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115

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T7436 Cilofexor

FXR; Autophagy Autophagy; Metabolism
Cilofexor 是一种法尼醇 X 受体激动剂,EC50为 43 nM。它抑制合成肽的结合,具有抗炎和抗纤维化作用。它可用于原发性硬化性胆管炎和非酒精性脂肪性肝炎的研究。
T4989 Fosfomycin Tromethamine

Antibacterial; Antibiotic Microbiology/Virology
Fosfomycin tromethamine 是一种能透过血脑屏障的广谱抗生素,不可逆地抑制细胞壁合成的早期阶段。它对多种细菌具有杀菌活性,包括耐多药、广泛耐药和耐全药细菌。
T7596 Firocoxib

非罗考昔,ML 1785713

COX Immunology/Inflammation; Neuroscience
Firocoxib (ML 1785713) 是一种可口服的 COX-2选择性抑制剂,IC50为 0.13 μM。它具有抗炎作用,对 COX-2的选择性比对 COX-1 的选择性高 58 倍,IC50为 7.5 μM。
T16501 PF-3644022

p38 MAPK; Serine Protease; MAPK MAPK; Proteases/Proteasome
PF-3644022 是可口服的,具有 ATP 竞争性的MAPKAPK2 (MK2)选择性抑制剂,IC50为 5.2 nM,Ki 为 3 nM。它有效抑制 TNFα 的产生并具有抗炎作用,还抑制 MK3 和 p38 调节/激活激酶,IC50分别为 53 和 5.0 nM。
T3131 Fosfomycin calcium

Phosphomycin calcium salt,Fosmicin,磷霉素钙

Antibacterial; Antibiotic Microbiology/Virology
Fosfomycin calcium (Phosphomycin calcium salt) 是一种能透过血脑屏障的广谱抗生素,不可逆地抑制细胞壁合成的早期阶段。它对多种细菌具有杀菌活性,包括耐多药、广泛耐药和耐全药细菌。
T61518 TAK-653

iGluR Membrane transporter/Ion channel; Neuroscience
TAK-653, a selective positive allosteric modulator (PAM) of AMPA receptors exhibiting minimal agonistic activity, elicits an antidepressant-like response while maintaining a favorable safety profile in rat models.
T11106 DSP-0565

2-(2'-fluorobiphenyl-2-yl)acetamide

Others Others
DSP-0565 在包括 scPTZ、6 Hz、MES 和杏仁核点燃在内的各种模型中表现出抗惊厥活性和良好的安全裕度。 DSP-0565 可用于作为广谱抗癫痫药物的研究。
T26531 ABT-963

ABT963

ABT-963 is a cyclooxygenase 2 (COX-2) inhibitor potentially for the treatment of osteoarthritis and pain. ABT-963 has excellent selectivity in human whole blood, high oral anti-inflammatory potency in vivo, and gastric safety in the animal studies.
T0911 Cefotaxime sodium

Cefotaxim sodium salt,头孢噻肟钠,Cefotaxime sodium salt,Cefotaxim (sodium salt),HR-756 (sodium salt)

Antibacterial; Antibiotic Microbiology/Virology
Cefotaxime sodium (Cefotaxim sodium salt) 是头孢类抗生素和耐内酰胺酶的头孢菌素,有抗革兰氏阳性菌和革兰氏阴性菌作用。
T25913L P-113 acetate

HIV Protease; Antibacterial; Antibiotic Microbiology/Virology; Proteases/Proteasome
P-113 acetate 是一种源自人类唾液蛋白组氨酸 5 的抗菌肽 (AMP),在患有口腔念珠菌病的牙龈炎和人类免疫缺陷病毒 (HIV) 患者中显示出良好的安全性和有效性。
T15562 Imazamox

CL29926,甲氧咪草烟,(±)-Imazamox

Others Others
Imazamox ((±)-Imazamox) 是一种具有高选择性、高活性、安全性、广谱活性的全身性除草剂,能够抑制植物中乙酰乳酸合酶(ALS) 的产生,进而抑制植物生长并最终导致植物死亡。
T38683 SCD1 inhibitor-3

SCD1-IN-3,SCD1 inhibitor-3,SCD1 inhibitor 17a

Dehydrogenase Metabolism
SCD1 inhibitor-3 (ML-270) 是一种高效、口服的化合物,可以抑制SCD1,且安全性极高。 SCD1 inhibitor-3 显示出在代谢疾病(包括肥胖、二型糖尿病和血脂异常,以及痤疮和癌症等各种皮肤病)方面的巨大研究潜力。
T16125 MMV390048

