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21

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1790	Fosaprepitant dimeglumine 福沙匹坦二甲葡胺,L785298,福沙吡坦二甲葡胺,MK-0517,Fosaprepitant dimeglumine salt	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Fosaprepitant dimeglumine (MK-0517) 是 Aprepitant 的前药。它是一种神经激肽 1 受体拮抗剂，可用于预防化疗引起的恶心呕吐。
T68068L	(R)-CJ 11974	Neurokinin receptor	GPCR/G Protein; Neuroscience

T10244	ACY-1083	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	ACY-1083 是一种选择性和脑穿透性 HDAC6 抑制剂 (IC50：3 nM)，可有效逆转化疗引起的周围神经病变。
T3716	Rolapitant 罗拉吡坦,SCH619734,罗拉匹坦	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Rolapitant (SCH619734) 是一种高效选择性具有口服活性的神经激肽 1 受体抑制剂，Ki 值为0.66 nM。
T0776	Phenothiazine ENT 38,吩噻嗪	Dopamine Receptor; Antibacterial; Antibiotic; Antifungal	GPCR/G Protein; Microbiology/Virology; Neuroscience
	Phenothiazine (ENT 38) 是一种抗生素，具有杀虫，抗菌，驱虫和杀真菌活性。它也可研究神经系统疾病。
T2589	Dolasetron Mesylate hydrate Dalasetron Mesylate Hydrate,多拉司琼甲磺酸盐一水合物	5-HT Receptor	GPCR/G Protein; Neuroscience
	Dolasetron Mesylate hydrate (Dalasetron Mesylate Hydrate) 是一种选择性血清素受体拮抗剂，可竞争性阻断血清素对 5HT3 受体的作用，从而抑制化疗和放疗引起的恶心和呕吐。
T9955	EX-A5758	NOS	Immunology/Inflammation
	EX-A5758是一种新型推定的小分子 nNOS-NOS1 AP 抑制剂，可抑制炎症性伤害感受和化疗引起的神经性疼痛，并与紫杉醇协同降低肿瘤细胞活力
T39024	PrNMI	Cannabinoid Receptor	GPCR/G Protein
	PrNMI是一种针对外周限制性大麻素1受体(CB1R)的高效、口服活性激动剂。它展现出显著的镇痛特性，有效抑制化疗引起的周围神经病痛症状及癌症引起的骨痛。
T22393	Palonosetron RS25259,帕洛诺司琼,RS 25259 197	5-HT Receptor	GPCR/G Protein; Neuroscience
	Palonosetron, a 5-HT3 antagonist with Ki of 0.17 nM, is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
T68371	Rolapitant hydrochloride hydrate
	Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of ...
T38692	Fabesetron 法贝司琼,FK1052 free base
	Fabesetron (FK1052) is an orally active compound that acts as a dual antagonist, targeting both the 5-HT3 and 5-HT4 receptors. It exhibits efficacy in studying emesis induced by cancer chemotherapy, showing potential for managing both acute and delayed symptoms.
T82475	Emfilermin
	Emfilermin，一种重组人白血病抑制因子 (LIF)，适用于研究化疗引发的周围神经病变。
T72820	(R)-Casopitant (R)-GW679769
	(R)-Casopitant ((R)-GW679769) 是Casopitant 的异构体。Casopitant 是一种 NK(1)-受体拮抗剂。Casopitant 可用于化疗引起的恶心和呕吐的研究。
T81424	Polysaccharidase Tremella polysaccharide
	Polysaccharidase (Tremella polysaccharide) 是一种提升免疫功能的真菌多糖。该化合物展现出治疗化疗和放疗导致的白细胞减少症的研究潜力。
T79303	IACS-52825
	IACS-52825是一种选择性DLK抑制剂，具有1.3 nM的Kd值，适用于研究化疗引起的周围神经病变。
T72184	Ac-Tyr-Val-Lys-Asp-aldehyde
	Ac-Tyr-Val-Lys-Asp-aldehyde，一种caspase-1抑制剂，适用于慢性疾病相关贫血、化疗诱导贫血及钻石黑扇贫血的研究。
T60305	ZLc-002
	ZLc-002 是一种选择性的 nNOS-Capon 偶联小分子抑制剂。ZLc-002 抑制炎症和化疗引起的神经性疼痛。ZLc-002 可用于焦虑和炎症研究。
T72866	(Rac)-ZLc-002
	(Rac)-ZLc-002 是nNOS 与一氧化氮合酶 1 衔接蛋白 (NOS1AP) 相互作用的抑制剂，抑制炎症性痛觉和化疗诱导的神经性疼痛，并与 Paclitaxel 协同降低肿瘤细胞活力。
T72623	Nampt activator-3
	NAMPTactivator-3 是一种 NAT 衍生物，是一种 NAMPT 激活剂，EC50为 2.6 μM，KD 为 132 nM。NAMPTactivator-3 有效保护培养细胞免受 FK866 介导的毒性。NAMPTactivator-3 在化疗引起的周围神经病变 (CIPN) 小鼠模型中表现出强大的神经保护功效，没有任何明显的毒性。
T65440	Sodium Thiosulfate Pentahydrate
	Sodium thiosulfate (Pentahydrate) is an antioxidant and antifungal. Sodium thiosulfate protects against cisplatin-induced hearing loss in children and is not associated with serious adverse events attributed to its use[3]. The addition of sodium thiosulfate, administered 6 hours after cisplatin chemotherapy, resulted in a lower incidence of cisplatin-induced hearing loss among children with standard-risk hepatoblastoma, without jeopardizing overall or event-free survival[4]. Calciphylaxis is a p...
T36521	Alaproclate (hydrochloride)
	Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentratio...

化合物

Fosaprepitant dimeglumine

Cat.No: T1790

Synonym: 福沙匹坦二甲葡胺,L785298,福沙吡坦二甲葡胺,MK-0517,Fosaprepitant dimeglumine salt

Target: Neurokinin receptor

Cat.No: T68068L

Target: Neurokinin receptor

Cat.No: T10244

Target: HDAC

Cat.No: T3716

Synonym: 罗拉吡坦,SCH619734,罗拉匹坦

Target: Neurokinin receptor

Cat.No: T0776

Synonym: ENT 38,吩噻嗪

Target: Dopamine Receptor, Antibacterial, Antibiotic, Antifungal

Dolasetron Mesylate hydrate

Cat.No: T2589

Synonym: Dalasetron Mesylate Hydrate,多拉司琼甲磺酸盐一水合物

Target: 5-HT Receptor

Cat.No: T9955

Target: NOS

Cat.No: T39024

Target: Cannabinoid Receptor

Cat.No: T22393

Synonym: RS25259,帕洛诺司琼,RS 25259 197

Target: 5-HT Receptor

Rolapitant hydrochloride hydrate

Cat.No: T68371

Cat.No: T38692

Synonym: 法贝司琼,FK1052 free base

Cat.No: T82475

Cat.No: T72820

Synonym: (R)-GW679769

Polysaccharidase

Cat.No: T81424

Synonym: Tremella polysaccharide

Cat.No: T79303

Ac-Tyr-Val-Lys-Asp-aldehyde

Cat.No: T72184

Cat.No: T60305

Cat.No: T72866

Nampt activator-3

Cat.No: T72623

Sodium Thiosulfate Pentahydrate

Cat.No: T65440

Alaproclate (hydrochloride)

Cat.No: T36521

Cat. No.	Product Name	Target	Signaling Pathways
T1156	Palonosetron hydrochloride 盐酸帕洛诺司琼,RS 25259 197,Palonosetron HCl,RS 25259	5-HT Receptor	GPCR/G Protein; Neuroscience
	Palonosetron hydrochloride (RS 25259) 是一种 5-HT3 拮抗剂，用于预防和治疗化疗引起的恶心和呕吐。
T1285	Anethole trithione 茴三硫,Anetholtrithion	Others; AChR	Neuroscience; Others
	Anethole trithione (Anetholtrithion) 是硫杂环胆碱，是一种胆汁分泌刺激剂，可增强唾液分泌并增加 mAChR 受体，用于口干症的研究。
T2563	Acetyl-L-carnitine hydrochloride Acetyl L-carnitine hydrochloride,O-Acetylcarnitine,乙酰-L-肉(毒)碱盐酸盐,O-acetyl-L-carnitine,O-Acetyl-L-carnitine hydrochloride	Others; Endogenous Metabolite	Metabolism; Others
	Acetyl-L-carnitine hydrochloride (Acetyl L-carnitine hydrochloride) 是一种由内源性左旋肉碱的乙酰化形式的盐酸盐组成的营养补充剂，具有潜在的神经保护、认知增强、抗抑郁和免疫调节活性。还可缓解化疗、糖尿病或其他疾病引起的周围神经病变。此外，乙酰左旋肉碱可能通过增加T淋巴细胞成熟来调节免疫反应，并可能下调促炎细胞因子对病毒(如SARS-CoV-2)的反应。它还可能破坏ACE2信号通路并抑制活性氧(ROS)的产生。

天然产物

Palonosetron hydrochloride

Cat.No: T1156

Synonym: 盐酸帕洛诺司琼,RS 25259 197,Palonosetron HCl,RS 25259

Target: 5-HT Receptor

Anethole trithione

Cat.No: T1285

Synonym: 茴三硫,Anetholtrithion

Target: Others, AChR

Acetyl-L-carnitine hydrochloride

Cat.No: T2563

Synonym: Acetyl L-carnitine hydrochloride,O-Acetylcarnitine,乙酰-L-肉(毒)碱盐酸盐,O-acetyl-L-carnitine,O-Acetyl-L-carnitine hydrochloride

Target: Others, Endogenous Metabolite

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