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13

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T6403	Siponimod 辛波莫德,BAF-312	S1P Receptor; LPL Receptor	GPCR/G Protein
	Siponimod (BAF-312) 是有效，选择性的鞘氨醇-1-磷酸 (S1P)受体调节剂，对 S1P1 和 S1P5 受体具有特异性，EC50 分别为 0.39 nM 和 0.98 nM。 BAF312 对 S1P1 和 S1P5 受体的特异性比 S1P2、S1P3 和 S1P4 受体高 1000 倍以上。
T6561	Laquinimod LAQ,ABR-215062,拉喹莫德	Apoptosis; Others; NF-κB	Apoptosis; NF-κB; Others
	Laquinimod (LAQ) 是一种免疫调节剂，可预防中枢神经系统的神经变性和炎症。
T9239	RS-25344	PDE	Metabolism
	RS-25344 是一种有效的选择性磷酸二酯酶 (PDE) 4 抑制剂。它在体外抑制嗜酸性粒细胞趋化性并增加精子的进行性运动。
T22282	Brr2-IN-3 Brr2 Inhibitor 9,Brr2 Inhibitor C9	Others	Others
	Brr2-IN-3 (Brr2 Inhibitor C9) 是选择性 Brr2解旋酶变构抑制剂。它呈剂量依赖性地抑制解旋酶(IC50:1.3 μM)。
T37621	Ezeprogind disulfate	Beta Amyloid	Neuroscience
	Ezeprogind disulfate 是一种神经营养诱导剂。 Ezeprogind disulfate 针对所有神经退行性变，包括 Abeta 蛋白或 tau 蛋白。 Ezeprogind disulfate 可用于神经系统疾病相关研究，包括进行性核上性麻痹（PSP）、tau 蛋白病、阿尔茨海默病和帕金森病等。
T39274	Lumasiran sodium
	Lumasiran sodium, an investigational RNA interference (RNAi) therapeutic agent, targets glycolate oxidase to reduce hepatic oxalate production, thereby reducing urinary oxalate excretion. This compound shows promise in addressing the underlying cause of progressive kidney failure in individuals with primary hyperoxaluria type 1 (PH1).
T72522	Aurora kinase-IN-1
	Aurora kinase-IN-1 是aurora kinase 的有效抑制剂。Aurora kinase-IN-1 上调 G1 细胞周期抑制蛋白 (包括 p21 和 p27) 以及 G1 进行性细胞周期蛋白 D1 的表达，并下调 G1-to-S 进行性细胞周期蛋白，导致细胞周期停滞在 G1/S 边界。Aurora 激酶-IN-1 还诱导细胞凋亡 (apoptosis）。Aurora 激酶-IN-1 是化疗药物的先导化合物。
T40701	Ezeprogind AZP-2006
	Ezeprogind (AZP-2006) is an orally active neurotrophic inducer that effectively addresses the underlying factors contributing to neurodegeneration, with a broad scope extending beyond the conventional targets like Abeta protein and tau protein. Exhibiting potent neuroprotective properties, Ezeprogind is a valuable tool for studying a range of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, Alzheimer's disease, Parkinson's disease, and others.
T35552	Ganglioside GD3 Mixture (sodium salt)
	Ganglioside GD3 is synthesized by the addition of two sialic acid residues to lactosylceramide and can serve as a precursor to the formation of more complex gangliosides by the action of glycosyl- and sialyltransferases. It induces apoptosis in HuT-78 cutaneous T cell lymphoma cells in a concentration-dependent manner and disrupts the mitochondrial membrane potential when used at a concentration of 200 μM. Expression of ganglioside GD3 in GD3-negative SK-MEL-28-N1 malignant melanoma cells increa...
T38090	3'-sulfo Galactosylsphingosine (ammonium salt)
	3'-sulfo Galactosylsphingosine is a form of sulfatide that is lacking the fatty acyl group. It decreases migration and adhesion of B35 neuroblastoma cells and increases cell rounding when used at a concentration of 20 μM. It also inhibits PKC and cytochrome c oxidase activity when used at concentrations of 150 and 50-100 μM, respectively. 3'-sulfo Galactosylsphingosine accumulates in patients with metachromatic leukodystrophy, a lysosomal storage disorder characterized by arylsulfatase A (ASA) d...
T38187	6-Aminophenanthridine
	6-Aminophenanthridine is an antiprion agent. It inhibits prion formation in yeast- and mammalian-based screening assays when used alone and, to a greater extent, when used in combination with the α2-adrenergic receptor agonist guanabenz . 6-Aminophenanthridine (300 μM) inhibits protein folding activity of the ribosome (PFAR) by directly competing with protein substrates for the active site and decreases the yield of refolded protein without affecting the refolding rate. It prevents progressive w...
T61607	Laquinimod sodium
	Laquinimod (ABR-215062) sodium 是一种可口服的羧酰胺衍生物，是一种有效的免疫调节剂，可防止中枢神经系统的神经变性和炎症。Laquinimod sodium 减少星形胶质细胞NF-κB 的活化以防止铜酮 (Cuprizone) 诱导的脱髓鞘。Laquinimod sodium 具有用于多发性硬化症 (MS；RRMS 或 CPMS) 的复发缓解 (RR) 和慢性进行性 (CP) 形式以及神经退行性疾病研究的潜力。
T83772	1-Linoleoyl Lysophosphatidic Acid sodium 1-Linoleoyl-2-hydroxy-sn-glycero-3-PA,LPA(18:2),PA(18:2(9Z,12Z)/0:0),1-Octadecadienoyl-2-hydroxy-sn-glycero-3-phosphate,18:2 Lyso PA,1-Octadecadienoyl-2-hydroxy-sn-glycero-3-PA,PA(18:2/0:0),1-Linoleoyl-2-hydroxy-sn-glycero-3-phosphate,1-Linoleoyl LPA
	1-Linoleoyl LPA（1-亚油酰LPA）是LPA2受体的激动剂，属于一种含有亚油酸的甘油磷脂，在sn-1位置含亚油酸。它是小鼠和人体血浆中最丰富的LPA。1-Linoleoyl LPA在表达LPA2受体的Sf9细胞中选择性地增加细胞内钙水平（EC50约为10 nM），相较于表达LPA1和LPA3受体的Sf9细胞（EC50分别约为200和80 nM）。携带NCTC克隆2472肿瘤的小鼠中，1-linoleoyl LPA的血清水平增加。与患有初发进行性多发性硬化症的患者相比，复发缓解型多发性硬化症患者的血浆1-Linoleoyl LPA水平降低，且与神经功能缺损严重程度负相关。

