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82

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7512	BMS-191011 BMS-A	Potassium Channel	Membrane transporter/Ion channel
	BMS-191011 (BMS-A) 是一种大电导 Ca2+激活的钾通道 (Ca2+-activated potassium (maxi-K) channel) 激活剂，在中风模型中有研究价值。
T9532	MRT-81	Others	Others
	MRT-81 是一种人和啮齿动物 smoothened 受体的有效拮抗剂，能够抑制 hedgehog 的活性，在 Shh-light2 细胞中的IC50值为 41 nM。它可用于研究癌症。
T9786	Lu AF27139	P2X Receptor	Membrane transporter/Ion channel; Neuroscience
	Lu AF27139 是一种有效的选择性 P2X7 受体拮抗剂（人和大鼠的 IC50 分别为 12 和 2.4 nM，小鼠、人和大鼠的 Ki 分别为 22、54 和 13 nM）。 Lu AF27139 可用于中枢神经系统疾病研究。
T25824	ML400 ML 400,CID-73050863,ML-400,CID73050863,CID 73050863	Phosphatase	Metabolism
	ML400 (CID73050863) 是 LMPTP 的变构抑制剂，EC50 为 1μM。 ML400 显示出良好的细胞活性和啮齿动物药代动力学。
T21818	Pregnenolone Carbonitrile Pregnenolone 16α-carbonitrile ,5-Pregnen-3β-ol-20-one-16α-carbonitrile	P450	Metabolism
	Pregnenolone Carbonitrile (5-Pregnen-3β-ol-20-one-16α-carbonitrile) 是一种啮齿动物-PXR 的激活剂，可诱导 CYP3A 的表达。
T39762	AHR antagonist 5 free base	Aryl Hydrocarbon Receptor	Immunology/Inflammation
	AHR antagonist 5 free base 是一种具有口服活性的 AHR 拮抗剂，在人和啮齿动物细胞系中的 IC50 约为 35-150 nM。
TP1666L	Kisspeptin-10, rat acetate(478507-53-8 free base)	GPR; Kisspeptin	Endocrinology/Hormones; GPCR/G Protein
	Kisspeptin-10, rat acetate(478507-53-8 free base) 是啮齿动物 Kisspeptin 受体 (KISS1, GPR54) 的内源性配体。
T0489	Flutamide SCH 13521,氟他胺	Androgen Receptor	Endocrinology/Hormones
	Flutamide (SCH 13521) 是一种抗雄激素化合物，在啮齿动物和犬科动物中的效力与环丙孕酮大致相同。
T1860	Imepitoin AWD 131-138,ELB-138,伊匹妥英	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Imepitoin (AWD 131-138) 是一种新型的低亲和力部分苯二氮卓受体激动剂，有抗惊厥和抗焦虑作用。
T40588	Acifluorfen	Others	Others
	Acifluorfen 是一种除草剂。Acifluorfen 是一种原卟啉原氧化酶抑制剂，可促进原卟啉 IX 的积累，并诱导啮齿动物肝脏发生肿瘤。它会引起敏感植物物种中的色素和脂质强烈的光氧化破坏。
T22419	S-Methylisothiourea sulfate (S)-Methylisothiourea sulfate,S-甲基异硫脲硫酸盐,S-甲基异硫脲半硫酸盐	NOS; NO Synthase; HSV	Immunology/Inflammation; Microbiology/Virology
	S-Methylisothiourea sulfate ((S)-Methylisothiourea sulfate) 是一种选择性 iNOS 抑制剂，在感染性休克的啮齿动物模型中发挥有益作用。
T8960	MONNA	Chloride channel	Membrane transporter/Ion channel
	MONNA 是 TMEM16A (Anoctamin-1)阻滞剂，IC50为 80 nM。它在氯离子存在或不存在的情况下诱导啮齿动物抵抗动脉的血管舒张。
T24051	Exisulind Sulindac sulfone,CP248	Apoptosis; PKA	Apoptosis; Tyrosine Kinase/Adaptors
	Exisulind (CP248) 通过激活蛋白激酶 G (PKG) 诱导细胞凋亡。 Exisulind 在实体瘤和血液癌细胞系中表现出抗肿瘤活性，并且是结肠癌、前列腺癌、膀胱癌、乳腺癌和肺癌啮齿动物模型中肿瘤生长的抑制剂。
T16977	Talampanel GYKI-53773,LY-300164	Apoptosis; GluR	Apoptosis; Neuroscience
	Talampanel (LY-300164) 是一种口服和选择型 AMPA 受体拮抗剂，具有抗癫痫活性。在啮齿动物的中风模型中，它具有神经保护作用。Talampanel 减弱 caspase-3 依赖性细胞凋亡。
T15260	Evenamide NW-3509	Sodium Channel	Membrane transporter/Ion channel
	Evenamide (NW-3509) 是一种口服有效的电压门控钠通道 (sodium channel, VGSC) 阻滞剂，Ki 为 0.4 µM，在精神分裂症中有研究价值。Evenamide 在精神病，躁狂症，抑郁和攻击性的各种啮齿动物模型中具有显著功效。
T36851L	Peptide5 acetate	Others	Others
	Peptide5 acetate 可减少脊髓损伤后的动物肿胀、星形胶质细胞增生和神经元细胞死亡。 Peptide5 acetate 显着降低啮齿动物离体模型中的脊髓损伤 (SCI) 程度。
T70084	Dersalazine Dersalazine Free Base	IL Receptor; Platelet aggregation	Immunology/Inflammation; Others
	Dersalazine (Dersalazine Free Base) 是血小板活化因子抑制剂，通过下调 IL-17表达，在不同啮齿动物型结肠炎中发挥肠道抗炎活性，对溃疡性结肠炎患者具有潜在疗效。
T4364	Aftin-4 Aftin 4,Aftin4	Beta Amyloid; Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	Aftin-4 是一种 β-淀粉样蛋白42(Aβ42) 的诱导剂。
T25853	NBQX Disodium FG9202 disodium,NBQX 2Na	GluR	Neuroscience
	NBQX Disodium (FG9202 disodium) 是高度选择性，竞争型的 AMPA 受体拮抗剂，具有保护神经系统和抗惊厥活性的作用。NBQX Disodium 是NBQX 的盐类物质。 NBQX 是一种有效并具有选择性的AMPA /红藻氨酸受体拮抗剂，可用于拮抗谷氨酸的兴奋性毒性。在啮齿类动物模型中具有抗惊厥作用。
T14212	AMG-1694	Glucokinase	Metabolism
	AMG-1694 是一种强效的葡萄糖激酶-葡萄糖激酶调节蛋白（GK-GKRP）干扰物，能促进 GK-GKRP 复合物的解离，其 IC50 值为 7 nM，从而间接提高 GK 酶的活性。AMG-1694 可使几种啮齿动物糖尿病模型的血糖水平恢复正常，并降低糖尿病动物而非正常血糖动物的血糖。AMG-1694 能有效逆转 GKRP 对 GK 活性的抑制作用，并促进 GK 转位。
T4436	RO1138452 CAY10441	Others; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Others
	RO1138452 (CAY10441) 是一种选择性和可口服的前列环素受体拮抗剂，pKi 为8.3。它拮抗卡前列环素诱导的人神经母细胞瘤腺苷酸环化酶的激活，以剂量依赖性方式阻断环 AMP 积累，具有镇痛活性。
T67791	BMS-903452	GPR	Endocrinology/Hormones; GPCR/G Protein
	BMS-903452是一种有效的、具有选择性的 GPR119激动剂，EC50为14 nM。BMS-903452可用于治疗急性和慢性啮齿动物糖尿病。GPR119主要在胰腺 b 细胞和胃肠道肠内分泌细胞中表达，对9种不同的细胞色素 P450酶没有显著的抑制作用(IC50 > 40 μM)，不激活 PXR (EC50>50 μM)，并且对肝脏(HEPG2)细胞系没有毒性。
T1880	P7C3	Others	Others
	P7C3 是一种 aminopropyl carbazole 类化合物，具有口服活性，可透过血脑屏障，具有神经保护作用。它可用于神经退行性疾病，如帕金森病的研究。
T36696	DMBA
	7,12-Dimethylbenz[a]anthracene (DMBA) is a polycyclic aromatic hydrocarbon (PAH) that has been found in tobacco smoke and diesel exhaust and has carcinogenic activity.1,2It undergoes metabolic activation by numerous enzymes, including the cytochrome P450 (CYP450) isoform CYP1B1, as well as microsomal epoxide hydrolase (mEH), producing a variety of reactive metabolites that form DNA adductsin vivo, and it has been commonly used to induce tumor formation in various rodent models.2,3,1DMBA increase...
T31406	Dezaguanine Dezaguanina,NSC 261726,CI-908,CI 908
	Dezaguanine is a novel antipurine antimetabolite with significant activity against transplantable rodent solid tumors, particularly breast adenocarcinoma.
T14356	AVE-8134	PPAR	DNA Damage/DNA Repair; Metabolism
	AVE-8134 is an agonist of PPARα. For human and rodent PPARα receptor, the EC50 values are 100 and 3000 nM, respectively.
TP1666	Kisspeptin-10, rat
	Kisspeptin-10, rat is an Endogenous ligand for the rodent kisspeptin receptor (KISS1, GPR54).
T69135	AGN-2979
	AGN-2979 is a tryptophan hydroxylase (TPH) activation inhibitor that shows antidepressant properties in rodent models of depression.
T28032	MF266-1 MF 266-1,MF-266-1
	MF266-1, a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of osteoarthritis and rheumatoid.
T39502	Lipid 5
	Lipid 5 is an amino lipid compound that demonstrates proficient mRNA delivery in rodent and primate models, displaying favorable pharmacokinetics and minimal toxicity.
T12419	PF-04634817 succinate	COX	Immunology/Inflammation; Neuroscience
	PF-0463481 succinate is a potent and orally active dual antagonist of CCR2/CCR5 with comparable human and rodent CCR2 potency with IC50 of 20.8 nM.
T12419L	PF-04634817	CCR	Immunology/Inflammation; Microbiology/Virology
	PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2/CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481
T69304	MRL20
	MRL20 is a selective PPARγ modulator (SPPARγM) which displays robust anti-diabetic activity with an improved therapeutic window in comparison to a PPARγ full agonist in a rodent efficacy model.
T16113	ML753286	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.
T28894	SZV558 SZV 558,SZV-558
	SZV558 is a potent inhibitor of both human and rodent MAO-B. SZV558 is safe in high doses with no hERG and mutagenic activities and demonstrated neuroprotection in an in vivo chronic model of PD.
T9586	Broparestrol (E)-	Others	Others
	Broparestrol (E)- 具有抗生育活性，是啮齿动物乳腺肿瘤发生的有效抑制剂。
T68955	Musettamycin
	Musettamycin is a potent inducer of erythroid differentiation in hemopoietic cells lines of rodent and human origin. It also has antimicrobial effects similar to the anthracycline class since it inhibits gram-positive bacteria and typically doesn't affect gram-negative bacteria.
T26862	BMS-902483
	BMS-902483 is a potent α7 partial agonist. BMS-902483 improved cognition in preclinical rodent models. BMS-902483 showed FLIR α7 EC50=9.3nM; α7 Electrophysiology, rat; Area EC50 = 140 nM; Peak, Area (Ymax %) = 40, 54. 5-HT3A IC50 = 480 nm.
T68567	AMG-131 besylate
	AMG-131 besylate is a hypoglycemic agent. It is a potent PPARγ partial agonist that displays robust glucose-lowering activity in rodent models of diabetes while exhibiting a reduced side-effects profile compared to marketed TZDs.
T38666	CP-346086 dihydrate
	CP-346086 dihydrate is a potent and orally active inhibitor of microsomal triglyceride transfer protein (MTP), exhibiting an IC50 value of 2.0 nM for both human and rodent MTP. This compound effectively lowers plasma cholesterol and triglyceride levels in vivo.
T69950	Delgocitinib EtOH
	Delgocitinib, also known as LEO-124249 and JTE052, is a potent and selective JAK inhibitor. JTE-052 reduces skin inflammation and ameliorates chronic dermatitis in rodent models: Comparison with conventional therapeutic agents. JTE-052 regulates contact hypersensitivity by downmodulating T cell activation and differentiation.
T39303	CP-346086
	CP-346086 is a highly potent and orally bioavailable inhibitor of microsomal triglyceride transfer protein (MTP), exhibiting an IC50 value of 2.0 nM against both human and rodent MTP. This compound effectively reduces plasma levels of cholesterol and triglycerides when administered in vivo.
TP2340	Hemoregulatory peptide 5b hp 5B,Pglu-glu-asp-cys-lys-OH,Peedck,Glp-glu-asp-cys-lys-OH,SP1 Pentapeptide
	Hemoregulatory peptide 5b is a synthetic analog of granulocyte chalone which initially identified in extracts of rodent bone marrow and human leukocytes. Monomer inhibits both formations of GM-CFC colonies and cytotoxic drug-induced recruitment of murine
T36178	Aspalatone
	Aspalatone is an anti-platelet aggregator (IC50 = 180 μM, in vitro) that prolongs bleeding time significantly in a rodent model of thromboembolism. Additionally at a minimal effective dose of 24 mg/kg, aspalatone generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy in rat hippocampus.
T21886	HE-3235
	Apoptone 是 3β- 雄烷二醇合成类似物，是一种具有口服生物可利用度的抗癌剂。Apoptone 在前列腺癌和乳腺癌的啮齿类动物模型中具有活性。
T78019	Nangibotide TFA LR12 TFA
	Nangibotide TFA为TREM-1受体抑制剂，调控先天免疫反应。该化合物能降低啮齿动物心肌缺血再灌注模型的系统性及局部炎症。
T60537	ARUK3001185
	ARUK3001185 (Compound 8l) 是选择性的、口服有效的、脑渗透性的 Notum 抑制剂（IC50 = 6.7 nM），适合在啮齿动物疾病模型中口服给药。
T14205	AM679	Others	Others
	AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6 nM/154 nM(FLAP binding/hLA/hWB) [1] AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 =
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.
T70639	AM-9514
	AM-9514 is a novel, potent Glucokinase (GK) activator. AM-9514 showed a favorable combination of in vitro potency, enzyme kinetic properties, acceptable pharmacokinetic profiles in preclinical species, and robust efficacy in a rodent PD model. Glucokinase (GK) activators represent a class of type 2 diabetes therapeutics actively pursued due to the central role that GK plays in regulating glucose homeostasis.

