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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T40130	Nur77 modulator 1 Nur77 modulator 1	Others	Others
	Nur77 modulator 1 可与Nur77结合，KD 为 3.58 μM。它上调 Nur77 表达，介导Nur77亚细胞定位，诱导Nur77 依赖的内质网应激和自噬，可导致细胞凋亡，Nur77 modulator 1显示出抗肝癌生物活性。
T1467	Acemetacin 阿西美辛,K-708,TVX 1322	COX	Immunology/Inflammation; Neuroscience
	Acemetacin (TVX 1322) 是一种非甾体抗炎类的化合物。
T6341	PF04929113 PF-04929113,SNX-5422,PF 04929113	HSP; HER	Angiogenesis; Cytoskeletal Signaling; JAK/STAT signaling; Metabolism; Tyrosine Kinase/Adaptors
	PF04929113 (SNX-5422) 是一种合成的新型小分子 Hsp90 抑制剂。作为一种具有强大疗效和耐受性的口服制剂，它被定位为一种突破性疗法，在广泛的癌症中具有广泛的适用性。
T23146	PHA 568487 free base PHA 568487	AChR	Neuroscience
	PHA 568487 free base 是一种选择性的 α7 烟碱乙酰胆碱受体激动剂，可用于减缓神经炎症。
T1180	Blonanserin 布南色林,AD-5423	Dopamine Receptor; Sigma receptor; 5-HT Receptor; Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Blonanserin (AD-5423) 是一种有效的5-HT2A 和多巴胺 D2 受体拮抗剂，Ki 为 0.812 和 0.142 nM，是一种非典型的抗精神病试剂。
T14199	ALZ-801 Valiltramiprosate	Beta Amyloid	Neuroscience
	ALZ-801 是一种可口服的小分子 β-淀粉样蛋白抗寡聚体和聚集抑制剂，是曲米酸的缬氨酸偶联前药，与母体化合物相比，具有显著改善的 PK 特性和胃肠道耐受性。它是治疗阿尔茨海默病的先进且显著改善的候选药物。
T81263	RMC-7977	Ras	GPCR/G Protein; MAPK
	RMC-7977是一种可逆的三重复合RAS抑制剂，对KRAS、NRAS和HRAS的突变型及野生型(WT)变体表现出广谱活性。该化合物能够引发肿瘤消退，在多种依赖RAS的临床前癌症模型中显示出良好的耐受性。此外，RMC-7977还能有效抑制KRASG12C癌瘤模型的生长。[1]
T14313	Apricitabine AVX754,SPD754	HIV Protease; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
	Apricitabine (SPD754) 是一种具有高选择性和口服活性的HIV-1逆转录酶抑制剂(Ki=0.08μM)，是2′-脱氧-3′-氧-4′-硫代胞苷(dOTC)的(-)对映体。 Apricitabine 对DNA 聚合酶α、β和γ具有抑制作用，Ki 值分别为300μM、12μM 和112.25μM。Apricitabine 在抗逆转录病毒HIV 感染者中显示出良好的抗逆转录病毒治疗效果，具有良好的耐受性和较低的选择性抗性。
T73990	Lipid M
	Lipid M (pKa: 6.75) 可用于递送 mRNA 疫苗，引发强大的免疫反应并提高耐受性。
T64045	Antitubercular agent-20
	Antitubercular agent-20 是口服具有活力的抗结核剂。Antitubercular agent-20 对 MTB H37Rv 和 MDR-MTB 表现出良好的抗结核效果，其 MIC＜0.016 μg/ml。在 BALB/c 小鼠中，Antitubercular agent-20 表现出较低的细胞毒性和较好的耐受性。
T70930	GSK SYK inhibitor
	The immunoregulator spleen tyrosine kinase (SYK) is upregulated in cutaneous lupus erythematosus (CLE). This double-blind, multicentre, Phase Ib study evaluated the safety, tolerability, pharmacokinetics, pharmacodynamics and clinical efficacy of the selective SYK inhibitor GSK2646264 in active CLE lesions
T78529	Pelacarsen TQJ230,AKCEA-APO(a)-LRx,ISIS 681257
	Pelacarsen (AKCEA-APO(a)-LRx)为一肝脏特异性反义寡核苷酸，靶向载脂蛋白(a)（apolipoprotein(a)），能够降低高达80%的脂蛋白(a)浓度，并展示出良好的耐受性。
T21394	Sarecycline hydrochloride P005672,P-005672,WC-3035,WC 3035,Sarecycline HCl,WC3035,P 005672
	Sarecycline, a novel and tetracycline-derived antibiotic, is being developed for use as an oral once daily antibiotic treatment for patients suffering from moderate to severe acne vulgaris. Sarecycline has anti-inflammatory activity and the potential for
T70837	Rimegepant sulfate hydrate
	Rimegepant, also known as BMS-927711 and BHV-3000, is a potent, selective, competitive, and orally active calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraines. Rimegepant has shown in vivo efficacy without vasoconstriction effect. BMS-927711 is superior to placebo at several different doses (75 mg, 150 mg, and 300 mg) and has an excellent tolerability profile.
T80079	Mazdutide TFA LY-3305677 TFA,IBI-362 TFA,OXM-3 TFA
	Mazdutide (IBI-362; LY-3305677) TFA 是一款GLP-1R与GCGR的共激动剂，同时是长效合成胃泌酸调节素类似物。该化合物安全性和耐受性良好，适用于肥胖与T2D研究。
T70138	AZ0108
	AZ0108 is an orally bioavailable, potent PARP1,2,6 inhibitor that potently inhibits centrosome clustering and is suitable for in vivo efficacy and tolerability studies. AZ0108 has been utilized as in vitro tools and in vivo probes to investigate the biological consequences of inhibiting centrosome clustering through PARP enzymes. AZ0108 is more selective in its enzyme inhibition profile and effects on cellular pathways and phenotypes. Specifically, AZ0108 inhibits PARPs 1, 2, and 6 with approxi...
T73117	ROCK2-IN-5
	ROCK2-IN-5是一种复合型化合物，融合了Rho激酶抑制剂fasudil以及NRF2诱导剂咖啡酸和阿魏酸的结构元素。该化合物展示了优秀的多靶点作用特性和较高的耐受性。ROCK2-IN-5在针对SOD1基因变异型ALS研究中具备应用潜力。
T78546	Abraxane Nab-Paclitaxel
	Abraxane（Nab-Paclitaxel）为一种Paclitaxel纳米颗粒与白蛋白结合的制剂，展现出较高的疗效及耐受性。通过利用白蛋白传递Paclitaxel，Abraxane形成优异的药代动力学特性。
T81355	PTC258
	PTC258为针对伸长复合体蛋白1基因（ELP1）的特异性口服基因剪接调节剂，能促进ELP1在体外和体内的表达增加，并在小鼠模型中显示出良好的耐受性。
T72990	BAY 1214784
	BAY 1214784是一种针对人促性腺激素释放激素受体(hGnRH-R)的高效、选择性口服活性拮抗剂，属于螺二氢吲哚衍生物化合物。该化合物能显著降低血浆促黄体激素水平，最高可达49%，同时显示出较低的药代动力学变异性和良好的耐受性，表现出研究子宫肌瘤的潜力。
T78097	Mazdutide IBI-362,LY-3305677,OXM-3
	Mazdutide (IBI-362; LY-3305677) 是一种具有安全性和耐受性的胃泌酸调节素类似物，用于肥胖和2型糖尿病(T2D)的研究。它同时作为胰高血糖素样肽(GLP-1R)和胰高血糖素受体(GCGR)的共激动剂，表现出长效作用。
T37014	Inupadenant
	Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity[1]. [1]. Laurence Buisseret, et al. Phase 1 trial of the adenosine A2Areceptor antagonist inupadenant (EOS-850): Update on tolerability, and antitumor activity potentially associated with the expression of the A2A receptor within the tumor. Journal of Clinical Oncology. Volume 39, Issue 15_suppl.
T22233	Aliskiren
	Aliskiren(CGP 60536)是口服有效的肾素抑制剂，IC50为1.5 nM。
T37441	KMN-80
	The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other pro...

