Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1909 |
L-701324
7-氯-4-羟基-3-(3-苯氧基)苯基-2(1H)-喹啉,L701324 |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
L-701324 是一种 NMDA 受体,对甘氨酸位点具有高亲和力和选择性,用作口服活性和长效抗惊厥药。 | |||
T33604 |
Z-Glycine
Carbobenzoxyglycine,N-苄氧羰基-甘氨酸,N-Carbobenzoxyglycine |
Others | Others |
Z-Glycine (Carbobenzoxyglycine) 是一种药物-脂质结合物,旨在促进脑渗透,基于其亲脂性和与生物膜中脂质的相似性。 | |||
T5518 |
N-acetylcysteine amide
|
Reactive Oxygen Species; ROS | Immunology/Inflammation; Metabolism; NF-κB |
N-Acetylcysteine amide 是一种硫醇抗氧化剂,也是一种神经保护剂,能够透过细胞膜和血脑屏障的,可降低ROS 的产生。 | |||
T15632 |
JW 642
|
Lipase | Metabolism |
JW 642 是一种高效的MAGL 抑制剂,对小鼠、大鼠和人源脑细胞膜上MAGL 的IC50值分别为7.6nM、14nM 和3.7nM。 | |||
T10162 |
5-HT3 antagonist 3
|
5-HT Receptor | GPCR/G Protein; Neuroscience |
5-HT3 antagonist 3 是一种高亲和力的 5-HT3 受体拮抗剂。5-HT3 antagonist 3 结合到大鼠脑皮质膜中的 5-HT3 受体,Ki 为 0.25 nM。 | |||
T13423 |
(1R,2R)-2-PCCA hydrochloride
(1R,2R)-2-PCCA(hydrochloride) |
Others | Others |
(1R,2R)-2-PCCA hydrochloride 是一种具有有效性、选择性和可穿过血脑屏障的 GPR88 受体激动剂,在 WT 小鼠纹状体膜中 EC50 值为1140 n。(1R,2R)-2-PCCA hydrochloride 可用于研究中枢神经系统。 | |||
T6352 |
(-)-Dizocilpine maleate
C13737,(-)-MK 801 (Maleate),(-)-MK 801马来酸,(-)-MK 801 Maleate |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) 是一种选择性且非竞争性的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂,Ki 为 211.7 nM。它是一种 Dizocilpine 的活性较低的 (-)-对映体,具有抗抑郁作用。 | |||
T6554 |
JZL 184
JZL184 |
Lipase | Metabolism |
JZL 184 是不可逆的、选择性的MAGL 抑制剂,对MAGL 的选择性比 FAAH 高 300 倍以上。它可阻断脑膜中的 2-花生四烯酸甘油酯 (2-AG) 的水解 (IC50为 8 nM)。 | |||
T23394 |
SR 57227A
SR57227盐酸盐,SR 57227 hydrochloride |
5-HT Receptor | GPCR/G Protein; Neuroscience |
SR 57227A (SR 57227 hydrochloride) 是一种有效的、具有口服活性和选择性的 5-HT3 受体激动剂,具有穿越血脑屏障的能力和抗抑郁作用。它对大鼠皮质膜和整个 NG 108-15 细胞或其膜上的 5-HT3 受体结合位点的亲和力,IC50在 2.8 至 250 nM 之间。 | |||
T38140 |
Phosphatidylethanolamine from bovine
|
||
Phosphatidylethanolamines (bovine) 是从牛脑中分离出来的一种磷脂酰乙醇胺混合物,在 sn-1 和 sn-2 位置上带有不同的脂肪酰基。Phosphatidylethanolamines (bovine) 是在原核生物、哺乳动物、植物和酵母细胞膜中含量均很高的磷脂,约占哺乳动物磷脂总量的 25%。 | |||
TP1940L1 |
Ac-RYYRIK-NH2 acetate
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Ac-RYYRIK-NH2 acetate 是 nociceptin/orphanin FQ(noc/OFQ) 受体的激动剂,影响自发运动活动。 它是转染在 CHO 细胞中的 ORL1 的部分激动剂,可拮抗大鼠脑膜和切片中 noc/OFQ 对 [35S]-GTPgammaS 与 G 蛋白结合的刺激。 | |||
T3320 |
Dizocilpine Maleate
(+)-Mk-801 Hydrogen Maleate,MK 801,地卓亚平马来酸盐,Dizocilpine hydrogen maleate,地佐环平马来酸盐,(+)-MK 801 maleate,(+)-MK 801 (Maleate) |
NMDAR; iGluR | Membrane transporter/Ion channel; Neuroscience |
Dizocilpine Maleate (MK 801) 是一种选择性和非竞争性的 NMDA 受体拮抗剂,Kd 值为 37.2 nM。它用于治疗 NMDA 受体可能发挥重要作用的多种神经退行性疾病或疾病。 | |||
T23445 |
Anxiolytic/nonsedative agent-1
TCS 1205 |
GABA Receptor | Membrane transporter/Ion channel; Neuroscience |
Anxiolytic/nonsedative agent-1 (TCS 1205) 是一种有效的选择性 GABAA 激动剂。Anxiolytic/nonsedative agent-1 对牛脑膜中的 BzR 显示出明显的亲和力,对 α1β2γ2、α2β2γ2、α5β3γ2 的 Kis 分别为 14、121、239 nM。Anxiolytic/nonsedative agent-1 在体外表现出 α2 选择性功效,在体内表现出抗焦虑选择性作用。 | |||
T19686 |
SCH-37370
乙酰地氯雷他定 |
Platelet aggregation | Others |
SCH-37370 是一种有效且具有口服活性的血小板活化因子和组胺双重拮抗剂。 Sch 37370 阻断 [3H]pyrilamine 与大鼠脑膜中组胺-H1 受体的结合。 Sch 37370 选择性地抑制 PAF 诱导的人血小板聚集(IC50:0.6 mM),并且还与 PAF 竞争与人肺膜制剂中特定位点的结合(IC50:1.2 mM)。 | |||
T22744 |
DPCPX
PD 116948,1,3-二丙基-8-环戊基黄嘌呤 |
Adenosine Receptor | GPCR/G Protein; Neuroscience |
DPCPX (PD 116948) 是一种黄嘌呤衍生物,是一种选择性腺苷 A1 受体的拮抗剂,Ki 值为 0.46 nM。 | |||
T32423 |
KS 5-2
KS-5-2 |
||
