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。 | |||
T11689 |
ITI-214
ITI214 |
PDE | Metabolism |
ITI-214 是一种中枢神经系统活性抑制剂,具有口服生物活性的PDE1抑制剂 (Kiof 58 pM),对其他 PDE 家族成员和一系列酶、受体、转运体和离子通道具有良好的选择性,在各种运动和认知功能的动物模型中显示出有效性。 | |||
T0682 |
Lamivudine
GR109714X,BCH-189,拉米夫定 |
HIV Protease; Reverse Transcriptase | Microbiology/Virology; Proteases/Proteasome |
Lamivudine (BCH-189) 是一种核苷逆转录酶抑制剂,可抑制HIV 逆转录酶1和2 以及乙型肝炎病毒的逆转录酶。 | |||
T0688 |
Ganciclovir
BW 759,更昔洛韦,RS-21592,2'-Nor-2'-deoxyguanosine |
Nucleoside Antimetabolite/Analog; Others; Antibiotic; Antifection; HSV | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others |
Ganciclovir (2'-Nor-2'-deoxyguanosine) 是核苷类似物和口服抗病毒药物,对CMV 具有抗病毒活性。它用于治疗与艾滋病相关的巨细胞病毒感染的并发症。 | |||
T22337 |
Ganciclovir sodium
RS-21592 sodium,Cytovene IV sodium,2'-Nor-2'-deoxyguanosine sodium,BW 759 sodium,更昔洛韦钠 |
Nucleoside Antimetabolite/Analog; Others; Antifection; HSV | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others |
Ganciclovir sodium (Cytovene IV sodium) 是核苷类似物和口服抗病毒药物,具有抗病毒活性,尤其是针对巨细胞病毒和单纯疱疹病毒 1 型。 | |||
T12899L |
SEP-363856 hydrochloride
SEP-856 hydrochloride |
Others; 5-HT Receptor | GPCR/G Protein; Neuroscience; Others |
SEP-363856 hydrochloride (SEP-856 hydrochloride) 是一种口服活性和 CNS 活性的精神药物,具有独特的非 D2/5-HT2A 作用机制,发挥其抗精神病样作用,具有治疗精神分裂症的潜力。 | |||
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。 | |||
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。 | |||
T21327 |
Uridine triacetate
RG 2133 triacetate,PN-401,Tri-O-acetyluridine,PN401,RG 2133,RG-2133,PN 401,RG2133,RG2133 triacetate |
Others | Others |
Uridine triacetate (RG 2133 triacetate) 是一种具有口服活性的 Uridine 前药。Uridine triacetate 能在肠道内迅速被吸收,在循环中迅速脱乙酰,生成游离尿苷。Uridine triacetate 可用于研究 5-氟尿嘧啶 (5-FU) 和卡培他滨的毒性,或早发性心脏或中枢神经系统 (CNS) 毒性。 | |||
T61564 |
PF-03463275
PF-3463275 |
GlyT | Neuroscience |
PF-03463275 是一种具有口服活性和选择性的竞争性甘氨酸转运蛋白-1 (GlyT1) 可逆抑制剂,Ki 为 11.6 nM。PF-03463275 具有中枢神经系统渗透性,可用于改善与精神分裂症相关的认知障碍。 | |||
T60707 |
Quinupramine
|
||
Quinupramine 具有口服活性的抗抑郁剂,其抗抑郁活性与中枢血清素系统有关,与 β- 肾上腺素能系统无关。Quinupramine 能够渗入中枢神经系统并且影响某些神经传递的过程。 | |||
TQ0291 |
Firategrast
SB 683699 |
Integrin | Cytoskeletal Signaling |
Firategrast (SB 683699) 是一种具有口服活性和特异性的α4β1/α4β7整合素拮抗剂。Firategrast 减少淋巴细胞进入中枢神经系统 (CNS) 的运输,降低多发性硬化症 (MS) 的活性。Firategrast 用于复发缓解性多发性硬化症。Firategrast 治疗与中位脑脊液与 CD4,CD8和CD19淋巴细胞计数的适度降低有关。 | |||
T14835 |
BTRX-335140
CYM-53093 |
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
BTRX-335140 (CYM-53093) 是一种有效的选择性口服活性 κ 阿片受体 (KOR) 拮抗剂,对 κOR、μOR 和 δOR 具有拮抗活性,IC50 值分别为 0.8、110 和 6500 nM。它可以很好地分布到 CNS 中,在大鼠中具有良好的体外吸收、分布、代谢、排泄和毒性以及体内药代动力学特征。 | |||
T24510 |
MW108
MW-108,MW01-11-108,MW 108,MW01 11 108,MW0111108 |
||
MW108 is an active site targeted, CNS-active, p38αMAPK inhibitor. | |||
T30234 |
AX-A411-BS
|
||
AX-A411-BS is a CNS-active benzodiazepine with anxiolytic properties. | |||
T12677 |
(Rac)-SEP-363856
(Rac)-SEP-856 |
Others | Others |
(Rac)-SEP-363856 is the racemate of SEP-363856. SEP-363856 is an orally active and CNS active psychotropic agent with a unique | |||
T12899 |
SEP-363856
SEP-856 |
Others | Others |
SEP-363856 是一种口服活性和 CNS 活性的精神药物,具有独特的非 D2/5-HT2A 作用机制,发挥其抗精神病样作用,具有治疗精神分裂症的潜力。 | |||
T82425 |
Excitin 1
|
||
Excitin 1为具口服活性多肽,能改变大鼠行为并影响脑内单胺与氨基酸浓度。 | |||
T11056 |
DLK-IN-1
|
DNA Alkylation | DNA Damage/DNA Repair |
DLK-IN-1 is a selective oral active inhibitor of bisleucine zipper kinase (DLK, MAP3K12) with Ki of 3 nM. DLK-IN-1 is active in the Alzheimer's disease model, retains excellent CNS permeability, and after multiple days of administration, its concentration | |||