Parasite; PI4K Microbiology/Virology; PI3K/Akt/mTOR signaling
MMV390048 是一种抗疟药,是一种新型化学疟原虫 PI4K 抑制剂。它与疟原虫 PI4K 的 ATP 结合位点结合,不与除人类 PIP4K2C 外的其他恶性疟原虫和人类激酶结合。
T7587 Tenapanor

RDX-5791,RDX 5791,AZD 1722,Tenapanor free base,RDX5791,AZD-1722,AZD1722

Sodium Channel Membrane transporter/Ion channel
Tenapanor (RDX 5791) 是钠氢离子交换NHE3的有效抑制剂, 对人和大鼠NHE3的IC50分别是5和10 nM。
T72031 BI 1015550

PDE Metabolism
BI 1015550 是一种具有口服活性的PDE4B 抑制剂,IC50值为 7.2 nM。BI 1015550 具有良好的安全性,在炎症、过敏疾病、肺纤维化和慢性阻塞性肺疾病 (COPD) 中有潜在应用。
T0056 Oxeladin citrate

Others Others
Oxeladin citrate 是止咳剂,能够对各种病因引发咳嗽进行有效研究。
T0910 Terpin hydrate

Terpin Monohydrate,cis-Terpin hydrate,萜品(水合结晶)

Others Others
Terpin hydrate 是一种祛痰药,可除去急慢性支气管炎病人的黏液。
T3560 Desmethylanethol trithione

ADT-OH

VEGFR; Akt Angiogenesis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
Desmethylanethol trithione (ADT-OH) 是合成硫化氢的供体。它利用上调 FADD 诱导细胞凋亡,并对体内黑色素瘤的形成具有一定的抑制作用,可用于研究癌症疾病。
T4616 Metoclopramide

甲氧氯普胺,胃复安,5-Chloro-2-methoxyprocainamide

Dopamine Receptor; 5-HT Receptor GPCR/G Protein; Neuroscience
Metoclopramide (5-Chloro-2-methoxyprocainamide) 是5-HT3和多巴胺D2受体拮抗剂,IC50值分别为 308 和 483 nM,可用于恶心呕吐、胃食管反流和胃轻瘫的研究。
T4615 Balsalazide sodium hydrate

巴柳氮钠水合物,Balsalazide disodium dihydrate,巴柳氮钠,Balsalazide disodium salt dihydrate,Balsalazide disodium

STAT; Interleukin Immunology/Inflammation; JAK/STAT signaling; Stem Cells
Balsalazide sodium hydrate (Balsalazide disodium) 可通过调节IL-6/STAT3通路起抑癌作用,可用于治疗炎症性肠病。
T23986 Dezinamide

ADD94057,ADD-94057,ADD 94057

Dezinamide is a potential antiepileptic drug. It shows preliminary evidence of efficacy and safety in an open-label study.
T13548 AN7973

Others Others
AN7973 blocks intracellular parasite development and inhibits Cryptosporidium growth. It is orally active, possesses favorable safety, stability, and PK parameters.
T30513 BMS-317180

BMS317180

BMS-317180 is a potent, novel, orally effective growth hormone secretagogue (GHS) that shows an excellent safety profile in preclinical studies. The compound was advanced into clinical development.
T0157L Roxatidine acetate

Roxatidine acetate is an anti-ulcer agent and histamine antagonist that inhibits gastric acid secretion. Compared to other similar drugs, Roxatidine acetate has an improved safety profile, in part because lower doses of roxatidine acetate are therapeutica
T33392 MIP-1095 I-123

123-I-MIP-1095,(123I)MIP 1095

MIP-1095 I-123, as a radiotracer, is under investigation in clinical trial NCT00712829 (Evaluating the Safety, Pharmacokinetics, Tissue Distribution, Metabolism and Dosimetry of Two Prostate Cancer Imaging Agents).
T70308 PLX7683

PLX7683 is a paradox breaker. Paradox breakers overcame several known mechanisms of resistance to first-generation RAF inhibitors. Dissociating MAPK pathway inhibition from paradoxical activation might yield both improved safety and more durable efficacy than first-generation RAF inhibitors
T27400 Ganaplacide

KAF 156,KAF-156,GNF-156,GNF 156,GNF156,KAF156

Ganaplacide is an antimalarials with activity against asexual and sexual blood stages and the preerythrocytic liver stages of malarial parasites. KAF156 showed antimalarial activity without evident safety concerns in a small number of adults with uncompli
T15651 KDU731

Others Others
KDU731 is a promising drug candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety. KDU731is an orally active C. parvum inhibitor of PI4K (IC50: 25 nM). KDU731 blocks Cryptosporidium infection in vitro and in vi
T74705 5'-ODMT cEt m5U Phosphoramidite (Amidite)

