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22

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1418	Bucladesine sodium dbcAMP,Dibutyryl-cAMP sodium salt,布拉地新钠盐,Dibutyryl-cAMP,DC2797,Sodium dibutyryl cAMP,Bucladesine,Bucladesine sodium salt	PKA; PDE	Metabolism; Tyrosine Kinase/Adaptors
	Bucladesine sodium (DC2797) 是一种 cAMP 类似物，具有细胞渗透性。Bucladesine sodium 也是一种 cAMP 依赖性的蛋白激酶 (PKA) 激活剂，一种磷酸二酯 (PDE) 抑制剂。Bucladesine sodium 具有抗炎活性。
T22967	MEDICA16 MEDICA 16	GPR; Others; ATP Citrate Lyase	Endocrinology/Hormones; GPCR/G Protein; Metabolism; Others
	MEDICA16 是 GPR40 的特异性激动剂以及 GPR120 的部分激动剂。 MEDICA16 是一种 ATP-柠檬酸裂解酶抑制剂，可显着降低腓肠肌中的细胞内 TG 含量，同时增加胰岛素敏感性。
T10601	BRCA1-IN-2	Others	Others
	BRCA1-IN-2 是一种可穿过细胞膜的 BRCA1 蛋白-蛋白相互作用（PPI）抑制剂，具有抗肿瘤活性，通过破坏 BRCA1 (BRCT)2 与蛋白质的相互作用来发挥作用。
T5315	TCA1 TCA-1,TCA 1	Antibacterial; Antibiotic	Microbiology/Virology
	TCA1 (TCA 1) 是一种小分子，具有抗耐药性和持续性结核病的活性。
T40296	MCA17-1 MCA17-1
	MCA17-1 exhibits superior bioactivity compared to the positive control, obeticholic acid (OCA), in the treatment of liver fibrosis.
T72195	KCa1.1 channel activator-2
	KCa1.1 channel activator-2 (化合物 3F) 是一种槲皮素衍生物，是选择性的血管 KCa1.1 channel 刺激剂。KCa1.1 channel activator-2 具有强效的肌肉松弛活性。
T72194	KCa1.1 channel activator-1
	KCa1.1 channel activator-1 (化合物 1E) 是一种槲皮素衍生物，是选择性的血管 KCa1.1 channel 刺激剂。KCa1.1 channel activator-1 也显示 CaV1.2 channel 通道阻断活性。KCa1.1 channel activator-1 表现出较弱的肌肉松弛活性。
T10600	BRCA1-IN-1	Others	Others
	BRCA1-IN-1 is a novel small-molecule-like inhibitor of BRCA1 (IC50: 0.53 μM; Ki: 0.71 μM).
TP1895L1	KYL acetate(676657-00-4 free base)	Ephrin Receptor	Tyrosine Kinase/Adaptors
	KYL acetate(676657-00-4 free base) 是EphA4受体酪氨酸激酶抑制剂（Kd = 0.8 μM）；抑制 EphA4-EphrinA5 相互作用 (IC50 = 6.34 μM)。防止 AβO 诱导的突触损伤、树突棘丢失并防止海马 CA3-CA1 传输中 LTP 的阻断。在细胞培养基中表现出较长的半衰期（在 PC3 和 C2C12 培养基中分别为 8 和 12 小时）。它有神经保护作用。
TP1945L1	Pep2m, myristoylated acetate Pep2m, myristoylated acetate(1423381-07-0 free base)	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	Pep2m, myristoylated acetate(1423381-07-0 free base) 是一种细胞可渗透的肉豆蔻酰化形式的 pep2m。 GluA2（AMPA 受体）亚基的 C 末端与 N-乙基马来酰亚胺敏感融合蛋白 (NSF)（一种调节 AMPA 受体功能的蛋白质）之间相互作用的肽抑制剂。降低 CA1 神经元中的突触后电流、培养的海马神经元中 AMPA 介导的电流和 AMPA 受体表面表达。
T38192	Unifiram	Others	Others
	Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。
T0782	Benzthiazide Aquatag,苄噻嗪,Lemazide,Dihydrex	Carbonic Anhydrase	Metabolism
	Benzthiazide (Lemazide) 是长效利尿剂及抗高血压剂。它也是碳酸酐酶 9 的抑制剂，他对 CA9，CA2 和 CA1 的 Ki 分别为 8.0，8.8 和 10 nM。它对肿瘤细胞增殖具有抑制作用。
T73099	Etbicyphat Trimethylopropane phosphate
	Etbicyphat (Trimethylopropane phosphate)作为一种GABA(A)受体竞争性拮抗剂展现出显著效果。通过诱发海马体CA1神经元的类似癫痫的活动并与GABA(A)-benzodiazepine受体结合，Etbicyphat的作用机制得到了阐述。
T37208	NAP-1
