Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9786 |
Lu AF27139
|
P2X Receptor | Membrane transporter/Ion channel; Neuroscience |
Lu AF27139 是一种有效的选择性 P2X7 受体拮抗剂(人和大鼠的 IC50 分别为 12 和 2.4 nM,小鼠、人和大鼠的 Ki 分别为 22、54 和 13 nM)。 Lu AF27139 可用于中枢神经系统疾病研究。 | |||
T9697 |
ASK1-IN-1
|
ASK | Apoptosis |
ASK1-IN-1 是一种凋亡信号调节激酶 1(SK1) 抑制剂,具有良好的效价 (细胞IC50=138 nM; BiochemicalIC50=21 nM)。ASK1-IN-1具有中枢神经系统渗透性。 | |||
T7388 |
GSK805
|
ROR | Metabolism |
GSK805 是能够生物利用的、具有 CNS 穿透性的 RORγt 抑制剂。 | |||
T16849 |
SB-222200
|
Neurokinin receptor | GPCR/G Protein; Neuroscience |
SB-222200 是一种选择性口服活性的,具有血脑屏障渗透性的 NK-3 受体拮抗剂,用于中枢神经系统疾病的研究。 | |||
T13323 |
VU6012962
|
GluR | Neuroscience |
VU6012962 是一种可渗透 CNS ,可口服的代谢型谷氨酸受体 7 阴性变构调节剂,IC50为 347 nM。 | |||
T5353 |
ABX-1431
Elcubragistat |
Lipase | Metabolism |
ABX-1431 (Elcubragistat) 是口服具有活力的、选择性CNS-渗透性单酰基甘油脂肪酶抑制剂,IC50=14 nM。 | |||
T14947 |
CHDI-390576
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
CHDI-390576 is a CNS penetrant class IIa HDAC inhibitor (IC50s: 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9). It shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform. | |||
T13321 |
VU6005649
|
GluR | Neuroscience |
VU6005649 是一种中枢神经系统渗透性的mGlu7/8受体激动剂,对于mGlu7受体和mGlu8受体的EC50分别为 0.65 μM 和 2.6 μM。 | |||
T28069 |
ML380
ML 380,ML-380 |
AChR | Neuroscience |
ML380 是一种高效的中枢神经系统渗透剂 M5 正变构调节剂,对人和大鼠 M5 的 EC50值分别为 190 和 610 nM。它对 M1 和 M3 mAChR 亚型具有中等选择性,可增加 Ach 对 M5 mAChR 的亲和力。 | |||
T5494 |
MW-150
MW01-18-150SRM |
p38 MAPK; Autophagy | Autophagy; MAPK |
MW-150 (MW01-18-150SRM) 是一种选择性、CNS 渗透性和口服活性的 p38α MAPK 抑制剂,Ki 为 101 nM。它可抑制内源性 p38α MAPK 在活化的神经胶质中磷酸化内源性底物 MK2 的能力。 | |||
T15387 | GLP-1R Antagonist 1 | Glucagon Receptor | GPCR/G Protein |
GLP-1R Antagonist 1 (compound 5d) 是口服有效的、能透过中枢神经系统的,胰高血糖素样肽 1 受体 (GLP-1R) 的非竞争性抑制,其 IC50 值为 650 nM。 | |||
T13318 |
VU0650786
|
GluR | Neuroscience |
VU0650786 是能透过中枢神经系统的,选择性谷氨酸受体亚型 3 的一种负变构调节剂,IC50值为 392 nM,有抗抑郁和抗焦虑活性。 | |||
T23000 |
ML289
VU0463597,ML 289 |
GluR | Neuroscience |
ML289 (VU0463597)是一种高效、选择性的,可透过血脑屏障的 mGlu3 (IC50=0.66 μM) 负变构调节剂。ML289 的选择性是 mGlu2 的 15 倍,对 mGlu5 无活性。 | |||
T5956 |
VP3.15 dihydrobromide
|
GSK-3; PDE | Metabolism; PI3K/Akt/mTOR signaling; Stem Cells |
VP3.15 dihydrobromide 是一种口服具有活力的、高效的、CNS 可渗透的PDE7-GSK3双重抑制剂,对 PDE7 和 GSK3 作用的IC50值分别为 1.59 μM 和 0.88 μM。它具有神经保护和神经修复作用,可用于研究多发性硬化症 (MS) 潜在的抗炎和促髓鞘再生联合。 | |||
T10393 |
AT-007
|
Reductase | Endocrinology/Hormones; Metabolism |
AT-007 是口服有效的,中枢神经系统渗透性醛糖还原酶的高效抑制剂, IC50为 100 pM。在 GALT 缺失大鼠中,它降低了有毒的半乳糖醇水平并预防了疾病并发症。 | |||