5'-ODMT cEt m5U Phosphoramidite Amidite 为锁核酸(LNA)类似物,具备良好的安全性及反义活性。
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
T70754 NMS-P953

NMS-P953 is a JAK2 inhibitor, displaying significant tumor growth inhibition in SET-​2 xenograft tumor model. NMS-P953 has a mechanism of action confirmed in vivo by typical modulation of known biomarkers, and with a favorable pharmacokinetic and safety profile.
T61388 hAChE/Aβ1-42-IN-1

hAChE/Aβ1-42-IN-1 (Compound 16) 是一种有效的 hAChE 和 Aβ1-42聚集抑制剂。hAChE/Aβ1-42-IN-1 对 hepG2 细胞系显示出可接受的相对安全性,并具有良好的 BBB 渗透性和较宽的安全范围。hAChE/Aβ1-42-IN-1具有研究阿尔茨海默病 (AD) 的潜力。
T11687 Itacitinib adipate

Phosphatase Metabolism
Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor,Itacitinib adipate has been tested for efficacy and safety in a phase II trial in myelofibrosis.
T60761 PF-06305591 dihydrate

PF-06305591 dihydrate 是具有出色的临床前体外 ADME 和安全性的,电压门控钠通道 NaV1.8的高选择性阻断剂 (IC50 = 15 nM)。
T60959 As-358 hydrochloride

As-358 (hydrochloride) 显示出良好的体内安全性,并且抑制埃博拉病毒和马尔堡病毒,IC50值分别为 9.1 μM 和 18.1 μM。
TD0004 Celfinder nucleic acid gel stain *10,000× concentrate in DMSO*

Celfinder is a new kind of nucleic acid dye, which has the advantages of safety and sensitivity, and can be used as a dye for various kinds of nucleic acid electrophoresis.Unlike EB, which is highly carcinogenic, Celfinder is a flower-like dye with low to
T74703 5'-ODMT cEt G Phosphoramidite (Amidite)

5'-ODMT cEt G Phosphoramidite Amidite 是一种具有良好安全性及反义活性的有效核酸类似物。
T73878 NOSO-502

NOSO-502为一种对肠杆菌科表现出抑制效果的细菌翻译(bacterialtranslation)抑制剂,具备良好的安全性及抗菌特性。
T69250 JMX0312

JMX0312 is a salicylamide derivative used as a potent inhibitor of HAdV infection. JMX0312 showed significantly improved anti-HAdV activities with nanomolar to submicromolar IC50 values and high selectivity indexes (SI > 100), indicating better safety windows, compared to those of the lead compound niclosamide.
T32402 KLS-13019

KLS-13019 is a Cannabidiol-Derived Neuroprotective Agent with Improved Potency, Safety, and Permeability. (EC50=40nM; T1=7500). KLS-13019 was 50-fold more potent and >400-fold safer than cannabidiol and exhibited an in vitro profile consistent with imp
T28510 REDX05358

REDX 05358,REDX-05358

REDX05358 is a highly selective and potent pan RAF inhibitor with a potential therapeutic for BRAF and RAS mutant tumors. REDX05358 has improved therapeutic potential and predicted safety profile. REDX05358 demonstrates subnanomolar binding affinity for B
T73875 Fotagliptin benzoate

Fotagliptin benzoate,作为一种二肽基肽酶IV (DPP-4) 抑制剂(IC50=2.27 nM),在大鼠和狗中展现了安全性,适用于2型糖尿病的研究。
T30539 BMS-711939

BMS 711939,BMS711939

BMS-711939 is a potent and specific peroxisome proliferator-activated receptor (PPARα) agonist that has demonstrated excellent efficacy and safety in vivo in preclinical studies with an EC50 of 4 nM for PPARα in humans.
T61797 HIV-1 inhibitor-15

HIV-1 inhibitor-15 (compound 9d) is a potent and broad-spectrum inhibitor targeting HIV-1. It exhibits inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, and E138K with respective EC50 values of 1.7 nM, 4 nM, 2 nM, 6 nM, and 9 nM. In addition to its high efficacy, HIV-1 inhibitor-15 possesses favorable solubility, safety profiles, and oral bioavailability [1].
T79087 Antifungal agent 59

Antifungalagent 59,一种抗真菌剂,具有0.01-1 μg/mL的MIC值,能够有效抑制真菌生物膜的形成,并显示出良好的安全性。
T80613 Linvoseltamab

REGN5458

Linvoseltamab为双特异性抗体,针对BCMA(TNFRSF17)与CD3epsilon。该化合物于复发/难治性多发性骨髓瘤(RRMM)模型中展示了良好的安全性和效力。
T62864 Hetrombopag

Hetrombopag 是一种 thrombopoietin receptor 的有效激动剂。Hetrombopag 具有良好的耐受性且安全性可控。Hetrombopag 具有潜力进行免疫性血小板减少症的研究。
T71157 Neladenoson dalanate

Neladenoson bialanate ; BAY-1067197,BAY-1067197,Neladenoson bialanate

Neladenoson dalanate (Neladenoson bialanate ; BAY-1067197) 是部分腺苷 A1 受体激动剂的前体,具有口服活性。Neladenoson dalanate 具有良好的药代动力学和安全性,可用于慢性心脏疾病的研究。
T64028 Iruplinalkib

Iruplinalkib 是一种选择性的、有效的、口服具有活力的 ALK 和 ROS1 酪氨酸激酶抑制剂。在伴有 ALK 或 ROS1 重排的晚期 NSCLC 中,Iruplinalkib 具有良好的安全性,并表现出抗肿瘤的潜能。
T39587 APJ receptor agonist 4

APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease.

化合物

Cilofexor
Cat.No: T7436
Synonym:
Target: FXR, Autophagy
Fosfomycin Tromethamine
Cat.No: T4989
Synonym:
Target: Antibacterial, Antibiotic
Firocoxib
Cat.No: T7596
Synonym: 非罗考昔,ML 1785713
Target: COX
PF-3644022
Cat.No: T16501
Synonym:
Target: p38 MAPK, Serine Protease, MAPK
Fosfomycin calcium
Cat.No: T3131
Synonym: Phosphomycin calcium salt,Fosmicin,磷霉素钙
Target: Antibacterial, Antibiotic
TAK-653
Cat.No: T61518
Synonym:
Target: iGluR
DSP-0565
Cat.No: T11106
Synonym: 2-(2'-fluorobiphenyl-2-yl)acetamide
Target: Others
ABT-963
Cat.No: T26531
Synonym: ABT963
Target:
Cefotaxime sodium
Cat.No: T0911
Synonym: Cefotaxim sodium salt,头孢噻肟钠,Cefotaxime sodium salt,Cefotaxim (sodium salt),HR-756 (sodium salt)
Target: Antibacterial, Antibiotic
P-113 acetate
Cat.No: T25913L
Synonym:
Target: HIV Protease, Antibacterial, Antibiotic
Imazamox
Cat.No: T15562
Synonym: CL29926,甲氧咪草烟,(±)-Imazamox
Target: Others
SCD1 inhibitor-3
Cat.No: T38683
Synonym: SCD1-IN-3,SCD1 inhibitor-3,SCD1 inhibitor 17a
Target: Dehydrogenase
MMV390048
Cat.No: T16125
Synonym:
Target: Parasite, PI4K
Tenapanor
Cat.No: T7587
Synonym: RDX-5791,RDX 5791,AZD 1722,Tenapanor free base,RDX5791,AZD-1722,AZD1722
Target: Sodium Channel
BI 1015550
Cat.No: T72031
Synonym:
Target: PDE
Oxeladin citrate
Cat.No: T0056
Synonym:
Target: Others
Terpin hydrate
Cat.No: T0910
Synonym: Terpin Monohydrate,cis-Terpin hydrate,萜品(水合结晶)
Target: Others
Desmethylanethol trithione
Cat.No: T3560
Synonym: ADT-OH
Target: VEGFR, Akt
Metoclopramide
Cat.No: T4616
Synonym: 甲氧氯普胺,胃复安,5-Chloro-2-methoxyprocainamide
Target: Dopamine Receptor, 5-HT Receptor
Balsalazide sodium hydrate
Cat.No: T4615
Synonym: 巴柳氮钠水合物,Balsalazide disodium dihydrate,巴柳氮钠,Balsalazide disodium salt dihydrate,Balsalazide disodium
Target: STAT, Interleukin
Dezinamide
Cat.No: T23986
Synonym: ADD94057,ADD-94057,ADD 94057
Target:
AN7973
Cat.No: T13548
Synonym:
Target: Others
BMS-317180
Cat.No: T30513
Synonym: BMS317180
Target:
Roxatidine acetate
Cat.No: T0157L
Synonym:
Target:
MIP-1095 I-123
Cat.No: T33392
Synonym: 123-I-MIP-1095,(123I)MIP 1095
Target:
PLX7683
Cat.No: T70308
Synonym:
Target:
Ganaplacide
Cat.No: T27400
Synonym: KAF 156,KAF-156,GNF-156,GNF 156,GNF156,KAF156
Target:
KDU731
Cat.No: T15651
Synonym:
Target: Others
5'-ODMT cEt m5U Phosphoramidite (Amidite)
Cat.No: T74705
Synonym:
Target:
GSK SYK inhibitor
Cat.No: T70930
Synonym:
Target:
NMS-P953
Cat.No: T70754
Synonym:
Target:
hAChE/Aβ1-42-IN-1
Cat.No: T61388
Synonym:
Target:
Itacitinib adipate
Cat.No: T11687
Synonym:
Target: Phosphatase
PF-06305591 dihydrate
Cat.No: T60761
Synonym:
Target:
As-358 hydrochloride
Cat.No: T60959
Synonym:
Target:
Celfinder nucleic acid gel stain *10,000× concentrate in DMSO*
Cat.No: TD0004
Synonym:
Target:
5'-ODMT cEt G Phosphoramidite (Amidite)
Cat.No: T74703
Synonym:
Target:
NOSO-502
Cat.No: T73878
Synonym:
Target:
JMX0312
Cat.No: T69250
Synonym:
Target:
KLS-13019
Cat.No: T32402
Synonym:
Target:
REDX05358
Cat.No: T28510
Synonym: REDX 05358,REDX-05358
Target:
Fotagliptin benzoate
Cat.No: T73875
Synonym:
Target:
BMS-711939
Cat.No: T30539
Synonym: BMS 711939,BMS711939
Target:
HIV-1 inhibitor-15
Cat.No: T61797
Synonym:
Target:
Antifungal agent 59
Cat.No: T79087
Synonym:
Target:
Linvoseltamab
Cat.No: T80613
Synonym: REGN5458
Target:
Hetrombopag
Cat.No: T62864
Synonym:
Target:
Neladenoson dalanate
Cat.No: T71157
Synonym: Neladenoson bialanate ; BAY-1067197,BAY-1067197,Neladenoson bialanate
Target:
Iruplinalkib
Cat.No: T64028
Synonym:
Target:
APJ receptor agonist 4
Cat.No: T39587
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T8262 Fosfomycin sodium

