net-1

SAHA chloroalkane T1 is a novel compound formed by combining Vorinostat (SAHA) with a chloroalkane capture tag, referred to as T1. This innovative approach involves tethering the SAHA molecule with the T1 tag, resulting in the formation of SAHA chloroalkane T1.

C24 Phytosphingosine (t18:0/24:0) is a phytoceramide, which is a family of sphingolipids found in the intestine, kidney, and extracellular spaces of the stratum corneum of the mammalian epidermis. C24 Phytosphingosine (t18:0/24:0) is composed of a phytosphingosine backbone amine-linked to a C24 fatty acid chain. It has been used with other ceramides to create stratum corneum substitutes to study percutaneous penetration and psoriasis in vitro. In a stratum corneum model of healthy skin, the incorporation of long-chain-containing phytoceramides, such as C24 phytosphingosine (t18:0/24:0), increases permeability of the membrane in comparison with incorporation of dihydroceramides.

XRP44X (XRP 44X) 是Ras 诱导的转录激活的抑制剂，IC50为 10 nM，通过 FGF-2 抑制 Ras-Erk-1 2 通路激活。它抑制Elk3。它还对微管有影响。

Cavα2δ1&NET-IN-1 是电压门控钙通道 α2δ-1 亚单位 (Cavα2δ-1) 和去甲肾上腺素转运蛋白 (NET) 的双重抑制剂。Cavα2δ1&NET-IN-1 抑制 Cavα2δ-1 的 Ki 为 112 nM。Cavα2δ1&NET-IN-1 抑制 NET 的 Ki 为 383 nM，IC50为 67 nM。Cavα2δ1&NET-IN-1 可用于疼痛研究。

Atomoxetine-d3 hydrochloride 是氘代标记的Atomoxetine hydrochloride。Atomoxetine hydrochloride 是去甲肾上腺素重吸收抑制剂，与人NET，SERT 和DAT 的放射性配体结合的 Ki 分别为5，77和1451 nM。

NEt-iFQ 是一种荧光视黄醇 X 受体 (RXR) 激动剂，具溶剂变色性。NEt-iFQ 可选择性结合 RXR-LBP 并发荧光。

Prostaglandin F2αethyl amide (PGF2α-NEt), a PGF2α analog featuring an N-ethyl amide modification at the C-1 carboxyl group, possesses ocular hypotensive activity similar to PG esters. Introduced as alternative prostaglandin ocular hypotensive prodrugs, PGF2α-NEt and other PG N-ethyl amides, contrary to claims of not converting to free acids in vivo, have been demonstrated by our laboratory studies to undergo conversion by bovine and human corneal tissue into the respective free acids at a rate of approximately 2.5 µg g corneal tissue hr. This suggests PGF2α-NEt is expected to elicit typical PGF2α free acid intraocular effects, albeit with slower hydrolysis kinetics characteristic of PG N-amides.

Cavα2δ1&NET-IN-2 是电压门控钙通道 α2δ-1 亚单位 (Cavα2δ-1) 和去甲肾上腺素转运蛋白 (NET) 的双重抑制剂。Cavα2δ1&NET-IN-2 抑制 Cavα2δ-1 的Ki 为 454 nM。Cavα2δ1&NET-IN-2 抑制 NET 的Ki 为 59 nM，IC50为 7 nM。Cavα2δ1&NET-IN-2 可用于疼痛研究。

DOTA-JR11为SSTR2生长抑素受体拮抗剂，能经68Ga标记，应用于神经内分泌肿瘤（NETs）配对成像研究。

DOTA-LM3是一款靶向生长抑素受体(SSTR)的拮抗剂，其结构为p-Cl-Phe-cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2。该化合物通常通过同位素标记，如177Lu-DOTA-LM3和68Ga-DOTA-LM3，进行体内肿瘤示踪。68Ga-DOTA-LM3显示出有优异的生物分布特性、高度的肿瘤摄取能力、稳定的肿瘤内保留及较低的安全风险。而177Lu-DOTA-LM3则被用于研究DOTATOC阴性的肝转移案例，针对胰腺NET和广泛性的肿瘤血栓形成治疗具有潜在应用价值。

Cavα2δ1&NET-IN-3 (example 216) 是电压门控钙通道 (VGCC) 的亚基 α2δ 和去甲肾上腺素转运蛋白 (NET) 抑制剂。Cavα2δ1&NET-IN-3 对人的 Cav2.2 钙通道 α2δ-1 亚基和 NET 的 Ki 均为 100-500 nM。

N-Methyl-2-phenylpropan-1-amine hydrochloride 是 β-甲基苯乙胺 (BMPEA) 的类似物，在 NET 和 DAT 的实验测定中显示出神经递质释放的活性。

4’-hydroxy Atomoxetine glucuronide is a metabolite of the norepinephrine transporter (NET) inhibitor atomoxetine .1It is formed from atomoxetine by glucuronidation of the intermediate metabolite 4-hydroxy atomoxetine.2 1.Todor, I., Popa, A., Neag, M., et al.Evaluation of a potential metabolism-mediated drug-drug interaction between atomoxetine and bupropion in healthy volunteersJ. Pharm. Pharm. Sci.19(2)198-207(2016) 2.Sauer, J.-M., Ring, B.J., and Witcher, J.W.Clinical pharmacokinetics of atomoxetineClin. Pharmacokinet.44(6)571-590(2005)

2-chloro Palmitic acid is a monochlorinated form of palmitic acid . It is produced in a myeloperoxidase (MPO) and time-dependent manner in neutrophils stimulated by phorbol 12-myristate 13-acetate . 2-chloro Palmitic acid (10 μM) induces neutrophil extracellular trap (NET) formation (NETosis) in human neutrophils, increasing DNA release from neutrophils, colocalization of MPO with extracellular DNA (ecDNA), and trapping of E. coli. It increases COX-2 protein levels in human coronary artery endothelial cells (HCAECs) when used at a concentration of 50 μM and increases production of P-selectin, von Willebrand factor, and angiopoietin-2 in HCAECs, as well as neutrophil and platelet adherence, when used at a concentration of 10 μM. 2-chloro Palmitic acid (10-50 μM) also induces apoptosis in THP-1 cells and primary human monocytes and increases caspase-3 activity in THP-1 cells.

DOTA-LM3 TFA是一種特定結合生長抑素受體(SSTR)的拮抗劑。其結構為p-Cl-Phe-cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2。這種複合物常以177Lu-DOTA-LM3 TFA和68Ga-DOTA-LM3 TFA的形式被同位素標記，用於腫瘤的體內示踪。68Ga-DOTA-LM3 TFA展示了優異的生物分布特性、高腫瘤吸收率、良好的腫瘤保留性以及較低的安全風險。而177Lu-DOTA-LM3 TFA則被用於研究DOTATOC陰性的肝轉移，例如胰腺神經內分泌腫瘤(NET)和廣泛的腫瘤血栓形成。

PAD4-IN-3（compound 4B）是PAD4抑制剂，表现出体内外的抗肿瘤活性。该化合物通过共价连接RGD序列肽修饰的壳聚糖（K-CRGDV），形成增强的氧化应激反应性纳米剂。K-CRGDV-PAD4-IN-3能够主动靶向肿瘤，抑制PAD4活性，阻断中性粒细胞胞外陷阱（NET）的形成，并通过改善肿瘤免疫微环境来响应肿瘤微环境。

Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity. Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg g corneal tissue hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides.