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28

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2010	S0859	Others	Others
	S0859 是一种 N-氰基磺酰胺，是选择性高亲和力的 Na+/HCO3-共转运体抑制剂，可逆性地抑制 NBC 介导的细胞内 pH (pHi) 恢复，Ki 为1.7 μM。
T38843	Enavogliflozin DWP-16001	SGLT	GPCR/G Protein
	Enavogliflozin (DWP-16001) 是一种口服有效的，选择性的钠-葡萄糖协同转运体 -2 抑制剂，具有抗糖尿病的功效。
TQ0011	PF-06869206	Sodium Channel	Membrane transporter/Ion channel
	PF-06869206 是口服有效的磷酸钠协同转运蛋白NaPi2a(SLC34A1) 选择性抑制剂，IC50为 380 nM。
T17243	VU0463271 N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide	Potassium Channel	Membrane transporter/Ion channel
	VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) 是一种有效的、特异性的 KCC2 拮抗剂，其 IC50 为 61 nM，特异性是密切相关的 Na-K-2Cl 协同转运蛋白 1 (NKCC1) 的 100 倍以上，在更大的 GPCR、离子通道和转运蛋白面板中没有活性。
T4999	Ertugliflozin 埃格列净,MK-8835,PF-04971729	SGLT	GPCR/G Protein
	Ertugliflozin (PF-04971729) 是选择性的、口服有效的钠离子依赖的葡萄糖协同转运蛋白2 (SGLT2) 抑制剂，对h-SGLT2 的IC50值为 0.877 nM。Ertugliflozin 在2型糖尿病中有研究价值。
TQ0139	VU 0240551 N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide,VU0240551-2-D4	Potassium Channel; Calcium Channel; HER	Angiogenesis; JAK/STAT signaling; Membrane transporter/Ion channel; Metabolism; Tyrosine Kinase/Adaptors
	VU 0240551 是神经元 K-Cl 协同转运蛋白 KCC2 抑制剂的特异性拮抗剂，IC50 为 560 nM。 VU 0240551 抑制 L 型钙通道和 hERG。
T5444	CLP290 CLP-290	Potassium Channel	Membrane transporter/Ion channel
	CLP-290 是一种神经特异性 K+-Cl−共转运体 KCC2的口服激活剂，在多种神经和精神疾病方面具有研究潜力。CLP290 能显著降低 STZ 大鼠的血液中 AVP 和血糖水平。
T14984	CLP257	Potassium Channel	Membrane transporter/Ion channel
	CLP257 是有效的 K+-Cl- 协同转运蛋白 KCC2 选择性激活剂 (EC50: 616 nM)。它可减轻神经性疼痛大鼠的超敏反应，并在翻译后调节质膜 KCC2 蛋白周转。它在 KCC2 活性降低的神经元中恢复受损的 Cl- 转运。
T4564	Ethacrynic acid Edecrin,利尿酸,Etacrynic Acid,Hydromedin	Others; Calcium Channel; NF-κB; GST	Membrane transporter/Ion channel; Metabolism; NF-κB; Others; oxidation-reduction
	Ethacrynic acid (Edecrin) 是谷胱甘肽 S-转移酶抑制剂，也是NF-κB 信号传导途径的有效抑制剂，并且还调节白三烯的形成。它还可抑制 L 型电压依赖性和储存操作的钙通道，从而导致气道平滑肌细胞松弛。它是利尿剂，具有抗炎特性，可减轻类维生素 A 诱导的小鼠耳部水肿。
T35336	Furosemide sodium Frusemide Sodium,Lasix	Na-K-Cl cotransporter	Membrane transporter/Ion channel
	Furosemide sodium (Frusemide Sodium) 是 Na+/K+/2Cl- (NKCC)，NKCC1 和 NKCC2 共转运蛋白的有效的和具有口服活性抑制剂。Furosemide sodium 也是 GABAA 受体拮抗剂，对含 α6 受体的选择性是含 α1 受体的 100 倍。Furosemide sodium 用作利尿试剂，用于充血性心力衰竭，高血压和水肿的研究。
T21399	Luseogliflozin TS71,TS-071,TS 71,TS071,TS-71,TS 071
	Luseogliflozin, a potent and competitive inhibitor of sodium-dependent glucose cotransporter 2 (SGLT2), competitively inhibits human SGLT2-mediated glucose uptake with a Ki value of 1.10 nM.
T16818	S-8921	Others	Others
	S-8921 is an inhibitor of ileal Na+/bile acid cotransporter.
T17221	Velagliflozin	SGLT	GPCR/G Protein
	Velagliflozin is an orally available inhibitor of sodium-glucose cotransporter 2.
T13179	Tofogliflozin CSG452	Others	Others
	Tofogliflozin is a highly specific inhibitor of sodium/glucose cotransporter 2 (SGLT2) (Kis: 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2. IC50s: 2.9/14.9/6.4 nM (human/rat/mouse SGLT2)).
T11528	H100	Others	Others
	H100 is a Cl- transport inhibitor, no effect against KCl cotransporter. It has partial effects against both the NaK2Cl cotransporter and the Band 3 anion exchanger.
T30534	BMS-639432
	BMS-639432 is a potent sodium-glucose cotransporter type II (SGLT2) inhibitor.
T15752	Licogliflozin LIK066	SGLT	GPCR/G Protein
	Licogliflozin (LIK066) 是钠-葡萄糖协同转运蛋白 (SGLT1和SGLT2) 的有效抑制剂。
T28971	Tianagliflozin
	Tianagliflozin, a sodium/glucose cotransporter 2 (SGLT-2) inhibitor, is used potentially for the treatment of type 2 diabetes.
T61713	Bumetanide sodium
	Bumetanide sodium is a potent loop diuretic that acts as a blocker for the sodium-potassium-chloride cotransporter (NKCC). It selectively inhibits NKCC1 and NKCC2, with IC50 values of 0.68 μM and 4.0 μM for hNKCC1A and hNKCC2A, respectively [1] [2].
T12892	SGL5213	SGLT	GPCR/G Protein
	SGL5213 is an oral active and low-absorbable inhibitor of sodium-dependent glucose cotransporter 1 (SGLT1)(hSGLT1 and hSGLT2 with IC50 values of 29 nM and 20 nM , respectively),and has potential to treat type 2 diabetes.
T68236	TP0438836
	TP0438836 is a potent, low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor for the treatment of type 2 diabetes. TP0438836 showed IC50 values 28nM and 7 nM for hSGLT1 and hSGLT2 resepctively.
T15797	LX2761	Others	Others
	LX2761 is a chemically stable and effective inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 (IC50s: 2.2 nM and 2.7nM for hSGLT1 and hSGLT2). However, it shows specific SGLT1 inhibition in the gastrointestinal (GI) tract.
T35728	Hydrochlorothiazide Impurity C
	Hydrochlorothiazide impurity C is a potential impurity found in commercial hydrochlorothiazide preparations. [1] Hydrochlorothiazide is a thiazide diuretic that inhibits the apical membrane sodium chloride cotransporter in the distal and collecting duct nephron segments.[2][3][4]
T35619	Dapagliflozin-3-O-β-D-Glucuronide
	Dapagliflozin-3-O-β-D-glucuronide is a metabolite of dapagliflozin . Dapagliflozin is a first generation selective sodium glucose cotransporter (SGLT) 2 inhibitor that blocks glucose transport.[1] Dapagliflozin is metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A9 to dapagliflozin-3-O-β-D-glucuronide, which is 2,600-fold less potent than the parent compound with regard to SGLT2 inhibition.[2]
T68922	YM543 free base
	YM543 free base 为口服有效的钠-葡萄糖协同转运蛋白(SGLT) 2抑制剂，主要用于降低血糖水平，适用于糖尿病研究。
T72143	Velagliflozin proline hydrate
	Velagliflozin proline hydrate 是 Velagliflozin 的临床形式。Velagliflozin 是一种可口服的钠-葡萄糖协同转运蛋白 2 (SGLT2) 抑制剂，具有抗糖尿病的活性。特别是，Velagliflozin 减少肾葡萄糖重吸收，促进葡萄糖尿，从而降低血糖和胰岛素浓度。
T70390	YM-543 choline
	YM-543, also known as ASP-543, is a selective SGLT2 inhibitor. Sodium-glucose cotransporter 2 (SGLT2) is a specifically expressed transporter in the kidney that plays an important role in renal glucose reabsorption, and its inhibition may present a novel therapeutic strategy for treating diabetes. YM543 potently and selectively inhibited mouse and human SGLT2 activities at nanomolar ranges. In vivo single oral administration of YM543 dose-dependently and significantly reduced blood glucose level...
T35876	Chlorthalidone Impurity G
	Chlorthalidone impurity G is a potential impurity found in commercial preparations of chlorthalidone that has moderate antihypertensive effects. Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including the isoforms CAVB, VII, IX, XII, and XIII (Kis = 2.8-23 nM) an...