	NAP-1 is a compound with anesthetic activity.1 It increases paired-pulse inhibition in the CA1 region of rat hippocampal brain slices when used at a concentration of 100 μM. NAP-1 also induces loss of righting reflex in tadpoles (EC50 = 0.53 μM).References NAP-1 is a compound with anesthetic activity.1 It increases paired-pulse inhibition in the CA1 region of rat hippocampal brain slices when used at a concentration of 100 μM. NAP-1 also induces loss of righting reflex in tadpoles (EC50 = 0.53 μ...
T24919	UBP714 UBP 714,UBP-714
	UBP714 is a derivative of the NMDA receptor negative allosteric modulator UBP608. It also enhanced NMDAR mediated field EPSPs in the CA1 region of the hippocampus. UBP714 is a novel template for the development of potent and subunit selective NMDAR potent
T76590	(d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin
	(d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin，是一种催产素受体拮抗剂，可消除 CA1 锥体神经元中催产素增强的抑制性突触后电流。
T28653	S-8510 free base SB 737552,SB-737552,S8510,SB737552,S-8510,S 8510
	S-8510 is a GABA-A receptor inverse agonist. S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimal electroconvulsive shock- or strychnine-induced convulsion in ddY mice. S-8510 ameliorated memory impairment induced
TP1895	KYL peptide KYL
	KYL peptide is an EphA4 receptor tyrosine kinase inhibitor (Kd = 0.8 μM); inhibits EphA4-EphrinA5 interactions (IC50 = 6.34 μM). Prevents AβO induced synaptic damage, dendritic spine loss and prevents the blocking of LTP in hippocampal CA3-CA1 transmissions. Exhibits a long half life in cell culture media (8 and 12 hours in PC3 and C2C12 media respectively). Neuroprotective.
TP1945	Pep2m, myristoylated
	Cell-permeable, myristoylated form of pep2m. Peptide inhibitor of the interaction between the C-terminus of the GluA2 (AMPA receptor) subunit and N-ethylmaleimide-sensitive fusion protein (NSF), a protein that regulates AMPA receptor function. Reduces pos
T70063	GYKI 52466 HCl
	GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of general...
T64672	Colivelin TFA
	Colivelin (sequence SALLRSIPAPAGASRLLLLTGEIDLP) is composed of activity-dependent neurotrophic factor (ADNF) C-terminally fused to AGA-(C8R)HNG17, a potent HN derivative. It works as a neuroprotective peptide and activator of STAT3. Colivelin-induced neuroprotection has been confirmed to occur via two neuroprotective pathways: one mediated by Ca2+/calmodulin-dependent protein kinase IV, triggered by ADNF, and one mediated by signal transducer and activator of transcription 3, triggered by HN. Co...
T37388	Afizagabar
	Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy[1]. Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons[1]. Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes t...

化合物

Bucladesine sodium

Cat.No: T1418

Synonym: dbcAMP,Dibutyryl-cAMP sodium salt,布拉地新钠盐,Dibutyryl-cAMP,DC2797,Sodium dibutyryl cAMP,Bucladesine,Bucladesine sodium salt

Target: PKA, PDE

Cat.No: T22967

Synonym: MEDICA 16

Target: GPR, Others, ATP Citrate Lyase

Cat.No: T10601

Target: Others

Cat.No: T5315

Synonym: TCA-1,TCA 1

Target: Antibacterial, Antibiotic

Cat.No: T40296

Synonym: MCA17-1

KCa1.1 channel activator-2

Cat.No: T72195

KCa1.1 channel activator-1

Cat.No: T72194

Cat.No: T10600

Target: Others

KYL acetate(676657-00-4 free base)

Cat.No: TP1895L1

Target: Ephrin Receptor

Pep2m, myristoylated acetate

Cat.No: TP1945L1

Synonym: Pep2m, myristoylated acetate(1423381-07-0 free base)

Target: PKC

Cat.No: T38192

Target: Others

Cat.No: T0782

Synonym: Aquatag,苄噻嗪,Lemazide,Dihydrex

Target: Carbonic Anhydrase

Cat.No: T73099

Synonym: Trimethylopropane phosphate

Cat.No: T37208

Cat.No: T24919

Synonym: UBP 714,UBP-714

(d(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin

Cat.No: T76590

S-8510 free base

Cat.No: T28653

Synonym: SB 737552,SB-737552,S8510,SB737552,S-8510,S 8510

Cat.No: TP1895

Synonym: KYL

Pep2m, myristoylated

Cat.No: TP1945

Cat.No: T70063

Cat.No: T64672

Cat.No: T37388

Cat. No.	Product Name	Target	Signaling Pathways
T9143	D-Isoleucine (2R,3R)-2-Amino-3-methylpentanoic acid,D-异亮氨酸,(R)-Isoleucine	Others	Others
	D-Isoleucine ((2R,3R)-2-Amino-3-methylpentanoic acid) 是一种异亮氨酸立体异构体，是 Asc-1 反转运蛋白的选择性激活剂。它能够释放内源性 D-丝氨酸，提高海马 CA1-CA3 的长期增效作用。
TN1601	Effusol 灯心草菲酚,厄弗酚	Caspase	Apoptosis; Proteases/Proteasome
	Effusol 是一种从 Juncus effuses 中分离到的酚类物质，对 DPPH 自由基(IC50:79 μM) 及 ABTS 自由基(IC50:2.73 μM)具有较强的清除活性。它能挽救皮质酮减弱的 CA1 LTP，保护海马功能对抗应激诱导的认知能力下降。
T14011	2-Arachidonoylglycerol	Cannabinoid Receptor; Endogenous Metabolite	GPCR/G Protein; Metabolism
	2-Arachidonoylglycerol 属于人内源性代谢物，是中枢神经系统中的一种内源性大麻素配体。
T6S2115	Ginkgolide J BN 52024,7-beta-Hydroxyginkgolide A,银杏内酯 J,银杏内酯J	PDE	Metabolism
	Ginkgolide J (BN 52024) 是一种银杏叶中非黄酮部分的主要成分(IC50:12-54 µM)，具有神经保护和抗神经元凋亡功能。
T36448	(E)-Ajoene
	(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanoth...

天然产物

Cat.No: T9143

Synonym: (2R,3R)-2-Amino-3-methylpentanoic acid,D-异亮氨酸,(R)-Isoleucine

Target: Others

Cat.No: TN1601

Synonym: 灯心草菲酚,厄弗酚

Target: Caspase

2-Arachidonoylglycerol

Cat.No: T14011

Target: Cannabinoid Receptor, Endogenous Metabolite

Cat.No: T6S2115

Synonym: BN 52024,7-beta-Hydroxyginkgolide A,银杏内酯 J,银杏内酯J

Target: PDE

Cat.No: T36448

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