T35028 |
Valiglurax
VU2957,VU 0652957,VU 2957,VU-0652957,VU0652957,VU-2957 |
GluR | Neuroscience |
Valiglurax (VU2957),也称为 VU0652957和 VU2957,是一种强效、选择性、中枢神经系统渗透剂,可口服生物利用的 mGlu4正变构调节剂。VU2957具有良好的跨物种的体内外药理学和药代动力学性质。VU2957被评估为治疗帕金森病的临床前开发候选药物。 | |||
T61025 |
GSK-1482160
|
P2X Receptor | Membrane transporter/Ion channel; Neuroscience |
GSK-1482160是一种CNS-渗透的P2X7受体负变构调节剂,具有口服活性。P2X7受体参与中枢和外周免疫细胞产生促炎细胞因子,因此GSK-1482160具有研究炎症性疾病的潜力。GSK-1482160具有出色的体外效价(在包括人类在内的多种物种的重组和初始P2X7受体的功能和电生理测试中)和交叉靶标选择性。 | |||
T28068 |
ML375
ML 375,ML-375 |
||
ML375 is a potent, selective and CNS penetrant M5 negative allosteric modulator (NAM). | |||
T24616 |
PF-04781340
|
||
PF-04781340 is an effective, selective, and CNS penetrant agonist of 5-HT2C receptor. | |||
T28364 |
PF-03463275 2HCl
PF3463275,PF 3463275,PF03463275,PF-3463275 |
||
PF-03463275 is an orally available, CNS-penetrant inhibitor of SLC6A9, a GlyT1 glycine transporter. | |||
T24523 |
NBUMP
|
||
PF-04781340 is an effective, selective, and CNS penetrant agonist of the 5-HT2C receptor. | |||
T28377 |
PF-06827443
PF6827443,PF 6827443,PF-6827443 |
||
PF-06827443 is a orally bioavailable, CNS-penetrant M1-selective PAM with minimal agonist activity. | |||
T13359 |
XPC-6444
|
Others | Others |
XPC-6444 is a isoform-selective, and CNS-penetrant inhibitor of NaV1.6 with IC50 of41 nM for hNaV1.6,with anticonvulsant activity. | |||
T13310 |
VP3.15
|
Others | Others |
VP3.15 is an orally bioavailable and CNS-penetrant dual inhibitor of phosphodiesterase (PDE)7- GSK3 (IC50s: 1.59 μM and 0.88 μM for PDE7 and GSK-3). | |||
T71335 | PF-3774076 | ||
PF-3774076 is a CNS penetrant, potent, selective, partial agonist at the human α1A adrenoceptor. PF-3774076 is selective over α1B and α1D adrenoceptors. | |||
T68881 |
OL-135
|
||
OL-135 is a CNS penetrant, highly potent and selective reversible inhibitor of FAAH. OL-135 exhibits analgesic pharmacology in various animal models without the motor impairment associated with direct CB1 agonism. | |||
T16934 |
SRX246
|
Others | Others |
SRX246 has no interaction at V1b and V2 receptors. SRX246 shows negligible binding at 64 other receptors classes, including 35 G-proteincoupled receptors. SRX246 is a potent and CNS-penetrant vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V | |||
T61073 | KH-259 | ||
