tr 1

LY3022859 (IMC-TR1) 是靶向 TBFbR2 的人源化抗体，可用于研究晚期实体瘤。

TR antagonist 1 是一种高效甲状腺激素受体（TR）拮抗剂（对 TRα 和 TRβ 的 IC50 分别为 36 和 22 nM），可用于研究内分泌异常引起的疾病。

TRβ agonist 1 为一种选择性且对突变敏感的甲状腺激素受体 β (TRβ) 激动剂，其EC50值为21 nM。该化合物适用于血脂异常、非酒精性脂肪性肝炎 (NASH) 与甲状腺激素抵抗 (RTH) 研究。

Meclinertant (SR 48692) 是神经降压素受体-1（NT1）拮抗剂，可阻断神经降压素诱导的兴奋，可用于研究神经系统疾病。

Trifluoromethyl-tubercidin (TFMT)可抑制宿主Mtr1并抑制病毒复制。TFMT 通过其S-adenosyl-l-methionine 结合袋相互作用抑制Mtr1，限制流感病毒复制。TFMT 能有效抑制病毒在小鼠体内的复制，毒性很小。

Montelukast sodium (MK0476) 是可口服的半胱氨酸白三烯受体1 选择性拮抗剂，可用于研究预防哮喘和肝损伤。它还可减少心脏损伤，在肠缺血-再灌注损伤中也具有抗氧化作用。

TbPTR1 inhibitor 2 被确定为改进的蝶啶还原酶-1 (PTR1) 抑制剂和抗锥虫药物的新发展。

7-Amino-4-(trifluoromethyl)coumarin (Coumarin 151) 是一种荧光标记物，其激发和发射波长分别为400和500 nm，可用来灵敏的检测蛋白酶。

BTR-1 (5-Benzylidene-3-ethyl rhodanine) 是一种活性抗癌剂， 可激活细胞凋亡并诱导细胞死亡。它能够诱导细胞周期 S 期停滞，影响 DNA 复制。

Aristolochic acid A 是植物提取物 Aristolochic acids 的主要成分，主要存在于 Aristolochia和 Asarum 草本植物中，能够显著降低激活蛋白1（AP-1）和NF-κB的活性，并下调人细胞中与膀胱癌相关的BLCAP基因的表达，常用于诱导肾毒性模型。

Nevanimibe is an orally active and selective inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) (EC50 of 9 nM).

Nevanimibe hydrochloride (PD-132301 hydrochloride) 是一种口服有效的，选择性酰基辅酶 A：胆固醇 O-酰基转移酶 1 抑制剂，EC50为 9 nM。它抑制 ACAT2，EC50为 368 nM。它诱导细胞凋亡，具有抗肾上腺皮质癌的潜力。

Montelukast (Singular) 是可口服的半胱氨酸白三烯受体1 选择性拮抗剂，可用于研究预防哮喘和肝损伤。它还可减少心脏损伤，在肠缺血-再灌注损伤中也具有抗氧化作用。

SBI-553 是能透过血脑屏障的NTR1的别构抑制剂，EC50值为 0.34 μM。

LZTR1-KRAS modulator 1 作为一种KRAS-LZTR1相互作用的调节剂，能够促进LZTR1-KRAS复合物的聚集。

TR-100 是一种小分子抑制剂，靶向肿瘤相关肌钙蛋白 (Tpm)。通过与 Tpm3.1 的 C-末端结合，TR-100 改变了 Tpm3.1 和肌动蛋白丝之间的相互作用，从而影响肌动蛋白丝束的稳定性和功能。此机制使 TR-100 在不影响心肌功能的前提下，特异性地作用于癌细胞的肌动蛋白丝束。TR-100 可用于研究 Tpm3.1 在癌细胞增殖和存活中的作用，以及 Tpm3.1 在胰岛素刺激下对葡萄糖摄取和胰岛素分泌的影响。

Fimasartan (BR-A-657) 是血管紧张素受体 AT1 非肽类拮抗剂，用于研究高血压和心力衰竭。

MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂，在豚鼠和人肺膜的 Ki 分别为0.22 和 2.1 nM。

Naloxegol oxalate (NKTR-118) 是一种外周选择性 opioid 样物质拮抗剂，用于治疗 opioid 样物质引起的便秘。

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.

Resolvin conjugate in tissue regeneration 1 (RCTR1) is a specialized pro-resolving mediator (SPM) biosynthesized from docosahexaenoic acid by isolated human macrophages and apoptotic polymorphonuclear (PMN) neutrophils.1It has been found in human spleen and bone marrow.2RCTR1 is produced via lipoxygenase-mediated oxidation of DHA to 7(S)-8-epoxy-17(S)-HDHA, which is conjugated to glutathione.1,2,3RCTR1 (10 nM) increases phagocytosis ofE. colior apoptotic neutrophils in isolated human monocyte-derived macrophages.2It decreases chemotaxis induced by leukotriene B4in isolated human neutrophils when used at a concentration of 10 nM. RCTR1 (1 and 10 nM) accelerates tissue regeneration in planaria. Intraperitoneal administration of RCTR1 (100 ng/animal) shortens the inflammatory resolution period and decreases inflammatory exudate neutrophil infiltration in a mouse model ofE. coli-induced peritonitis. 1.Dalli, J., Ramon, S., Norris, P.C., et al.Novel proresolving and tissue-regenerative resolvin and protectin sulfido-conjugated pathwaysFASEB J.29(5)2120-2136(2015) 2.de la Rosa, X., Norris, P.C., Chiang, N., et al.Identification and complete stereochemical assignments of the new resolvin conjugates in tissue regeneration in human tissues that stimulate proresolving phagocyte functions and tissue regenerationAm. J. Pathol.188(4)950-966(2018) 3.Rodriguez, A.R., and Spur, B.W.First total synthesis of pro-resolving and tissue-regenerative resolvin sulfido-conjugatesTetrahedron Lett.58(16)1662-1668(2017)

Protectin conjugates in tissue regeneration 1 (PCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid . DHA is oxidized to 16S,17S-epoxy-protectin, which is then converted to PCTR1 by glutathione S-transferase. PCTR1 levels increase during resolution of acute microbial-induced peritonitis in mice. PCTR1 (30 ng, i.p.) administration 12 hours post-infection increases macrophage numbers and activity and shortens the resolution phase of inflammation by 57%. It also reduces the levels of PGE2 , PGD2 , and TXB2 in peritoneal exudates.

Maresin conjugates in tissue regeneration 1 (MCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages at the site of inflammation. DHA is oxidized to maresin 1 , which is then converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase. MCTR1 accelerates tissue regeneration in planaria (1 and 100 nM). Pretreatment with MCTR1 (50 ng/mouse, i.p.) prior to E. coli administration reduces neutrophil infiltration, shortens the inflammatory resolution period, and increases phagocytosis of E. coli by macrophages. When administered at a dose of 100 ng 12h post E. coli infection in a mouse model of peritonitis, MCTR1 reduces the amount of eicosanoids in the exudate.

TR-14035 (MDK-1191) 是一种具有口服活性的 α4β7/α4β1整合素双重抑制剂，对 α4β7和 α4β1作用的 IC50值分别为 7 和 87 nM，可用于炎症和自体免疫疾病的研究。