化合物

Cat.No: T2010

Target: Others

Cat.No: T38843

Synonym: DWP-16001

Target: SGLT

Cat.No: TQ0011

Target: Sodium Channel

Cat.No: T17243

Synonym: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide

Target: Potassium Channel

Cat.No: T4999

Synonym: 埃格列净,MK-8835,PF-04971729

Target: SGLT

Cat.No: TQ0139

Synonym: N-(4-Methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide,VU0240551-2-D4

Target: Potassium Channel, Calcium Channel, HER

Cat.No: T5444

Synonym: CLP-290

Target: Potassium Channel

Cat.No: T14984

Target: Potassium Channel

Ethacrynic acid

Cat.No: T4564

Synonym: Edecrin,利尿酸,Etacrynic Acid,Hydromedin

Target: Others, Calcium Channel, NF-κB, GST

Furosemide sodium

Cat.No: T35336

Synonym: Frusemide Sodium,Lasix

Target: Na-K-Cl cotransporter

Cat.No: T21399

Synonym: TS71,TS-071,TS 71,TS071,TS-71,TS 071

Cat.No: T16818

Target: Others

Cat.No: T17221

Target: SGLT

Cat.No: T13179

Synonym: CSG452

Target: Others

Cat.No: T11528

Target: Others

Cat.No: T30534

Cat.No: T15752

Synonym: LIK066

Target: SGLT

Cat.No: T28971

Bumetanide sodium

Cat.No: T61713

Cat.No: T12892

Target: SGLT

Cat.No: T68236

Cat.No: T15797

Target: Others

Hydrochlorothiazide Impurity C

Cat.No: T35728

Dapagliflozin-3-O-β-D-Glucuronide

Cat.No: T35619

YM543 free base

Cat.No: T68922

Velagliflozin proline hydrate

Cat.No: T72143

Cat.No: T70390

Chlorthalidone Impurity G

Cat.No: T35876

Cat. No.	Product Name	Target	Signaling Pathways
TN1847	Kushenol X 苦参醇X	Others	Others
	Kushenol X exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).
TN1841	Kushenol A 苦参新醇 A,Leachianone E	cAMP	GPCR/G Protein
	Kushenol A is a kind of Adenosine 3', 5'-cyclic monophosphate(cAMP)phosphodiesterase inhibitiors, it shows selective alpha-glucosidase inhibitory activity. Kushenol A and kushenol C exhibit inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).
TN1842	Kushenol I	GABA Receptor; Antifection	Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
	Kushenol I is a GABAA receptor modulator, it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).Kushenol I is shown to be active against the plant pathogenic fungus Cladosporium cucumerinum.
TN4399	Kushenol C	SGLT; NF-κB; ROS; BACE; Antifection	GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience; NF-κB
	Kushenol C is a good 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenger, and it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2). Kushenol C shows antimicrobial activity against Staphylococcus aureus and Streptococcus mutan
TN2553	1-Methyl-2-undecyl-4(1H)-quinolone 1-Methyl-2-undecylquinolin-4(1H)-one	MAO	Metabolism; Neuroscience
	1-Methyl-2-undecyl-4(1H)-quinolone, and dihydroevocarpine should also be served as the chemical markers together with evodiamine for the quality control of Evodia rutaecarpa (Juss.) Benth. 1-Methyl-2-undecyl-4(1H)-quinolone shows a selective inhibition of type B MAO (MAO-B) activity with the IC(50) value of 15.3 microM using a substrate kynuramine, but does not inhibit type A MAO (MAO-A) activity.It can mitigate high phosphate-induced human aortic valve interstitial cells (HAVICs) calcification ...

天然产物

Cat.No: TN1847

Synonym: 苦参醇X

Target: Others

Cat.No: TN1841

Synonym: 苦参新醇 A,Leachianone E

Target: cAMP

Cat.No: TN1842

Target: GABA Receptor, Antifection

Cat.No: TN4399

Target: SGLT, NF-κB, ROS, BACE, Antifection

1-Methyl-2-undecyl-4(1H)-quinolone

Cat.No: TN2553

Synonym: 1-Methyl-2-undecylquinolin-4(1H)-one

Target: MAO

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