T36644 | Rezivertinib | ||
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI) with potent activity against both common activation EGFR and resistance T790M mutations. Additionally, Rezivertinib demonstrates excellent central nervous system (CNS) penetration and exhibits antitumor activity[1][2]. | |||
T61497 |
Rho-Kinase-IN-2
|
||
Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK), which can penetrate the central nervous system (CNS). It exhibits a high affinity for ROCK2 with an inhibition constant (IC50) of 3 nM. This compound is of potential interest for further investigations in the field of Huntington's disease research [1]. | |||
T81438 |
PLP (180-199)
|
||
PLP (180-199) 是一种具备生物活性的肽段,为髓磷脂蛋白(PLP)中氨基酸 180 至 199 的区域。作为中枢神经系统中含量最高的髓磷脂蛋白,PLP (180-199) 在多发性硬化症(MS)的研究中具有重要应用,MS 为一种以中枢神经系统慢性炎症性脱髓鞘为特征的疾病。 | |||
T40119 |
TC-2559 difumarate
|
||
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist with an EC 50 of 0.18 μM. It exhibits selectivity for α4β2 receptors over α2β4, α4β4, and α3β4 receptors, with EC 50 s ranging from 10 to 30 μM. TC-2559 difumarate also demonstrates antinociceptive effects. | |||
T78793 |
MAOA-IN-1
|
Monoamine Oxidase | Neuroscience |
MAOA-IN-1(化合物15)是一种口服有效的MAOA抑制剂,对前列腺癌细胞显示出细胞毒性。该化合物表现出Caco-2渗透性,同时具有较低的CNS渗透性。MAOA-IN-1可以用于研究抗癌和抗炎适应症。 | |||
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。 | |||
T62841 |
Tinlorafenib
|
||
Tinlorafenib (PF-07284890) (compound 10) 是一种口服具有活力的、具有中枢神经系统 (CNS) 渗透性的 BRAF kinase 抑制剂,能够作用于 BRAFV600E (IC50: 4.25 nM) 和 V600K (IC50: 2.7 nM)。Tinlorafenib 能够用于 BRAF 相关的中枢神经系统恶性和良性肿瘤以及颅外恶性肿瘤的研究。 | |||
T11606 |
ICA-105665
PF-04895162 |
Others | Others |
ICA-105665 (PF-04895162) 是一种有效的口服活性的神经元 Kv7.2/7.3和 Kv7.3/7.5钾通道激动剂。ICA-105665 在人肝细胞中具有低细胞毒性潜力,但抑制肝线粒体功能和胆盐输出蛋白 (BSEP) 转运 (IC50为 311 μM)。ICA-105665 可穿透中枢神经系统 (CNS)并具有抗癫痫作用。 | |||
T21750 |
A 784168
|
||
A-784168 是一种有效的、口服活性的香草素受体 1 型 (TRPV1) 抑制剂。香草素受体 1 型 (TRPV1) 是一种配体门控非选择性阳离子通道,被认为是各种疼痛刺激 (如内源性脂质、辣椒素、热和低 pH 值) 的重要整合剂。口服给药时,A-784168 具有良好的 CNS 渗透性。 | |||
T71243 | ASP3662 | ||
ASP3662, also known as SPI-62, is a potent, selective and CNS-penetrable inhibitor of 11β-HSD1. The effects of ASP3662 suggest that selective inhibition of 11β-HSD1 may be an attractive approach for the treatment of neuropathic and dysfunctional pain, as observed in fibromyalgia. ASP3662 inhibited human, mouse and rat 11β-HSD1 but not human 11β-HSD2, in vitro. ASP3662 inhibited in vitro conversion of glucocorticoid from its inactive to active form in extracts of rat brain and spinal cord. | |||
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。 | |||
T62172 | Dual AChE-MAO B-IN-1 | ||
Dual AChE-MAO B-IN-1 (compound 15) 是一种安全的、代谢稳定的神经保护剂。Dual AChE-MAO B-IN-1 是一种强效的、口服具有活力的中枢神经系统渗透的人 AChE(IC50=550 nM) 和 MAO-B (IC50=8.2 nM)抑制剂,对 AChE 和 MAO-B 的 IC50 值分别为 550 nM、8.2 nM。 | |||
T70856 |
3-Oxobetulin Acetate
|
||
3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg/ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg/ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg/ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblasto... | |||
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。 | |||
T73359 |
NYX-2925
|
||
NYX-2925 是一种口服有效的NMDAR 调节剂。NYX-2925 恢复 mPFC 中 GluN2A 和 GluN2B 上活化的Src 和Src 磷酸化位点的水平。NYX-2925 对 CAMKII 没有影响,也没有任何成瘾或镇静/共济失调的副作用。NYX-2925 可用于多种 NMDA 受体介导的中枢神经系统疾病的研究。 |