transaminase

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。

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。

γ-Acetylenic GABA hydrochloride 是一种 GABA 转氨酶抑制剂。

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。

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。

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) 。

NNC 05-2090 hydrochloride 是一种 betaine GABA transporter (BGT-1) 抑制剂，IC50 值为 10.6 μM。NNC 05-2090 hydrochloride 可用于研究癫痫和神经疾病。

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。

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。

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。

E17241作为ABCA1基因表达的诱导剂，具有显著的生物活性（EC50 = 280 nM）。它同时也是一种过氧化物酶体增殖激活受体（PPARs）的激动剂，在HepG2细胞中能通过激活PPARγ、PPARα和PPARδ，促进PPAR介导的基因表达（EC50分别为290, 3,900, 和879 nM）。在RAW 264.7巨噬细胞中，E17241可以增强ABCA1蛋白的水平，这一作用在使用针对PKCζ mRNA的siRNA时失效。在用E17241处理的RAW 264.7细胞中，当浓度为0.4, 2, 或 10 µM时，可增加胆固醇的外流。此外，针对ApoE- -小鼠的动脉粥样硬化模型表明，每日25 mg kg的E17241剂量能有效降低血浆中的胆固醇、丙氨酸转氨酶（ALT）、天门冬氨酸转氨酶（AST）水平以及肝脏中的胆固醇和甘油三酯含量，且减少了主动脉的病变面积。此外，每日50 mg kg的E17241剂量可以在高脂高糖（HFHG）饮食下减轻KKAy糖尿病小鼠的血糖水平和体重。

3HKT-IN-1 (Compound 17122279) 是一种抑制 Anopheles gambiae 3-hydroxykynurenine transaminase (3HKT) 的化合物，适用于疟疾研究。

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.

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 transaminase (ALT), as well as serum and hepatic cholesterol and triglyceride, levels and reduces markers of NASH in the same model. |1. Bays, H.E., Schwartz, S., Littlejohn, T., 3rd, et al. MBX-8025, a novel peroxisome proliferator receptor-δ agonist: Lipid and other metabolic effects in dyslipidemic overweight patients treated with and without atorvastatin. J. Clin. Endocrinol. Metab. 96(9), 2889-2897 (2011).|2. Haczeyni, F., Wang, H., Barn, V., et al. The selective peroxisome proliferator-activated receptor-delta agonist seladelpar reverses nonalcoholic steatohepatitis pathology by abrogating lipotoxicity in diabetic obese mice. Hepatol. Commun. 1(7), 663-674 (2017).

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 steatosis and plasma alanine transaminase (ALT) and aspartate aminotransferase (AST) levels in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a methionine and choline-deficient diet at the same dose. 1.Li, Z., Chen, Y., Zhou, Z., et al.Discovery of first-in-class thiazole-based dual FFA1 PPARδ agonists as potential anti-diabetic agentsEur. J. Med. Chem.164352-365(2019) 2.Li, Z., Zhou, Z., Hu, L., et al.ZLY032, the first-in-class dual FFA1 PPARδ agonist, improves glucolipid metabolism and alleviates hepatic fibrosisPharmacol Res.159105035(2020)

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) reduces tumor growth in an SW1990 mouse xenograft model. |1. Zhang, P., Li, X.-M., Wang, J.-N., et al. New butenolide derivatives from the marine-derived fungus Paecilomyces variotii with DPPH radical scavenging activity. Phytochem. Lett. 11, 85-88 (2015).|2. Sun, W., Luan, S., Qi, C., et al. Aspulvinone O, a natural inhibitor of GOT1 suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism. Cell Commun. Signal. 17(1), 111 (2019).

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.) induces contralateral turns in a rat model of Parkinson's disease induced by 6-OHDA .4 1.Wu, M., Zhou, X.-J., Konno, R., et al.D-dopa is unidirectionally converted to L-dopa by D-amino acid oxidase, followed by dopa transaminaseClin. Exp. Pharmacol. Physiol.33(11)1042-1046(2006) 2.Ling, Z.-D., Pieri, S.C., and Carvey, P.M.Comparison of the neurotoxicity of dihydroxyphenylalanine stereoisomers in cultured dopamine neuronsClin. Neuropharmacol.19(4)360-365(1996) 3.Karoum, F., Freed, W.J., Chuang, L.-W., et al.D-dopa and L-dopa similarly elevate brain dopamine and produce turning behavior in ratsBrain Res.440(1)190-194(1988) 4.Moses, J., Siddiqui, A., and Silverman, P.B.Sodium benzoate differentially blocks circling induced by D-and L-dopa in the hemi-parkinsonian ratNeurosci. Lett.218(3)145-148(1996)

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.

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。

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。

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.

Schisantherin B (Schizantherin-B) 是一种天然产物。

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 oxaloacetate transaminase (GOT) levels and increases glutamate pyruvate transaminase (GPT) and lactate dehydrogenase (LDH) levels, markers of xenobiotic stress, in the plasma of carp (C. carpio) when administered in tank water at a concentration of 10 µg L. Clofibric acid has been found in wastewater effluent.

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。