KS 5-2 has affinity to isolated synaptic membranes from rat brain. | |||
T68874 |
Kojic amine
|
||
Kojic amine is a GABA receptor agonist; potent and specific inhibitor of Na+-independent GABA binding to rat brain membranes. | |||
T71987 |
5-hydroxy Isatin
|
||
5-hydroxy Isatin is an inhibitor of monoamine oxidase A and also inhibits atrial natriuretic peptide-induced activation of particulate guanylyl cyclase in rat brain and heart membranes. | |||
T23587 |
8-CSC
8 CSC,CSC |
||
8-CSC is a dual agent endowed with good hMAO-B inhibitory activity (Ki: 235 nM in baboon liver mitochondria) and A2A affinity (Ki: 36 nM in rat brain striatal membranes receptor). | |||
T40445 |
Cyclocreatine
|
||
Cyclocreatine, a Creatine analogue, exhibits potent bioenergetic protection by elevating ATP levels. It demonstrates the ability to traverse cell membranes, including the blood-brain barrier, wherein it undergoes phosphorylation and dephosphorylation by creatine kinases. | |||
T27772 |
L-736380
L-736,380,L 736380,L736,380,L 736,380 |
||
L-736380 is a CCK-B receptor antagonist. L-736,380 dose-dependently inhibited gastric acid secretion in anesthetized rats (ID(50), 0.064 mg/kg) and ex vivo binding of [(125)I]CCK-8S in BKTO mice brain membranes (ED(50), 1.7 mg/kg). | |||
T37189 |
BTCP maleate
|
||
BTCP 与豚鼠脑膜一起预孵育可增加 [3H]TCP 从 PCP 位点的解离速率。 | |||
T70538 |
PD-85639
|
||
PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membr... | |||
T15415 |
GR 159897
|
Others | Others |
GR 159897 is a competitive, brain-penetrated non-peptide NK2 receptor antagonist with anti-tumor effects. GR 159897 inhibits binding of [3H]GR100679 to human NK2-CHO cells and rat colon membranes (pKis: 9.51 and 10, respectively). It can antagonize bronch | |||
T37205 |
CCK (26-31) (sulfated)
|
||
CCK (26-31) is an N-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. The sulfated form of CCK (26-31) inhibits binding of [125I]CCK-33 to guinea pig cortical membranes by 21% when used at a concentration of 0.1 mM. | |||
T37203 |
CCK (26-30) (sulfated)
|
||
CCK (26-30) is an N-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. The sulfated form of CCK (26-30) inhibits binding of [125I]CCK-33 to guinea pig cortical membranes by 10% when used at a concentration of 0.1 mM. | |||
T37665 |
Endosulfan I
|
||
Endosulfan I is an organochlorine insecticide and a stereoisomer of endosulfan II . It is active against a variety of insects, including bollworms (LD50 = 0.63 mg/g). Endosulfan I binds to GABA receptors in rat brain membranes with an IC50 value of 30 nM and is toxic to rats (LD50 = 18 mg/kg). | |||
T37953 |
Sphingomyelins (buttermilk)
|
||
Sphingomyelins (SMs) are bioactive sphingolipids found in mammalian cell membranes.1SMs make up 2-15% of the total organ phospholipid population but are found at higher concentrations in the brain and myelin sheaths surrounding peripheral nerves. They interact with cholesterol to control its distribution within cellular membranes and maintain cholesterol homeostasis in cells. SMs undergo hydrolysis by sphingomyelinase to form ceramides, which are sphingolipid mediators of intracellular signaling... | |||
T35920 |
N-methyl Paroxetine
|
||
N-methyl Paroxetine is a derivative of the selective serotonin reuptake inhibitor (SSRI) antidepressant paroxetine that inhibits [3H]paroxetine binding to rat cortical membranes (Ki = 4.3 nM). It inhibits serotonin uptake in rat brain synaptosomes with an IC50 value of 22 nM. N-methyl Paroxetine has been used as a precursor in the synthesis of paroxetine and is a potential impurity in commercial preparations of paroxetine. | |||
T22478 |
(±)-Anatoxin A fumarate
|
Others | Others |
(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium. It is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes | |||
T36861 |
Ganglioside GD1b Mixture (sodium salt)
Ganglioside GD1b Mixture (sodium salt) |
||
Ganglioside GD1b is an acidic glycosphingolipid that contains two sialic acid residues linked to an inner galactose unit. It is a component of plasma membranes where it packs densely with cholesterol to form lipid microdomains that modulate both intra- and intercellular signaling events. The concentration of ganglioside GD1b in human brain increases with age, constituting 7.85% of total sialic acid in the brain of 0- to 10-year-old subjects and 20.29% in 11- to 30-year-old subjects. Ganglioside ... | |||
T28321 |
PD 122860
PD-122860,PD122860 |
||
PD 122860 is a dihydropyridine with calcium channel blocking and sodium channel stimulating properties. In the rat heart, PD 122860 increased left ventricular contractility, decreased coronary resistance and altered the shape of the electrocardiogram T-wa | |||
T40572 |
Lesogaberan napadisylate
AZD-3355 napadisylate |
||
Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC 50 of 8.6 nM for human recombinant GABA B receptors. It demonstrates an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, as determined by its displacement of [3H]GABA binding in brain membranes. Notably, Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation. | |||
T76447 |
[DAla4] Substance P (4-11)
|
||
[DAla4] Substance P (4-11) 作为Substance P的衍生物,能够有效抑制125I-Bolton Hunter标记的Eledoisin(IC50值为0.5 μM)及125I-Bolton Hunter标记的Substance P (IC50值为0.15 μM)与大鼠大脑皮层膜之间的结合。 | |||
T36204 |
Methylatropine (nitrate)
|
||
Methylatropine is an antagonist of muscarinic acetylcholine receptors (IC50= <0.1 nM in a radioligand binding assay using isolated porcine brain membranes) and a derivative of atropine .1,2It reduces acetylcholine-induced decreases in blood pressure in rats when administered intravenously with an ED50value of 5.5 μg/kg.2Methylatropine reduces salivation, induces mydriasis, and increases heart rate in dogs.3 1.Schmeller, T., Sporer, F., Sauerwein, M., et al.Binding of tropane alkaloids to nicotin... | |||
T38282 | C22 Glucosylceramide (d18:1/22:0) | ||
C22 Glucosylceramide (d18:1/22:0) is an endogenous glucosylceramide. Glucosylceramides are major constituents of skin lipid membranes where they play a role in maintaining the water permeability barrier. They are precursors in the synthesis of lactosylceramide , as well as oligoglycolipids and gangliosides. Phospholipase A2 (PLA2) type XIIA knockdown increases C22 glucosylceramide (d18:1/22:0) expression in rat brain. It is also increased in the brain, but not the liver or spinal cord, of mice f... | |||
T37206 |
CCK (27-33) (non-sulfated)
|
||
CCK (27-33) is a C-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. Non-sulfated CCK (27-33) inhibits binding of [3H]naloxone in rat cerebellum membranes (IC50 = 4 uM) and inhibits electrically-stimulated contraction of isolated guinea pig ileum (IC50 = 17 uM), an effect that can be reversed by naloxone. Unlike sulfated CCK (27-33), the non-sulfated form does not reduce exploratory behavior in m... | |||
