sar-2

SAR-260301 is an orally available and selective inhibitor of PI3Kβ (IC50: 23 nM).

SAR-20347 是 TYK2、JAK1、JAK2和JAK3的抑制剂，IC50值分别为 0.6、23、26 和 41 nM。

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。

SAR296968 is a novel selective NCX inhibitor, improving cardiac function and restoring sympathovagal balance in heart failure.

Pimasertib (AS703026) 是一种高效选择性和ATP 非竞争性的MEK1 2抑制剂，可用于癌症研究。

18:1 PE (DOPE) pSar25 是聚乙二醇的衍生物，适用于脂质体和脂质纳米颗粒的递送系统。

Pilaralisib (XL-147) 是一种有效的、选择性的 I 类PI3Ks 抑制剂，能够抑制 PI3Kα (IC50:39 nM)，PI3Kβ (IC50:383 nM)，PI3Kγ (IC50:23 nM) 和 PI3Kδ (IC50:36 nM)。

Potent P2Y12 antagonist (IC50 = 17 nM). Displays antiplatelet and antithrombotic activity in vivo. Orally available. Boldron et al (2014) N-[6-(4-butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a novel intravenous and oral, reversible, and directly acting P2Y12 antagonist. J.Med.Chem. 57 7293 PMID:25075638

SAR247799（S1P1 agonist 3）是一种选择性和G蛋白偏向性的S1P1激动剂，比β-阻滞蛋白和内化信号通路更优先激活下游G蛋白信号通路，激活内皮细胞上的S1P 1 而不引起受体脱敏，可以保护内皮细胞而不影响淋巴细胞数量，可用于研究2型糖尿病、内皮功能障碍和血管高通透性。

Voxtalisib (XL765) 是一种PI3K 抑制剂，抑制p110α，p110β，p110γ和p110δ。它抑制mTORC1和mTORC2，IC50s 分别为 160 和 910 nM。它也抑制 DNA-PK (其 IC50=150 nM) 和 mTOR (其 IC50=157 nM)。

(+)-Donepezil is an isomer of Donepezil -- a nootropic acting as an inhibitor of acetylcholinesterase.

Seribantumab (MM 121) 是一种靶向 HER3 的人源化单克隆抗体，抑制 NRG1 刺激的 MCF-7 细胞生长和患者来源的乳腺和肺癌细胞的生长携带 NRG1 融合或 NRG1 扩增，抑制表达 CD74-NRG1 融合的同基因 HBEC 细胞的生长，并诱导 MDA-MB-175-VII 和 LUAD-0061AS3 细胞凋亡。

Azide-pSar20 (Azide-Polysarcosine20) 是一种 pSar-脂质衍生物，作为 PEG 的亲水替代品应用于药物递送的研究。

DSPE-pSar20 (DSPE-Polysarcosine20) 是一种 pSar 基的脂质衍生物。作为 PEG 的亲水替代品，DSPE-pSar20 在药物递送研究中具有应用价值。

ONO-5334 是一种具有选择性、口服活性和高效性的组织蛋白酶 K 抑制剂，具有抗 SAR-COV-2 和抗骨吸收活性，可用于研究骨质疏松症。

SAR405838 (MI 773) 是 MI-773 的类似物，具有抗肿瘤活性。它是一种高效、选择性的MDM2-p53相互作用抑制剂，与 MDM2 结合的Ki 值为 0.88 nM。

N-Hydroxypipecolic acid (NHP) 是植物代谢产物和系统性获得性抗性调节剂，可与免疫信号水杨酸协调建立系统性获得性抗性，诱导系统获得性耐药对细菌和卵菌感染。它在植物叶片中系统地积累，以应对病原菌的侵袭。

SAR-7226 Hydrate, a SGLT1 2 inhibitor, is used potentially for the treatment of type 2 diabetes.

SAR-629 is an MGL inhibitor or 2-AG degradation inhibitor.

Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 |Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibitor. Bioorg.Med.Chem.Lett. 11 2007 PMID:11454468 |Williams et al (2003) Development of a scintillation proximity assay for analysis of Na+ Cl- -dependent neurotransmitter transporter activity. Anal. Biochem. 321 31 PMID:12963052

BHBM is an acylhydrazone with antifungal activity.1,2 It is active against C. neoformans in vitro (MIC80 = 1 μg/ml).2 BHBM (0.25, 1, and 4 μg/ml) inhibits the synthesis of glucosylceramide, which is essential to fungal cell division, in C. neoformans but not J774 murine macrophages.1 In vivo, BHBM (1.2 mg/kg per day) increases survival in a mouse model of C. neoformans infection. |1. Haranahalli, K., Lazzarini, C., Sun, Y., et al. SAR studies on aromatic acylhydrazone-based inhibitors of fungal sphingolipid synthesis as next-generation antifungal agents. J. Med. Chem. 62(17), 8249-8273 (2019).|2. Lazzarini, C., Haranahalli, K., Rieger, R., et al. Acylhydrazones as antifungal agents targeting the synthesis of fungal sphingolipids. Antimicrob. Agents Chemother. 62(5), e00156-00118 (2018).

The diazomethyl ketone Z-LVG-CHN2 mimics part of the human cysteine proteinase-binding center, has been shown to be an irreversible inhibitor of this proteinase. The compound was also tested for antiviral activity against herpes simplex virus type 1 (HSV) and found to block the HSV replication. Irreversible inhibitor of streptopain.

Selective prostacyclin IP receptor antagonist (pKi = 8.3). Exhibits no affinity at other prostanoid receptors (EP1-4, FP and TP) in a radioligand binding assay. Demonstrates analgesic activity in rats. Orally bioavailable. Clark et al (2004) Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg.Med.Chem.Lett. 14 1053 PMID:15013022 |Jones et al (2006) Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations. Br.J.Pharmacol. 149 110 PMID:16880763 |Bley et al (2006) RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br.J.Pharmacol. 147 335 PMID:16331286

4-(N-Boc-amino)piperidine is an organic building block.1,2It has been used in the synthesis of aminopiperidine antiviral chemokine (C-C motif) receptor 5 (CCR5) antagonists and antibacterial agents. 1.Burrows, J.N., Cumming, J.G., Fillery, S.M., et al.Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureasBioorg. Med. Chem. Lett.15(1)25-28(2005) 2.Reck, F., Alm, R., Brassil, P., et al.Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II: Broad-spectrum antibacterial agents with reduced hERG activityJ. Med. Chem.54(22)7834-7847(2011)