ligation

Tussilagone 是Tussilago farfara 的主要活性成分，具有抗炎作用。它抑制盲肠结扎和穿刺导致脓毒症的小鼠的炎症反应，提高其生存率。它改善葡聚糖硫酸钠诱导的小鼠结肠炎的炎症反应。

Dermorphin 是在两栖类皮肤中发现的天然七肽，是 μ-阿片受体激动剂，可用于抑制神经痛。

Dermorphin TFA 是在两栖类皮肤中发现的天然七肽，是 μ-阿片受体激动剂，可用于抑制神经痛。

Sivopixant (S-600918) 是P2X3受体选择性拮抗剂 (P2X3IC50=4.2 nM; P2X2 3IC50=1100 nM)。Sivopixant 可用于缓解疼痛的研究。

Astragaloside IV (AS-IV) 是从黄芪中分离得到的一种皂苷，抑制ERK1 2和JNK 激活，在乳腺癌细胞 MDA-MB-231 中，下调(MMP)-2和(MMP)-9的信号通路。

Gue1654 是一种选择性 OXE-R 抑制剂，通过激活 BCAT1 缓解冠状动脉结扎诱导的小鼠缺血性心肌损伤和心肌细胞氧 葡萄糖剥夺诱导的损伤。Gue1654 抑制 OXE-R 抑制的蛋白激酶 C-ε （PKC-ε） 核因子 κB （NF-κB） 信号传导和心肌细胞凋亡。Gue1654 可用于研究心血管疾病。

SIRT5 inhibitor 7 (compound 58) 是底物竞争性和选择性的 SIRT5 抑制剂，IC 50 = 310 nM，显著减轻了脂多糖（LPS）和盲肠结扎 穿孔（CLP）诱导的脓毒性AKI小鼠的肾功能障碍和病理损伤，调节急性肾损伤（AKI）小鼠肾脏中蛋白琥珀酰化和促炎细胞因子的释放。

AM281 是选择性CB1受体拮抗剂，IC50=9.91 nM。它抑制 CB2 受体，IC50=13000 nM。

LP-935509 是一种选择性、脑渗透性、小分子接头蛋白-2 相关激酶 1 (AAK1) 竞争性抑制剂，能抑制 articulin-2-associated kinase 1 (AAK1)，其 IC50值为3.3 nM，Ki值为0.9 nM。LP-935509 是 BIKE 的强效抑制剂（IC50值为14 nM）和 GAK 的中度抑制剂（IC50值320±40 nM）。

Ferroptosis-IN-12（Cpd-A1）作为一种ferroptosis抑制剂，能有效抑制Erastin处理的小鼠肾小管上皮细胞（mTECs）中的ferroptosis。该化合物在缺血 再灌注（I R）或盲肠结扎穿刺（CLP）诱导的急性肾损伤（AKI）小鼠模型中显示出剂量依赖性的肾功能改善效果，能减轻肾小管损伤并消除炎症。在药代动力学的研究中，Ferroptosis-IN-12展示了良好的血浆稳定性和在肾脏组织中的高分布性。此外，Ferroptosis-IN-12在急性肾损伤（AKI）研究领域显示出应用潜力。

5-HT6 inverse agonist 1 (Compound 33) 是一种5-HT6受体拮抗剂，其Ki为23 nM，Kb为6.62 nM。该化合物可以抑制5-HT6R介导的Cdk5和mTOR信号通路，并在大鼠模型中减少脊神经结扎 (SNL) 诱导的触觉过敏。

Pyrromecaine is a local anesthetic used for surface anesthesia. Pyromecaine has a wide spectrum of antiarrhythmic action, exerts a favorable effect on the contractility of the left ventricle, and on the myocardial blood flow following the ligation of the

δ14-Triamcinolone acetonide is a potential impurity found in commercial preparations of triamcinolone acetonide. Triamcinolone acetonide is a synthetic corticosteroid. It decreases cytokine levels, the firing rate of sensory neurons, and mechanical hypersensitivity in a rat spinal nerve ligation model when used at a dose of 1.5 mg/kg prior to and following surgery for three days. Triamcinolone acetonide also decreases outflow facility in a mouse model of steroid-induced glaucoma when 20 μl of a 40 mg/ml suspension is administered subconjunctivally. Formulations containing triamcinolone acetonide are used in the treatment of diabetic macular edema.

