+ uptake and mobilization and adjuvant-induced arthritis. | |||
T69357 |
AL-34662
|
||
AL-34662 is a serotonin-2 receptor agonist with antihypertensive action. AL-34662 has a high-affinity for the 5-HT2 receptor and may potentially lead mobilization of [Ca2+]i in h-CM and h-TM cells leading to a decrease in ocular pressure. | |||
T37529 |
TC NTR1 17
|
||
Non-peptide neurotensin receptor 1 (NTS1) partial agonist (EC50 <15.6 nM and Emax = 63% of neurotensin response in Ca2+ mobilization assay). Exhibits over 50-fold selectivity for NTS1 over NTS2 and GPR35. Hershberger et al (2014) Imidazole-derived agonists for the neurotensin 1 receptor. Bioorg.Med.Chem.Lett. 24 262 PMID:24332089 | |||
TP1981 |
Neuropeptide S(Mouse)
Neuropeptide S (Mouse) |
||
Potent endogenous neuropeptide S receptor (NPSR) agonist (EC50 = 3 nM). Induces mobilization of intracellular Ca2+. Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice. | |||
T68959 |
Fenobam hydrate
|
||
Fenobam hydrate is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5). It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate and inhibits basal activity of mGluR5. Fenobam reduces stress-induced hyperthermia, exhibits anxiolytic-like activity, and may induce analgesia. | |||
T81279 |
RhB-PBP10 TFA
|
||
RhB-PBP10 TFA,一种Rhodamine B 标记的PBP10 TFA (FPR2 拮抗剂),有效选择性地抑制FPRL1 在中性粒细胞中诱导的颗粒动员以及氧自由基的分泌。 | |||
T38227 |
Quin C1
|
||
Potent and selective FPR2 agonist (EC50 = 15 nM). Induces Ca2+ mobilization in FPR2 but not FPR1-transfected mast cells. Induces neutrophil chemotaxis and degranulation in vitro. Reduces neutrophil and lymphocyte counts in bronchoalveolar lavage fluid in a mouse lung injury model. Anti-inflammatory. Zhou et al (2007) Pharmacological characterization of a novel nonpeptide antagonist for formyl peptide receptor-like 1. Mol.Pharmacol. 72 976 PMID:17652444 |Corminboeuf et al (2014) FPR2/ALXR agonist... | |||
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。 | |||
T61236 | CXCR2 antagonist 7 | ||
CXCR2 antagonist 7 (compound 19) 是一种有效的CXCR2拮抗剂。CXCR2 antagonist 7 显示出有效的CXCR2结合亲和力 (IC50=0.044 μM) 和钙动员 (IC50=0.66 μM)。 | |||
T36634 |
ZQ 16
|
||
Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 |Zhang et al (2016) Discovery and characte... | |||
T6764 |
ATI-2341
ATI2341 |
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
ATI-2341 是 C-X-C 趋化因子受体 4 型功能选择性变构激动剂,作为偏向配体有利于 Gα1 激活。它是一种变构激动剂,可激活抑制性异源三聚体 G 蛋白 (Gi) 以促进抑制 cAMP 产生并诱导钙动员。 | |||
T61359 | CXCR2 antagonist 6 | ||
CXCR2 antagonist 6 (compound 35c) 是一种有效的CXCR2拮抗剂。CXCR2 antagonist 6 显示出有效的CXCR2结合亲和力 (IC50=0.43 μM) 和钙动员 (IC50=0.11 μM)。 | |||
T75950 |
Neuropeptide S(Mouse) TFA
|
||
Neuropeptide S(Mouse) TFA, an endogenous agonist for the neuropeptide S receptor (NPSR) with an EC50 value of 3 nM, plays a significant role in physiological processes by inducing the mobilization of intracellular Ca2+. This compound elevates locomotor activity and wakefulness, and simultaneously decreases anxiety-like behavior in mice. | |||
T60655 | Resomelagon | ||
Resomelagon (AP1189) 是具有口服活性的有效黑素皮质素受体 (MR) 激动剂,可诱导Ca2+流动和 ERK1/2 磷酸化。Resomelagon 显示出抗炎活性, 可用于研究肥胖和慢性炎症。 | |||
T61235 | CXCR2 antagonist 5 | ||
CXCR2 antagonist 5 (compound 25) 是一种有效的CXCR2拮抗剂。 CXCR2 antagonist 5 显示出有效的CXCR2结合亲和力 (IC50=0.013 μM) 和钙动员 (IC50=0.1 μM)。 | |||
T62140 | HF50731 | ||
HF50731 是一种 CXCR4 的有效拮抗剂。HF50731 对 CXCR4 具有较强的结合亲和力 (IC50: 19.8 nM)。HF50731 利用 CXCR4 共受体,有效的抑制钙动员 (IC50: 119.2 nM)、细胞迁移 (IC50: 621.4 nM) 和 HIV-1 感染 (IC50: 1.5 nM)。 | |||
T81391 |
Prolactin-Releasing Peptide (12-31), rat
|
||
Prolactin-Releasing Peptide (12-31), rat 为催乳素释放肽的一个段落,对 GPR10 受体具有高度亲和性,并能在转染了 PrRP 受体的 CHOK1 细胞中激发钙离子动员。 | |||
T74650 | JPE-1375 | ||
JPE-1375 是一种补体C5a 受体 1 (C5aR1) 拮抗剂。JPE-1375 能有效抑制小鼠体内多形核白细胞动员 (EC50=6.9 µM) 和降低TNF 水平 (EC50=4.5 µM)。JPE-1375 可用于自身免疫性和炎性疾病的研究。 | |||
T78600 |
VU0029251
|
||
VU0029251为mGluR5部分拮抗剂,表现出对该受体的较高亲和力(Ki: 1.07 μM)。在表达大鼠mGluR5的HEK293细胞膜上,可抑制谷氨酸引起的钙动员(IC50: 1.7 μM)。 | |||
T75866 |
RFRP-3(human) TFA
|
||
RFRP-3 (Neuropeptide VF(124-131))(human) TFA,一种人 GnIH 肽同源物,是一种促性腺激素分泌抑制 Ca2+动员的有效抑制剂。RFRP-3(human) TFA 是一种NPFF1受体激动剂,它抑制 forskolin 诱导的 cAMP 生成的 IC50值为 0.7 nM。 | |||
T72536 |
GPR84 antagonist 2
|
||
GPR84antagonist 2 是一种口服有效的,选择性的 GPR84拮抗剂(IC50=8.95 nM)。GPR84antagonist 2 在钙动员试验中显示出更强的效力,并在 GPR84激活时抑制中性粒细胞和巨噬细胞的趋化性。GPR84antagonist 2 具有研究溃疡性结肠炎的潜力。 | |||
T75815 |
WKYMVM-NH2 TFA
|
||
WKYMVM-NH2 TFA 是一种高效的 N-甲酰肽受体 FPR1 与 FPRL1/2 激动剂,具备激活白细胞功效特性,包括趋化性、补体受体-3 的激活以及 NADPH 氧化酶的激活。 | |||
T37556 |
CAY10502
|
||
Phospholipase A2 (PLA2) catalyzes the hydrolysis of phospholipids at the sn-2 position leading to the production of lysophospholipids and free fatty acids. Calcium-dependent cytosolic PLA2 (cPLA2α) is a 85 kDa enzyme that plays a key role in the arachidonic cascade and the inflammatory response associated with this metabolic pathway. CAY10502 is a potent inhibitor of calcium-dependent cytosolic PLA2α (cPLA2α) with an IC50 value of 4.3 nM for the purified enzyme from human platelets. It inhibits ... | |||
T80421 |
CSD-CH2(1,8)-NH2
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
CSD-CH2(1,8)-NH2 是一种针对KOR的选择性且竞争性拮抗剂,具有较低的Ki值(6.8 nM),能够抑制DRG神经元内的钙动员,并能拮抗U50,488的抗伤害效应,常用于神经精神疾病研究领域。 | |||
T41016 |
Vercirnon sodium
GSK-1605786 sodium,CCX282-Bsodium,维塞诺钠盐,Traficet-ENsodium |
||
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9 . Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC 50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC 50 s>10 μM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC 50 values of 2.8 and 2.6 nM, respectivel... | |||
TP2106 |
Urantide
|
||
Selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-induced relaxation. Behav | |||
T83801 |
ε-NAADP+ sodium
Etheno-NAADP,β-Nicotinic Acid-1,N6-Ethenoadenine dinucleotide phosphate,Nicotinic Acid adenine dinucleotide phosphate |
||
ε-NAADP+是钙动员诱导剂NAADP的荧光衍生物。在海胆卵细胞匀浆中诱导钙释放(EC50 = 5 µM)。ε-NAADP+在275 nm和410 nm分别显示激发/发射峰值,且在DMSO中的相对发射增加了三倍。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5246 |
Trans-2-butene-1,4-dicarboxylic acid
trans-2-Butene-1,4-dicarboxylic Acid,3-Hexenedioic Acid,trans-3-Hexenedioic Acid,β-Hydromuconic Acid,反式-2-丁烯-1,4-二甲酸 |
Others; Endogenous Metabolite | Metabolism; Others |
Trans-2-butene-1,4-dicarboxylic acid (3-Hexenedioic Acid) 是内源性代谢产物的一种。 | |||
TN3319 |
9-Hydroxycanthin-6-one
|
Potassium Channel; GSK-3; Calcium Channel; Wnt/beta-catenin | Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells |
9-Hydroxycanthin-6-one might be the active component that contributed to the aphrodisiac effect of E. longifolia by antagonizing the smooth muscle tone of CC as well as SV probably through interfering with Ca2+ mobilization.9-Hydroxycanthin-6-one inhibits Wnt signaling through the activation of GSK3β independent of CK1α. | |||
T19253 |
Cyclic ADP-ribose
cADPR |
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Cyclic ADP-ribose (cADPR) is an effective calcium mobilization second messenger, which is synthesized from NAD + by ADP-ribosyl cyclase. Cyclic ADP-ribose mainly increases cytosolic calcium through Ryanodine receptor-mediated endoplasmic reticulum release | |||
TN2918 |
3-Acetoxy-8(17),13E-labdadien-15-oic acid
|
cAMP; Potassium Channel; Calcium Channel | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism |
ent-3-Acetoxy-labda-8(17),13-dien-15-oic acid have vasorelaxant and hypotensive actions, the mechanisms underlying the cardiovascular actions of the labdane involve the activation of the endothelial NO-cGMP pathway, the opening of K+ channels and the alteration on Ca2+ mobilization. | |||
T37687 | Cyclic ADP-ribose ammonium | ||
Cyclic ADP-ribose ammonium (cADPR ammonium) is a powerful calcium mobilization second messenger synthesized from NAD+ by an ADP-ribosyl cyclase. It primarily raises cytosolic calcium levels through Ryanodine receptor-mediated release from the endoplasmic reticulum, while also facilitating extracellular influx through the opening of TRPM2 channels [1][2][3]. | |||
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 |