化合物

Cat.No: T6403

Synonym: 辛波莫德,BAF-312

Target: S1P Receptor, LPL Receptor

Cat.No: T6561

Synonym: LAQ,ABR-215062,拉喹莫德

Target: Apoptosis, Others, NF-κB

Cat.No: T9239

Target: PDE

Cat.No: T22282

Synonym: Brr2 Inhibitor 9,Brr2 Inhibitor C9

Target: Others

Ezeprogind disulfate

Cat.No: T37621

Target: Beta Amyloid

Lumasiran sodium

Cat.No: T39274

Aurora kinase-IN-1

Cat.No: T72522

Cat.No: T40701

Synonym: AZP-2006

Ganglioside GD3 Mixture (sodium salt)

Cat.No: T35552

3'-sulfo Galactosylsphingosine (ammonium salt)

Cat.No: T38090

6-Aminophenanthridine

Cat.No: T38187

Laquinimod sodium

Cat.No: T61607

1-Linoleoyl Lysophosphatidic Acid sodium

Cat.No: T83772

Synonym: 1-Linoleoyl-2-hydroxy-sn-glycero-3-PA,LPA(18:2),PA(18:2(9Z,12Z)/0:0),1-Octadecadienoyl-2-hydroxy-sn-glycero-3-phosphate,18:2 Lyso PA,1-Octadecadienoyl-2-hydroxy-sn-glycero-3-PA,PA(18:2/0:0),1-Linoleoyl-2-hydroxy-sn-glycero-3-phosphate,1-Linoleoyl LPA

Cat. No.	Product Name	Target	Signaling Pathways
T37177	Norcholic Acid
	Norcholic acid is a bile acid and 23-carbon derivative of cholic acid .1Levels of norcholic acid are increased in the urine of patients with liver cirrhosis or cerebrotendinous xanthomatosis (CTX), an inborn error of metabolism characterized by a deficiency in the mitochondrial enzyme sterol 27-hydrolylase (CYP27A1) that leads to progressive neurological symptoms.2,3,4

天然产物

Cat.No: T37177

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