Fosfomycin Disodium,磷霉素钠

Antibacterial; Antibiotic Microbiology/Virology
Fosfomycin sodium 是一种能透过血脑屏障的广谱抗生素,不可逆地抑制细胞壁合成的早期阶段。它对多种细菌具有杀菌活性,包括耐多药、广泛耐药和耐全药的细菌。
T11589 Hydroxycitric acid tripotassium hydrate

柠檬酸钾一水合物,三水合钾柠檬酸,Potassium citrate monohydrate

ATP Citrate Lyase; HIF/HIF Prolyl-Hydroxylase; HIF Angiogenesis; Chromatin/Epigenetic; Metabolism
Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) 是一种藤黄果的主要活性成分,也是一种柠檬酸的衍生物。它可竞争性抑制柠檬酸裂解酶 (ATP citrate lyase) ,并具有减肥作用。它有效抑制结石形成,并抑制HIF,具有抗氧化,抗炎和抗肿瘤活性。
T0256 Citric acid trilithium salt tetrahydrate

Lithium citrate tribasic tetrahydrate,柠檬酸三锂盐四水合物,Trilithium citrate tetrahydrate

Dehydrogenase; GSK-3; HIF/HIF Prolyl-Hydroxylase; Antibacterial; GluR Chromatin/Epigenetic; Metabolism; Microbiology/Virology; Neuroscience; PI3K/Akt/mTOR signaling; Stem Cells
Citric acid trilithium salt tetrahydrate (Lithium citrate tribasic tetrahydrate) 是一种用于治疗精神疾病的药物。它也是一种医药和建筑材料, 可用于氨基酸定量分析时的梯度洗脱。

天然产物

Fosfomycin sodium
Cat.No: T8262
Synonym: Fosfomycin Disodium,磷霉素钠
Target: Antibacterial, Antibiotic
Hydroxycitric acid tripotassium hydrate
Cat.No: T11589
Synonym: 柠檬酸钾一水合物,三水合钾柠檬酸,Potassium citrate monohydrate
Target: ATP Citrate Lyase, HIF/HIF Prolyl-Hydroxylase, HIF
Citric acid trilithium salt tetrahydrate
Cat.No: T0256
Synonym: Lithium citrate tribasic tetrahydrate,柠檬酸三锂盐四水合物,Trilithium citrate tetrahydrate
Target: Dehydrogenase, GSK-3, HIF/HIF Prolyl-Hydroxylase, Antibacterial, GluR
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