化合物

Cat.No: T7512

Synonym: BMS-A

Target: Potassium Channel

Cat.No: T9532

Target: Others

Cat.No: T9786

Target: P2X Receptor

Cat.No: T25824

Synonym: ML 400,CID-73050863,ML-400,CID73050863,CID 73050863

Target: Phosphatase

Pregnenolone Carbonitrile

Cat.No: T21818

Synonym: Pregnenolone 16α-carbonitrile ,5-Pregnen-3β-ol-20-one-16α-carbonitrile

Target: P450

AHR antagonist 5 free base

Cat.No: T39762

Target: Aryl Hydrocarbon Receptor

Kisspeptin-10, rat acetate(478507-53-8 free base)

Cat.No: TP1666L

Target: GPR, Kisspeptin

Cat.No: T0489

Synonym: SCH 13521,氟他胺

Target: Androgen Receptor

Cat.No: T1860

Synonym: AWD 131-138,ELB-138,伊匹妥英

Target: GABA Receptor

Cat.No: T40588

Target: Others

S-Methylisothiourea sulfate

Cat.No: T22419

Synonym: (S)-Methylisothiourea sulfate,S-甲基异硫脲硫酸盐,S-甲基异硫脲半硫酸盐

Target: NOS, NO Synthase, HSV

Cat.No: T8960

Target: Chloride channel

Cat.No: T24051

Synonym: Sulindac sulfone,CP248

Target: Apoptosis, PKA

Cat.No: T16977

Synonym: GYKI-53773,LY-300164

Target: Apoptosis, GluR

Cat.No: T15260

Synonym: NW-3509

Target: Sodium Channel

Peptide5 acetate

Cat.No: T36851L

Target: Others

Cat.No: T70084

Synonym: Dersalazine Free Base

Target: IL Receptor, Platelet aggregation

Cat.No: T4364

Synonym: Aftin 4,Aftin4

Target: Beta Amyloid, Gamma-secretase

Cat.No: T25853

Synonym: FG9202 disodium,NBQX 2Na

Target: GluR

Cat.No: T14212

Target: Glucokinase

Cat.No: T4436

Synonym: CAY10441

Target: Others, Prostaglandin Receptor

Cat.No: T67791

Target: GPR

Cat.No: T1880

Target: Others

Cat.No: T36696

Cat.No: T31406

Synonym: Dezaguanina,NSC 261726,CI-908,CI 908

Cat.No: T14356

Target: PPAR

Kisspeptin-10, rat

Cat.No: TP1666

Cat.No: T69135

Cat.No: T28032

Synonym: MF 266-1,MF-266-1

Cat.No: T39502

PF-04634817 succinate

Cat.No: T12419

Target: COX

Cat.No: T12419L

Target: CCR

Cat.No: T69304

Cat.No: T16113

Target: AMPK

Cat.No: T28894

Synonym: SZV 558,SZV-558

Broparestrol (E)-

Cat.No: T9586

Target: Others

Cat.No: T68955

Cat.No: T26862

AMG-131 besylate

Cat.No: T68567

CP-346086 dihydrate

Cat.No: T38666

Delgocitinib EtOH

Cat.No: T69950

Cat.No: T39303

Hemoregulatory peptide 5b

Cat.No: TP2340

Synonym: hp 5B,Pglu-glu-asp-cys-lys-OH,Peedck,Glp-glu-asp-cys-lys-OH,SP1 Pentapeptide

Cat.No: T36178

Cat.No: T21886

Nangibotide TFA

Cat.No: T78019

Synonym: LR12 TFA

Cat.No: T60537

Cat.No: T14205

Target: Others

APJ receptor agonist 4

Cat.No: T39587

Cat.No: T70639

Cat. No.	Product Name	Target	Signaling Pathways
T2925	Schisandrin B gamma-Schisandrin,Schizandrin B,五味子素B,五味子乙素,Schisandrin B (Sch B),Wuweizisu-B	ATM/ATR; Reactive Oxygen Species; Autophagy	Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; NF-κB; PI3K/Akt/mTOR signaling
	Schisandrin B (Schisandrin B (Sch B)) 是从五味子中分离联苯环辛二烯衍生物，对啮齿类动物的肝脏和心脏的抗氧化作用。
T5S0661	Koumine	Others	Others
	Koumine 是一种从钩吻中得到的生物碱，具有高效抗肿瘤活性，在肿瘤细胞中能够提高 Bax/Bcl-2 的蛋白比例和 caspase-3 的表达。在类风湿性关节炎动物模型中，它能够预防关节炎的发展。它具有抗焦虑、抗应激、抗银屑病作用，也可用于缓解疼痛的研究。
T4S0969	Obtusifolin 决明蒽醌,决明蒽醌；美决明子素	Antioxidant; NF-κB	NF-κB; oxidation-reduction
	Obtusifolin 是分离自决明子的种子中，能够抑制NF-kB 通路，调节气道上皮细胞中 MUC5AC 粘蛋白的基因表达和产生。它通过靶向甲状旁腺激素相关蛋白来抑制邻苯二甲酸酯诱导的乳腺癌骨转移。

天然产物

Cat.No: T2925

Synonym: gamma-Schisandrin,Schizandrin B,五味子素B,五味子乙素,Schisandrin B (Sch B),Wuweizisu-B

Target: ATM/ATR, Reactive Oxygen Species, Autophagy

Cat.No: T5S0661

Target: Others

Cat.No: T4S0969

Synonym: 决明蒽醌,决明蒽醌；美决明子素

Target: Antioxidant, NF-κB

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