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21

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8765	iGOT1-01	Others	Others
	iGOT1-01 是一种天冬氨酸转氨酶 1 (谷氨酸草酰乙酸转氨酶 1；GOT1) 抑制剂，在 GOT1/GLOX/HRP 测定中IC50为 11.3 μM，在 MDH 偶联 GOT1 酶法测定中IC50为 85 μM。它显示出抗癌活性。
T8766	GOT1 inhibitor-1 GOT1 inhibitor 2c	Others	Others
	GOT1 inhibitor-1 (GOT1 inhibitor 2c) 是一种新型的、非共价的谷氨酸草酰乙酸转氨酶 1 (GOT1) 抑制剂(IC50:8.2 uM)，是一种戊酸衍生物。它可用于以及胰腺导管腺癌 (PDAC) 。
T0128L	Vigabatrin Hydrochloride 盐酸氨己烯酸,γ-Vinyl-GABA hydrochloride	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Vigabatrin Hydrochloride (γ-Vinyl-GABA hydrochloride) 是抑制性神经递质 GABA 乙烯基衍生物，不可逆地抑制 GABA 转氨酶对 GABA 的分解代谢，增加脑中 GABA 的水平。
T40659L	γ-Acetylenic GABA hydrochloride γ-Acetylenic GABA hydrochloride(57659-38-8 Free base)	Transaminase; GABA Receptor	Membrane transporter/Ion channel; Metabolism; Neuroscience
	γ-Acetylenic GABA hydrochloride 是一种 GABA 转氨酶抑制剂。
T67927	BAY-069	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	BAY-069 是一种抑制剂。BAY-069对支链氨基酸转氨酶 1 (BCAT1）具有抑制作用（IC50：31 nM ，对支链氨基酸转氨酶 2 （BCAT2) 具有抑制作用（IC50 ：153 nM）。BAY-069 是一种新型(三氟甲基)嘧啶二酮类化学探针，可用于抗癌研究。
T77795	L-DABA hydrobromide L-2,4-Diaminobutyric acid hydrobromide	Others; Endogenous Metabolite	Metabolism; Others
	L-DABA hydrobromide (L-2,4-Diaminobutyric acid hydrobromide) 是一种有效的 GABA 转氨酶抑制剂，具有抗肿瘤和抗惊厥活性，可用于研究神经系统疾病。
T0128	Vigabatrin Sabril,Vigabatrine,氨己烯酸	GABA Receptor; ABC	Membrane transporter/Ion channel; Neuroscience
	Vigabatrin (Sabril) 是 γ-氨基丁酸的类似物，是 4-氨基丁酸转氨酶的不可逆抑制剂，负责 γ-氨基丁酸分解代谢。它可用于可卡因依赖的治疗。
T6474	Divalproex Sodium Valproate semisodium,Epival,双丙戊酸钠	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Divalproex Sodium (Valproate semisodium) 结合并抑制 γ-氨基丁酸 (GABA) 转氨酶，其抗惊厥活性可通过增加 GABA 脑浓度和抑制分解 GABA 或阻止 GABA 再摄取到神经胶质和神经末梢的酶来发挥。它也是一种 HDAC 抑制剂。由丙戊酸钠和丙戊酸组成，具有抗惊厥和抗癫痫活性。 Divalproex 还可以通过抑制电压敏感的钠通道来抑制重复的神经元放电。
T7622L	Gabazine free base Chebi:34968,SR95531,C13796,J331.170H,SR 95531
	Gabazine free base is a specific antagonist of the GABA receptor. It does not affect GABA-transaminase or glutamate-decarboxylase activities.
T24080	Gabaculine HCl 708-B,Gabaculine hydrochlorlide
	Gabaculine is an irreversible inhibitor of GABA transaminase (GABA-T; Ki: 2.9 μM). Gabaculine alters plastid development and differentially affects the abundance of plastid-encoded DPOR and nuclear-encoded GluTR.
T76364	Ac-Leu-Leu-Norleucinol
	Ac-Leu-Leu-Norleucinol 是钙蛋白酶抑制剂，可用于研究对 Acetaminophen 引起的急性肝损伤，并能够降低诱导引发的谷草转氨酶 (ALT) 和谷丙转氨酶 (AST) 水平。
T71305	Clofibric Acid-d4
	Clofibric acid-d4 is intended for use as an internal standard for the quantification of clofibric acid by GC- or LC-MS. Clofibric acid is a peroxisome proliferator-activated receptor α (PPARα) agonist (EC50 = 50 µM in a transactivation assay) and the active metabolite of clofibrate. It is formed from clofibrate by tissue and serum esterases. Dietary administration of clofibric acid (0.067-0.22%) reduces serum cholesterol, phospholipid, and triglyceride levels in rats. It decreases glutamate oxal...
T40659	γ-Acetylenic GABA 4-Aminohex-5-ynoic acid,γ-Acetylenic GABA
	γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is a potent, irreversible inhibitor of GABA-transaminase. This compound effectively raises the concentration of γ-Aminobutyric acid (GABA) in the brain of rats.
T76178	Aspartate aminotransferase
	Aspartate aminotransferase (AST) 是一种转氨酶，常用于生化研究。Aspartate aminotransferase 催化天冬氨酸和 α-酮戊二酸转化为草酰乙酸和谷氨酸。Aspartate aminotransferase 可存在于在脑脊液、渗出液和渗出物。
T69068	Aspulvinone H
	Aspulvinone H is a natural inhibitor of glutamic oxaloacetate transaminase 1 (GOT1), suppressing glutamine metabolism, making PDAC cells sensitive to oxidative stress and inhibiting cell proliferation, exhibiting potent in vivo antitumor activity in an SW1990-cell-induced xenograft model.
T62185	GABA-AT-IN-1
	GABA-AT-IN-1 (Compound 6) 是一种能够透过血脑屏障的 γ-氨基丁酸转氨酶（GABA-AT）抑制剂。GABA-AT-IN-1 可以明显增加小鼠大脑 GABA 水平，能够用作抗惊厥药物。
T37605	D-DOPA
	D-DOPA is an enantiomer of the dopamine precursor L-DOPA . It can be converted to L-DOPAviasequential oxidation and transamination, which are mediated by D-amino acid oxidase (DAAO) and DOPA transaminase, respectively, in rat kidney homogenates.1It reduces the number of dopaminergic neurons in primary rat embryonic mesencephalic cultures in a concentration-dependent manner.2Intraventricular administration of D-DOPA (200 μg/animal) increases striatal dopamine levels in rats.3D-DOPA (20 mg/kg, i.p...
T35799	MBX-8025 (sodium salt)
	MBX-8025 is an agonist of peroxisome proliferator-activated receptor δ (PPARδ).1 It is greater than 750- and 2,500-fold selective for PPARδ over PPARα and PPARγ. MBX-8025 (10 mg/kg per day for eight weeks) reduces increases in fasting blood glucose and serum insulin levels, and decreases insulin resistance in Alms1 mutant (foz/foz) mice fed an atherogenic diet as a model of diet-induced obesity, type 2 diabetes, and non-alcoholic steatohepatitis (NASH).2 It also decreases serum alanine transamin...
T78059	Glucagon (Human) Hyperglycemic-glycogenolytic factor,Glukagon	Others	Others
	Glucagon 对蛋白质和氨基酸的代谢产生显著的调节作用。它抑制了氨基酸与肝脏、肌肉以及胰腺蛋白的结合，增加氮的排出，并促进肝脏内尿素的合成。同时，Glucagon 增加了肝脏中转氨酶和尿素循环酶的浓度，提高了肝脏对氨基酸的摄取，并加强了氨基酸与肝糖原之间的结合，从而降低了血液中的氨基酸浓度。
T35816	ZLY032
	ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1/GPR40; EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor δ (PPARδ; EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARδ over PPARα and PPARγ (EC50s = >10 μM for both). ZLY032 (40 mg/kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob/obmouse model of metabolic disease.2It reduces hepatic st...
T83735	Pap12-6 TFA
	Pap12-6是一种从蝶类P. xuthus幼虫中发现的papiliocin十二个N-端氨基酸衍生的抗菌肽。它对包括E. coli、P. aeruginosa和S. syphimurium在内的八种革兰氏阴性细菌（MIC50s = 4-8 µM）以及革兰氏阳性细菌S. aureus、耐甲氧西林的S. aureus 3126（MRSA-3126）、B. subtilis和S. epidermidis（MIC50s = 4-8 µM）具有活性，但在25 µM浓度下不影响人类红细胞、小鼠RAW 264.7巨噬细胞、人类HaCaT角质形成细胞或人类HEK293肾细胞的活性。Pap12-6在4和8 µM浓度下可引起E. coli的膜去极化。Pap12-6（10 µM）预处理可降低LPS刺激的RAW 264.7巨噬细胞中一氧化氮（NO2-）、Tnf-α和Il-6的分泌水平。在体内，Pap12-6（10 mg/kg）可以提高感染E. coli的小鼠的存活率，并且在剂量为1 mg/kg时减少感染E. coli小鼠的肺、肝和肾中菌落形成单位（CFUs）的数量。Pap12-6（1 mg/kg）在E. co...

化合物

Cat.No: T8765

Target: Others

GOT1 inhibitor-1

Cat.No: T8766

Synonym: GOT1 inhibitor 2c

Target: Others

Vigabatrin Hydrochloride

Cat.No: T0128L

Synonym: 盐酸氨己烯酸,γ-Vinyl-GABA hydrochloride

Target: GABA Receptor

γ-Acetylenic GABA hydrochloride

Cat.No: T40659L

Synonym: γ-Acetylenic GABA hydrochloride(57659-38-8 Free base)

Target: Transaminase, GABA Receptor

Cat.No: T67927

Target: Reactive Oxygen Species

L-DABA hydrobromide

Cat.No: T77795

Synonym: L-2,4-Diaminobutyric acid hydrobromide

Target: Others, Endogenous Metabolite

Cat.No: T0128

Synonym: Sabril,Vigabatrine,氨己烯酸

Target: GABA Receptor, ABC

Divalproex Sodium

Cat.No: T6474

Synonym: Valproate semisodium,Epival,双丙戊酸钠

Target: HDAC

Gabazine free base

Cat.No: T7622L

Synonym: Chebi:34968,SR95531,C13796,J331.170H,SR 95531

Cat.No: T24080

Synonym: 708-B,Gabaculine hydrochlorlide

Ac-Leu-Leu-Norleucinol

Cat.No: T76364

Clofibric Acid-d4

Cat.No: T71305

γ-Acetylenic GABA

Cat.No: T40659

Synonym: 4-Aminohex-5-ynoic acid,γ-Acetylenic GABA

Aspartate aminotransferase

Cat.No: T76178

Cat.No: T69068

Cat.No: T62185

Cat.No: T37605

MBX-8025 (sodium salt)

Cat.No: T35799

Glucagon (Human)

Cat.No: T78059

Synonym: Hyperglycemic-glycogenolytic factor,Glukagon

Target: Others

Cat.No: T35816

Cat.No: T83735

Cat. No.	Product Name	Target	Signaling Pathways
T3273	Bifendate 联苯双酯,Bifendatatum	HBV; Reverse Transcriptase	Microbiology/Virology
	Bifendate (Bifendatatum) 是 Schisandrin C 的合成中间体，在慢性 B 型肝炎的研究中具有抗HBV 功效，用于治疗病毒性肝炎和药物性肝损伤引起的转氨酶升高。
T7595	L-DABA L-2,4-Diaminobutyric acid,L-2,4-二氨基丁酸氢溴酸盐,L-DAB HBR	GABA Receptor; Endogenous Metabolite	Membrane transporter/Ion channel; Metabolism; Neuroscience
	L-DABA (L-2,4-Diaminobutyric acid) 是GABA 转氨酶的弱抑制剂，IC50值大于500 μM，具有抗肿瘤活性。
T6S1918	Schisantherin B Gomisin-B,Wuweizi ester-B,五味子酯乙,Schizantherin-B	Beta Amyloid; Others	Neuroscience; Others
	Schisantherin B (Schizantherin-B) 是一种天然产物。
T2S1814	p-Hydroxybenzaldehyde 4-Formylphenol,4-羟基苯甲醛;对羟基苯甲醛,4-hydroxybenzaldehyde,对羟基苯甲醛,p-Oxybenzaldehyde	Transaminase; GABA Receptor; Endogenous Metabolite	Membrane transporter/Ion channel; Metabolism; Neuroscience
	p-Hydroxybenzaldehyde (p-Oxybenzaldehyde) 是从天麻中提取的一种天然产物，对 GABA 转氨酶有抑制作用，有助于抗癫痫和抗惊厥活性。
TN2185	Schisantherin C	Others	Others
	Schisantherin A, B, C, and D show good effect in lowering the serum glutamic-pyruvic transaminase level of the patients suffering from chronic virus hepatitis.
T82365	Fulvotomentoside B
	Fulvotomentoside B, 一种可从黄毛乳杆菌中分离的皂苷，对于CCl4、d-gal 和对乙酰氨基酚所致中毒小鼠具有显著的保护作用。在减低血清SGPT和GT水平以及减轻肝脏病理损伤方面表现出突出的效果。
TN2181	Sarmentosin	Others	Others
	Sarmentosin significantly lowers the SGPT level of patients suffering from chronic viral hepatitis, and shows a suppressive effect on cell-mediated immune responses in mice. It shows a good effect in lowering serum glutamate-pyruvate transaminase.
T36179	Aspulvinone O
	Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) redu...

天然产物

Cat.No: T3273

Synonym: 联苯双酯,Bifendatatum

Target: HBV, Reverse Transcriptase

Cat.No: T7595

Synonym: L-2,4-Diaminobutyric acid,L-2,4-二氨基丁酸氢溴酸盐,L-DAB HBR

Target: GABA Receptor, Endogenous Metabolite

Schisantherin B

Cat.No: T6S1918

Synonym: Gomisin-B,Wuweizi ester-B,五味子酯乙,Schizantherin-B

Target: Beta Amyloid, Others

p-Hydroxybenzaldehyde

Cat.No: T2S1814

Synonym: 4-Formylphenol,4-羟基苯甲醛;对羟基苯甲醛,4-hydroxybenzaldehyde,对羟基苯甲醛,p-Oxybenzaldehyde

Target: Transaminase, GABA Receptor, Endogenous Metabolite

Schisantherin C

Cat.No: TN2185

Target: Others

Fulvotomentoside B

Cat.No: T82365

Cat.No: TN2181

Target: Others

Cat.No: T36179

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