il 13

RTIL 13 is a highly effective inhibitor of dynamin GTPase, exhibiting an IC50 value of 2.3 μM for dynamin I GTPase. Furthermore, it selectively interacts with the pleckstrin homology lipid binding domain. This compound effectively suppresses both receptor-mediated and synaptic vesicle endocytosis, demonstrating IC50 values of 9.3 μM and 7.1 μM, respectively.

Dupilumab (REGN-668) 是一种用于AD 的全身免疫调节剂。Dupilumab 是一种针对白细胞介素-4受体α亚基的完全人类单克隆抗体，可抑制IL-4和IL-13下游信号传导，具有改善特应性皮炎的作用。

PF-07038124 HCl 是一种具有选择性和高效性的 PDE4 抑制剂，对 PDE4B2 的 IC50 为0.5 nM。PF-07038124 HCl 抑制 IL-13、IL-4 和 IFNγ，可用于研究特应性皮炎和斑块状银屑病等皮肤疾病。

Tralokinumab 是一种全人源 IgG4 单克隆抗体，对单独的 IL-13 亲和力较高。Tralokinumab 具有潜在的抗炎活性，可预防IL-13与受体相互作用和随后的下游信号传导，可用于研究特应性皮炎 (AD) 。

Rolinsatamab 是一种完全人源化的选择性单克隆抗体，是一种有效的 IL-4 和 IL-13 双重抑制剂。Rolinsatamab 嵌合抗原受体序列 T 细胞。Rolinsatamab 可用于预防和治疗免疫疾病。

Abrezekimab (VR 942) 由 CDP7766、亮氨酸和海藻糖组成。Abrezekimab 是一种人源化靶向人 IL-13 的抗体。Abrezekimab 制止与 IL-13Rα1 亚基的结合。Abrezekimab 可用于研究哮喘和肺部疾病相关的生物障碍。

PDE4-IN-8 (Example 5) 是磷酸二酯酶4(PDE4)的有效抑制剂。PDE4-IN-8 对 PDE4B2 的 IC50值为 0.93 nM。然而，PDE4-IN-8 对 IL13、IL4、IFNy 的抑制作用微弱，IC50值分别为 4.04 nM, 36.33 nM, 2394 nM。

Cendakimab (RPC4046) 是一种靶向 IL-13 的人源化抗体，通过抑制白细胞介素（IL）-13受体（IL13R-α1和IL13R-α2）的结合，选择性地靶向白细胞介素（IL）-13，可用于研究特应性皮炎。

CNTO 607 (Anti-IL-13 Antibody) 是靶向 IL-13 的人源化抗体，可用于研究炎症。

Riltovetbart 是一种抗 IL-13 的单克隆抗体，同型对照是 IgG2 κ，来源是犬。

5-Fluorouracil-13C,15N2 is intended for use as an internal standard for the quantification of 5-flurouracil by GC- or LC-MS. 5-Fluorouracil is a pyrimidine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis. Intracellular metabolites of 5-fluorouracil exert cytotoxic effects by either inhibiting thymidylate synthetase, or through incorporation into RNA and DNA, ultimately initiating apoptosis.

Tadalafil-13C-d3 是 Tadalafil 的 13C 和氘代化合物。Tadalafil 的 CAS 号为 171596-29-5。Tadalafil 是一种PDE5抑制剂，IC50为 1.8 nM。

Sildenafil-13C-d3 是 Sildenafil 的 13C 和氘代化合物。Sildenafil 的 CAS 号为 139755-83-2。Sildenafil 是一种磷酸二酯酶 5 抑制剂，IC50为 5.22 nM。

Avanafil-13C-d3 是 Avanafil 的 13C 和氘代化合物。Avanafil 的 CAS 号为 330784-47-9。Avanafil 是一种高活性PDE-5抑制剂，IC50=5.2 nM，对PDE1，PDE6和PDE11活性较低。

IL-4-inhibitor-1 是 IL-4 的抑制剂 (EC50 = 1.81 µM)。

13-Methylberberine chloride 是一种黄连素类似物，可增加 IL-12 的产生，并在 LPS 激活的巨噬细胞转录后抑制 iNOS 的表达，具有抗脂肪和抗肿瘤作用。

Beclomethasone 17-propionate (倍氯米松17-单丙酸盐)是一种糖皮质激素，是Beclomethasone dipropionate（BDP）的活性代谢产物。作为糖皮质激素受体 (GR) 激动剂，17-BMP的亲和力比BDP高13倍，抑制促炎细胞因子的产生，如CXCL8、TNFα和IL-6，从而发挥抗炎作用，主要用于治疗哮喘、过敏性鼻炎等。

GED-0507-34 Levo((S)-3-(4-氨基苯基)-2-甲氧基丙酸)是一种可口服的PPARγ调节剂，用于改善炎症驱动的肠道纤维化，降低了促纤维化基因Acta2、COL1a1和Fn1的表达，减少了纤维化主要标志物α-SMA和胶原蛋白I-II的蛋白水平，以及TGFβ Smad途径的主要成分，降低了IL-13、CTGF、TGFB和ACTA1的表达，抑制了TGF-β诱导的成纤维细胞和IECs细胞系的活化。

NLRP3-IN-60 (Compound 39) 是一种口服生物活性的NLRP3抑制剂。在THP-1细胞中抑制pyroptosis，IC50值为13 nM。在人全血中，NLRP3-IN-60 抑制IL-1β释放，IC50值为225 nM。

PROTAC BTK Degrader-13 (Compound 25) 是一种专门靶向BTK的PROTAC降解剂，具有DC50为0.27 μM的活性。该化合物对BTK的抑制作用IC50值为0.44 μM，并对IL-2诱导的T细胞激酶（ITK）显示IC50为2.16 μM的抑制活性。同时，PROTAC BTK Degrader-13 能抑制p38 MAPK信号通路，阻止BCR（B细胞受体）信号通路被激活。(Pink: ligand for target protein BTK ligand 15; Black: linker; Blue: ligand for E3 ligase cereblon)

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decreases phorbol 12-myristate 13-acetate (TPA)- and ionomycin-induced increased expression of COX-2 (IC50= 1 μM) and protein levels of IL-2 in Jurkat cells (IC50= 5.2 μM).1 1.Rether, J., Serwe, A., Anke, T., et al.Inhibition of inducible tumor necrosis factor-α expression by the fungal epipolythiodiketopiperazine gliovirinBiol. Chem.388(6)627-637(2007) 2.Howell, C.R., and Stipanovic, R.D.Gliovirin, a new antibiotic from Gliocladium virens, and its role in the biological control of Pythium ultimumCan. J. Microbiol.29(3)321-324(1983) 3.Iwatsuki, M., Otoguro, K., Ishiyama, A., et al.In vitro antitrypanosomal activity of 12 low-molecular-weight antibiotics and observations of structure/activity relationshipsJ. Antibiot. (Tokyo)63(10)619-622(2010)

T-5342126 is a toll-like receptor 4 (TLR4) antagonist.1It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50= 27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s = 110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-dependent mice.2 1.Chavez, S.A., Martinko, A.J., Lau, C., et al.Development of β-amino alcohol derivatives that inhibit toll-like receptor 4 mediated inflammatory response as potential antisepticsJ. Med. Chem.54(13)4659-4669(2011) 2.Bajo, M., Montgomery, S.E., Cates, L.N., et al.Evaluation of TLR4 inhibitor, T5342126, in modulation of ethanol-drinking behavior in alcohol-dependent miceAlcohol Alcohol.51(5)541-548(2016)

C2 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide . C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0 G1 phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells.