transaminase

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。

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。

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。

Glutamic-Oxalacetic Transaminase, Porcine (EC 2.6.1.1) 是一种依赖于吡哆醛磷酸 (PLP) 的转氨酶，催化天冬氨酸和谷氨酸之间 α-氨基的可逆转移，是氨基酸代谢中的关键酶。

Glutamic-Pyruvic Transaminase, Porcine (EC 2.6.1.2) 是一种转氨酶，催化丙氨酸循环中的两个步骤。

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) 。

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。

Guanosine 5'-O-(2-thiodiphosphate) (trisodium) (GDPβS (trisodium)) 是一种 GDP 的非水解衍生物。它作为腺苷酸环化酶 (AC) 的抑制剂，Ki 值为 600 nM。在啮齿动物模型的大脑皮层膜中，Guanosine 5'-O-(2-thiodiphosphate) (trisodium) 可在无谷丙转氨酶 (GPT) 的情况下部分激活 AC，EC50 值为 400 nM。此外，该化合物能阻止心室肌细胞释放由去甲肾上腺素诱导的一氧化氮。

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.

4-methyl-2-Oxovalerate sodium salt 是亮氨酸经转氨酶催化生成的产物，能够促进胰岛素分泌。4-methyl-2-Oxovalerate sodium salt 可被氧化分解为乙酰辅酶 A 与乙酰乙酸，也可通过与谷氨酸发生转氨反应重新生成亮氨酸，同时产生 α- 酮戊二酸。

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。