化合物

Nur77 modulator 1

Cat.No: T40130

Synonym: Nur77 modulator 1

Target: Others

Cat.No: T1467

Synonym: 阿西美辛,K-708,TVX 1322

Target: COX

Cat.No: T6341

Synonym: PF-04929113,SNX-5422,PF 04929113

Target: HSP, HER

PHA 568487 free base

Cat.No: T23146

Synonym: PHA 568487

Target: AChR

Cat.No: T1180

Synonym: 布南色林,AD-5423

Target: Dopamine Receptor, Sigma receptor, 5-HT Receptor, Adrenergic Receptor

Cat.No: T14199

Synonym: Valiltramiprosate

Target: Beta Amyloid

Cat.No: T81263

Target: Ras

Cat.No: T14313

Synonym: AVX754,SPD754

Target: HIV Protease, DNA/RNA Synthesis

Cat.No: T73990

Antitubercular agent-20

Cat.No: T64045

GSK SYK inhibitor

Cat.No: T70930

Cat.No: T78529

Synonym: TQJ230,AKCEA-APO(a)-LRx,ISIS 681257

Sarecycline hydrochloride

Cat.No: T21394

Synonym: P005672,P-005672,WC-3035,WC 3035,Sarecycline HCl,WC3035,P 005672

Rimegepant sulfate hydrate

Cat.No: T70837

Cat.No: T80079

Synonym: LY-3305677 TFA,IBI-362 TFA,OXM-3 TFA

Cat.No: T70138

Cat.No: T73117

Cat.No: T78546

Synonym: Nab-Paclitaxel

Cat.No: T81355

Cat.No: T72990

Cat.No: T78097

Synonym: IBI-362,LY-3305677,OXM-3

Cat.No: T37014

Cat.No: T22233

Cat.No: T37441

Cat. No.	Product Name	Target	Signaling Pathways
T13506	3β-Ursodeoxycholic acid Isoursodeoxycholic acid
	3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) 是一种胆汁酸。3β-Ursodeoxycholic acid 经口服给药表现出良好的耐受性和良好的肠道吸收能力。3β-Ursodeoxycholic acid 可以在肠道和肝脏经历酶异构化，并生成UDCA。

天然产物

3β-Ursodeoxycholic acid

Cat.No: T13506

Synonym: Isoursodeoxycholic acid

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