5’-O-DMT-Ri can be used in the synthesis of oligoribonucleotides[1]. [1]. Kadokura M. Synthesis of 4-thiouridine, 6-thioinosine, and 6-thioguanosine 3’,5’-O-bisphosphates as donor molecules for RNA ligation and their application to the synthesis of photoactivatable TMG-capped U1 snRNA fragments. J Org Chem. 2000 Aug 25;65(17):5104-13.

LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. minnesota Re-LPS and induces agglutination with a minimal agglutinating concentration (MAC) of 12.1 μg/ml. It is a chemoattractant for, and can induce calcium mobilization in, human monocytes, neutrophils, and T cells that naturally express formyl peptide receptor-like 1 (FPRL1) and FPRL1-transfected HEK293 cells. LL-37 (10-15 μM) pretreatment of dengue virus type 2 (DENV-2) reduces its infectivity as well as levels of viral genomic RNA and NS1 antigen. In vivo, LL-37 inhibits cecal ligation and puncture-induced caspase-1 activation and pyroptosis of peritoneal macrophages, reduces levels of the inflammatory cytokines IL-1β, IL-6, and TNF-α, and improves survival in polybacterial septic mice.

Etoposide phosphate disodium (BMY-40481 disodium), a phosphate ester prodrug of etoposide, functions as a potent chemotherapeutic agent by selectively inhibiting topoisomerase II, hindering the re-ligation of DNA strands. It is regarded as the active equivalent of etoposide, effectively inducing cell cycle arrest, apoptosis, and autophagy in cancer cells.

Ni(II) protoporphyrin IX is a metalloporphyrin compound characterized by its limited propensity for axial ligation and its distortion upon binding to ferrochelatase.

BMS-986318 是一种有效的非胆汁酸FXR 激动剂，在FXRGal4 和 SRC-1 募集试验中的EC50分别为 53 和 350 nM。 BMS-986318 具有合适的 ADME 特性，并在肝胆汁淤积和纤维化的小鼠胆管结扎模型中具有效果。BMS-986318 可用于非酒精性脂肪性肝炎 (NASH)的研究。

JHU-58 is a novel dipeptide MrgC agonist. JHU-58 inhibited both mechanical and heat hypersensitivity in rats after an L5 spinal nerve ligation (SNL). JHU58 attenuated the evoked excitatory postsynaptic currents in substantia gelatinosa (SG) neurons in wild-type mice, but not in Mrg knockout mice, after peripheral nerve injury.

Z-LLY-FMK (Calpain Inhibitor IV) 为一种钙蛋白酶抑制剂，涉及调控多个细胞系统的凋亡过程。该化合物能够抑制胆总管结扎所引起的肠细胞凋亡(apoptosis)。

T4 RNA ligase为一RNA连接酶，催化单链DNA分子的连接作用。该酶在酶促低核糖核苷酸合成及RNA 3'端标记过程中应用。

AC-099 hydrochloride（化合物 3）作为NPFF2R的选择性全激动剂（EC50=1189 nM）和NPFF1R的部分激动剂（EC50=2370 nM），可降低大鼠脊神经结扎引起的痛觉超敏。

UFP101是一种合成肽类物质，作为nociceptin受体的拮抗剂（Ki为0.06 nM，测试于表达人类受体的CHO细胞中）。它对nociceptin受体的选择性高于κ-opioid受体（Ki为204 nM，测试于表达大鼠受体的CHO细胞中）。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS（EC50为1.86 nM）。通过脑室内给药，UFP101（10 nmol/每只动物）能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中，UFP101（0.003、0.03及0.3 mg/kg）能提高生存率。

TC 14012是一种化学肽模拟的拮抗剂，针对趋化因子(C-X-C motif)受体4（CXCR4；IC50 = 2.9 nM）和CXCR7激动剂。它能在表达CXCR7的HEK293T细胞中诱导β-arrestin招募（EC50 = 350 nM）。TC 14012可减少HIV在MT-4细胞中的细胞病理效应（EC50 = 0.4 nM），并以CXCR4依赖的方式抑制HIV在体外进入（IC50 = 19.3 nM）。它还能抑制由趋化因子(C-X-C motif)配体12（CXCL12）在MDA-MB-231乳腺癌细胞和人脐静脉内皮细胞（HUVECs）中诱导的迁移，当使用浓度范围从10到1,000 nM时。在通过左前降（LAD）冠状动脉结扎诱导的急性心肌梗死小鼠模型中，TC 14012（10 mg/kg）能减少梗死面积。