T71174 |
PBT434 HBr
|
||
PBT434 is a novel, brain-penetrant, small molecule inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is g... | |||
T35930 |
Ganglioside GM2 Mixture (sodium salt)
|
||
Ganglioside GM2 is a glycosphingolipid component of cellular membranes, primarily the plasma membrane. Levels of ganglioside GM2 are elevated in the brain of patients with Sandhoff disease, as well as feline and mouse models of the disease. Ganglioside GM2 accumulates in the lysosomes of individuals with Tay-Sachs disease and GM2-activator deficiency, as well as in the CNS of patients with and animal models of mucopolysaccharide storage disorders and Niemann-Pick disease types A, C1, and C2. Gan... | |||
T75907 |
Ac-RYYRIK-NH2 TFA
|
||
Ac-RYYRIK-NH2 TFA 作为高效的ORL1部分激动剂,充当ORL1的内源性配体,在CHO细胞中表现出较低的解离常数(Kd=1.5 nM)。该化合物以特异性方式激活G蛋白,作为竞争性拮抗剂,抑制noc/OFQ对大鼠脑膜和脑切片上 [35S]-GTPγS 结合G蛋白的作用。 | |||
T37439 |
C18 Globotriaosylceramide (d18:1/18:0)
|
||
C18 globotriaosylceramide is an endogenous sphingolipid found in mammalian cell membranes that is synthesized from lactosylceramide . It inhibits aggregation of human neutrophils induced by phorbol 12-myristate 13-acetate (PMA; 10008014) when used at a concentration of 1 μM. C18 globotriaosylceramide acts as a receptor for Shiga toxin in B cell-derived Raji cells and THP-1 monocytes. It accumulates in the brain, heart, kidney, liver, lung, and spleen in a mouse model of Fabry disease, a lysosoma... | |||
T72215 |
Lesogaberan hydrochloride
AZD-3355 hydrochloride |
||
Lesogaberan (AZD-3355) hydrochloride 是一种有效的选择性 GABAB 受体激动剂,对人重组 GABAB 受体的 EC50为 8.6 nM。通过脑膜中 [3H]GABA 结合位移测量,Lesogaberan hydrochloride 对大鼠 GABAB 和 GABAA 受体的亲和力 (Kis):分别为 5.1 nM 和 1.4 μM。Lesogaberan hydrochloride 通过外周作用模式抑制短暂的食管下括约肌松弛。 | |||
T80066 |
ShK toxin
|
Potassium Channel | Membrane transporter/Ion channel |
ShK toxin 是从加勒比海葵(Stichodactylu helianthus)的全身提取物中分离出的一种蛋白,能够阻断电压依赖性钾通道(Kv1.3 通道)。在竞争实验中,ShK toxin 与树突毒素 I 及α-树突毒素相互竞争,以与大鼠脑突触体膜结合,从而促进乙酰胆碱的释放。此外,ShK toxin 抑制培养的大鼠背根神经节神经元中的K+ 电流,并且能够抑制T淋巴细胞的增殖。 | |||
T38142 |
Phosphatidylethanolamines (soy)
|
||
Phosphatidylethanolamine is the most abundant phospholipid in prokaryotes and the second most abundant found in the membrane of mammalian, plant, and yeast cells, comprising approximately 25% of total mammalian phospholipids. In the brain, phosphatidylethanolamine comprises almost half of the total phospholipids. It is synthesized mainly through the cytidine diphosphate-ethanolamine and phosphatidylserine decarboxylation pathways, which occur in the endoplasmic reticulum (ER) and mitochondrial m... | |||
T32705 |
Levomefolate magnesium
L-Methylfolate magnesium |
||
Levomefolate magnesium is the magnesium salt of the metabolite of folic acid (Vitamin B9) and it is a predominant active form of folate found in foods and in the blood circulation, accounting for 98% of folates in human plasma. It is transported across th | |||
T81609 |
omega-3 Arachidonic acid ethyl ester
(all-Z)-8,11,14,17-Eicosatetraenoic acid ethyl ester,ω-3 Arachidonic acid ethyl ester |
||
omega-3 Arachidonic Acid ethyl ester 是一种少见的多不饱和脂肪酸,饮食来源稀少。ω-3脂肪酸对婴幼儿生长发育极为重要,能够帮助预防心脏病、血栓、高血压及炎症和自身免疫性疾病。该化合物在人血小板膜中通过抑制花生四烯酰辅酶A合成酶发挥作用,Ki值达到14 μM;同时在小牛脑提取物中也表现出抑制作用,IC50大约5 μM。omega-3 Arachidonic Acid ethyl ester 作为游离酸的亲脂性更强的形式,具备独特的生物活性。 |