nkt

α-Galactosylceramide (KRN7000) 是一种具有抗肿瘤和免疫刺激作用的合成糖脂。它是一种高效的 NKT 细胞激动剂，可与 CD1d 有效结合。它与 CD1d 的复合物可与 NKT 细胞的 T 细胞抗原受体结合。

human tachykinin NK1 receptor antagonist

Gusperimus trihydrochloride is a derivative of the antitumor antibiotic spergualin with immunosuppressant activity.

Naloxegol (NKTR-118; AZ-13337019) is an opioid-receptor antagonist[1]. [1]. Yoon SC, et al. Naloxegol in opioid-induced constipation: a new paradigm in the treatment of a common problem. Patient Prefer Adherence. 2017 Jul 24;11:1265-1271.

Senktide 是速激肽NK3受体激动剂。

Senktide acetate 是一种选择性速激肽 NK3 受体激动剂，促进 ELM 的巩固或表达，可用于研究阿尔茨海默症。

Vadaclidine is an orally acting antinociceptive muscarinic agonist.

SR-33805 is a calcium channel antagonist potentially for the treatment of atherosclerosis and heart failure. SR-33805 restored the MI-altered cell shortening without affecting the Ca(2+) transient amplitude, suggesting an increase of myofilament Ca(2+) sensitivity in MI myocytes. A SR33805-induced sensitization of myofilament activation was found to be associated with a slight increase in myosin light chain-2 phosphorylation and a more significant decrease on troponin I (TnI) phosphorylation. Decreased TnI phosphorylation was related to inhibition of protein kinase A activity by SR-33805.

Inbakicept 是一种 IL-15 受体α sushi 结构域与免疫球蛋白 G1（人 Fc 片段）融合蛋白二聚体，是一种 IL-15 超级激动剂蛋白复合物。 Inbakicept 与 IL-15 抗体 Nogapendekin alfa 可以结合形成复合物 Nogapendekin alfa inbakicept (ALT-803)，比例为1：2。ALT-803 具有潜在的抗癌抗肿瘤活性，可用于研究乳腺癌。

Dendrotoxin K TFA是一种特异的Kv1.1通道阻滞剂，通过时间依赖性方式调控突触前尖峰波形成，影响到谷氨酸在CA3神经元的释放。

Nogapendekin alfa inbakicept 是一种 IL-15 超级激动剂，能够激活 NK 细胞和 T 细胞，从而增强抗肿瘤免疫应答，目前正在用于非肌层浸润性膀胱癌 (NMIBC) 的研究。

α-Galactosylceramide analog 8 (α-GalCer analog 8) is a triazole derivative of α-galactosylceramide. [1] It increases IL-2 secretion by DN32.D3 NKT hybridoma cells when co-cultured with CD1d-transfected RBL cells pre-loaded with α-GalCer analog 8 at a concentration of 32 ng ml. α-GalCer analog 8 (32 ng ml) induces IL-4 secretion to a greater extent than the synthetic α-GalCer KRN 7000 in mouse splenocytes in vitro and in mouse serum following administration of a 1 µg per animal dose, indicating a Th2 response.

Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminomethyl)benzamide) is the analogue of BMS-509744, which can potently and selectively inhibit Itk kinase activity. In vitro: BMS-509744 could reduce TCR-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells [1]. In vivo: BMS-509744 suppressed the production of IL-2 induced by anti-TCR antibody administered to mice. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma [1]. Clinical trial: Up to now, both BMS-509744 and ITK inhibitor is still in the preclinical development stage.

KBC-007 is a synthetic branched chain-containing analog of α-galactosylceramide (α-GalCer). It induces IL-4 and IFN-γ secretion by mouse splenocytes when used at a concentration of 0.5 ng/ml and IL-2 secretion by DN32.D3 NKT hybridoma cells co-cultured with CD1d-transfected RBL cells pre-loaded with KBC-007 at a concentration of 8 ng/ml. KBC-007 (1 μg per animal) increases levels of IL-4, but not IFN-γ, to a similar degree as α-GalCer in mouse serum. KBC-007 (0.5 μg per animal) increases the survival rate of mice immunized with the inactivated influenza A virus A/PR/8/34 in a model of influenza infection.

ABX196, 作为NKT激动剂，是母体化合物-GalCer的类似物。

GCS-12 作为一种 Th1 2 平衡的磺酰胺糖脂,主要通过增强与CD1d的相互作用来发挥作用.该化合物能激活自然杀伤 T 细胞 (NKT cell),诱导它们分泌细胞因子IFN-γ和IL-4,进而在小鼠体内展示出显著的免疫调节和抗肿瘤活性.

GCS-11 是一种高效的 NKT 细胞激动剂,特别选择性地促进 IFN-γ 的产生,同时也能增加 IL-4 的分泌.该化合物展现了显著的抗癌活性,并可能作为癌症免疫治疗或疫苗开发中的有前途佐剂.

Nanrilkefusp alfa (SO-C101; SOT101) 是一种选择性的强效融合蛋白，由IL-15和IL-15Rαsushi+结构域组成。该化合物通过增殖和激活记忆性 CD8+T 细胞、自然杀伤细胞、γ δ T 细胞及自然杀伤 T 细胞，有效抑制肿瘤。在多种小鼠肿瘤模型中，Nanrilkefusp alfa 显著抑制肿瘤生长并防止黑色素瘤的远处转移。