KH-259 (compound 1) is a highly potent, selective, and CNS-penetrant HDAC6 inhibitor, demonstrating an IC50 of 0.26 μM. It exerts its antidepressant effects in mice by inhibiting HDAC6 within the brain. Therefore, KH-259 holds promise as a valuable tool for neurodegenerative diseases research [1]. | |||
T73840 | VU0453379 hydrochloride | ||
VU0453379 hydrochloride,是一种具有高选择性的中枢神经系统(CNS)可渗透的胰高血糖素样肽受体(GLP-1R)阳性变构调节剂(PAM),其EC50值为1.3 μM。 | |||
T79212 |
mTOR inhibitor-12
|
mTOR | PI3K/Akt/mTOR signaling |
mTORinhibitor-12(Compound 11)为选择性脑渗透性mTOR抑制剂,无遗传毒性风险,适用于中枢神经系统疾病研究。 | |||
T39492 |
FRM-024
|
||
FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease. | |||
T37732 |
AMG 21629
|
||
Potent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant. Tamayo et al (2008) Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. J.Med.Chem. 51 2744 PMID:18386885 |Gavva et al... | |||
T78211 |
STX-478
|
PI3K | PI3K/Akt/mTOR signaling |
STX-478(化合物 80)为口服活性、能穿透血脑屏障、选择性针对突变型构象PI3Kα的抑制剂。STX-478表现出对肿瘤的强效抑制和长期缩减效果,适用于癌症研究。 | |||
T9414 |
TPX-0131
|
||
TPX-0131 是一种有效、选择性、CNS 渗透性和口服活性的野生型ALK 抑制剂 (IC50为 1.4 nM) 并且有效对抗 ALK 耐药突变,例如G1202R(IC50为 0.3 nM)、L1196M(IC50为 0.3 nM)。TPX-0131 具有很强的抗肿瘤活性。 | |||
T79211 |
mTOR inhibitor-11
|
mTOR | PI3K/Akt/mTOR signaling |
mTORinhibitor-11(Compound 9)是具有穿透血脑屏障能力的mTOR抑制剂,其IC50针对pS6为21 nM。该化合物还可抑制pCHK1及PDE4D,其IC50值分别为17.2 μM和17.0 μM,适用于中枢神经系统疾病的研究。 | |||
T5487 | MW-150 dihydrochloride dihydrate | ||
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) 是一种选择性的,可透过神经系统,具有口服活性的的p38α MAPK 抑制剂,Ki 值为 101 nM。MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) 抑制内源性 p38α MAPK 磷酸化活化的神经胶质中内源性底物 MK2 的能力。 | |||
T81637 |
NT-0796
|
NOD-like Receptor (NLR) | Immunology/Inflammation |
NT-0796为一种选择性穿透中枢神经系统的NLRP3炎性体抑制剂,其PBMC方法中的IC50值为0.32 nM。该化合物为异丙酯类,能够在细胞内转化为NDT-197959(羧酸活性物)。NT-0796在神经炎症疾病研究中显示出潜力。 | |||
T83946 |
CHDI 00484077
|
||
CHDI 00484077是一种强效且选择性的IIa类组蛋白去乙酰化酶(HDAC)抑制剂,其体内IC50值为10-30 nM,而在HEK293和Jurkat细胞中的IC50值分别为0.01 nM和0.04 nM。在细胞中对IIa类HDACs具有150倍的选择性,优于I/IIb类HDACs。具有口服生物可用性和中枢神经系统(CNS)穿透能力。 | |||
T37293 | CMPI hydrochloride | ||
Potent positive allosteric modulator of α4β2 nAChRs (EC50 values are 20 and 18 nM for rat and human, respectively). Selective for hα4β2 over hα3β2, hα3β4 and hα7. Inhibits (α4)2(β2)3, muscle-type and Torpedo nAChRs (IC50 values are 0.5, 0.7 and 0.2 μM, respectively), but not (α4)3(β2)2 receptors. Exhibits ability to photoincorporate into aliphatic and nucleophilic amino acid side chains. Hamouda (2016) Photolabeling a nicotinic acetylcholine receptor (nAChR) with an (α4)3(β2)2 nAChR-selective p... |