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33

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11991	Mefentrifluconazole	P450; Antifungal	Metabolism; Microbiology/Virology
	Mefentrifluconazole 是一种有效的、选择性的和具有口服活性的真菌 CYP51 (Kd= 0.5 nM) 抑制剂，但对人芳香酶的抑制活性较低，IC50值为0.92 μM。它是一种新型唑类衍生物，用作农用广谱抗真菌剂。
T1498	Indapamide Veroxil,Noranat,吲达帕胺,Tertensif	Potassium Channel	Membrane transporter/Ion channel
	Indapamide (Noranat) 是具有口服活性的磺酰胺利尿剂，通过降低血管反应性和外周血管阻力来降低血压。它也具有减轻左心室肥大的作用。
T5329	Trandolapril	Angiotensin-converting Enzyme (ACE)	Metabolism
	Trandolapril 是 Trandolaprilat 的前体药物。Trandolapril 是一种口服血管紧张素转换酶抑制剂，在高血压和充血性心力衰竭及心肌梗死领域有研究价值。
T0267	Zonisamide AD 810,唑尼沙胺,CI 912	Calcium Channel; Sodium Channel; Carbonic Anhydrase	Membrane transporter/Ion channel; Metabolism
	Zonisamide (AD 810) 是锌酶碳酸酐酶 (carbonic anhydrase) 的有效抑制剂，对人类线粒体同工酶 hCA II 和 hCA V 作用的 Ki 值分别为 35.2 nM 和 20.6 nM。Zonisamide 具有抗癫痫活性，在癫痫、癫痫发作和帕金森病的研究中具有价值。
T83965	Tamsolusin Hydrochloride YM 12617,LY-253352	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Tamsolusin Hydrochloride (YM 12617) 是一种高选择性α-1A肾上腺素受体拮抗剂，可用于治疗良性前列腺肥大。
T3597	Cutamesine dihydrochloride AGY94806 dihydrochloride,库他美新二盐酸盐,SA4503 (dihydrochloride),SA4503 dihydrochloride	Sigma receptor	GPCR/G Protein
	Cutamesine dihydrochloride (SA4503 dihydrochloride) 是一种选择性 σ1 受体激动剂，IC50值为 17.4 nM。
T9818	NGD-8243 NGD8243,N-[4-(trifluoromethyl)phenyl]-7-[3-(trifluoromethyl)pyridin-2-yl]quinazolin-4-amine	TRP/TRPV Channel	Membrane transporter/Ion channel
	NGD-8243 (N-[4-(trifluoromethyl)phenyl]-7-[3-(trifluoromethyl)pyridin-2-yl]quinazolin-4-amine) 是一种 TRPV1 抑制剂，可用于预防和治疗心脏肥大的研究。
T31640	Enrasentan SB-217242,SB 217242,SB217242	Endothelin Receptor	GPCR/G Protein
	Enrasentan（sb-217242）是一种 ET（A）和 ET（B）受体的混合拮抗剂，可降低血压、防止心肌肥大和保护心肌功能。
T35337L	Teduglutide acetate	Glucagon Receptor	GPCR/G Protein
	Teduglutide acetate 是一种 GLP-2 类似物，可使小肠黏膜肥大。它通过改变 claudin-10 的分布部分恢复小肠上皮功能，促进钠再循环以进行钠耦合葡萄糖转运和水吸收。
T60165	VB124	Monocarboxylate transporter	Membrane transporter/Ion channel
	VB124 是一种具有口服活性的、有效且选择性的MCT4抑制剂。VB124 可特异性抑制 MDA-MB-231 细胞中乳酸的涌入和流出，IC50分别为 8.6 nM 和 19 nM。VB124 对 MCT4 的选择性高于 MCT1。VB124可用于心脏肥大、心力衰竭和代谢的研究。
T24270	KS370G KS-370-G,KS 370 G,Caffeic Acid Phenethyl Amide
	KS370G (Caffeic Acid Phenethyl Amide) 抑制 UUO 诱导的肾纤维化标志物表达。KS370G 是一种具有口服活性的降糖和心血管保护剂，可减少梗阻肾脏中胶原蛋白的沉积，并显著降低肾脏炎症趋化因子/粘附分子和单核细胞标志物的表达，改善压力过载小鼠心脏左室肥厚和功能。KS370G 可用于研究肾阻塞性肾病。
T1050	Prazosin hydrochloride Prazosin hydrochloride,哌唑嗪盐酸盐,Prazosin HCl,cp-12299-1,Peripress,Vasoflex,盐酸哌唑嗪,Minipress	Potassium Channel; MRP; Adrenergic Receptor; ABC; Autophagy	Autophagy; GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience
	Prazosin hydrochloride (Vasoflex) 是一种选择性肾上腺素能 α-1 拮抗剂，可降低外周阻力并放松血管平滑肌。它可用于研究高血压和酒精使用障碍。它是一种合成哌嗪衍生物，具有降压抗肾上腺素能特性。它抑制有机阳离子转运蛋白 OCT-1 和 OCT-3，IC50分别为 1.8 和 13 μM 。
T11807	L002	Others; Histone Acetyltransferase; STAT	Chromatin/Epigenetic; JAK/STAT signaling; Others; Stem Cells
	L002 是一种细胞可渗透的，可逆特定性乙酰转移酶 p300(KAT3B)抑制剂，IC50为 1.98 μM。它结合乙酰辅酶 A 口袋并竞争性抑制 FATp300 催化结构域，阻断组蛋白乙酰化和 p53 乙酰化，且抑制 STAT3 激活，有用于高血压引起的心脏肥大和纤维化的研究潜力。
T77599	Methyl retinoate Retinoic acid, methyl ester	Others	Others
	Methyl retinoate (Retinoic acid, methyl ester) 在体内实验中会诱导给部位发生无菌炎症，会使血液中白细胞数量增加，而红细胞和Hb含量减少。Methyl retinoate 可促进自发性白血病的产生。Methyl retinoate 可用于治疗因维生素A缺乏而产生的胃肥大和溃疡。
T36008	Nebentan potassium
	Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan potassium inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan potassium inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB re...
T68259	TUPS
	TUPS is a selective soluble epoxide hydrolase inhibitor which protects against isoprenaline-induced cardiac hypertrophy.
TP1224	[Sar1, Ile8]-Angiotensin II TFA Angiotensin 2 TFA,AngiotensinII TFA
	[Sar1, Ile8]-Angiotensin II (TFA) is a peptide compound that exerts various effects on vascular smooth muscle. These effects include the contraction of normal arteries as well as the hypertrophy or hyperplasia of cultured cells or diseased vessels.
T24594	Paraprost
	Paraprost consists of 1-glutamic acid, alanine, and glycine. It was used in prostate hypertrophy drug therapy.
T68822	Tyrphostin AG17
	Tyrphostin AG17 is a biochemical that promotes adipocyte apoptosis in vivo and is an effective modulator of adipocyte differentiation and WAT hypertrophy in vitro and in vivo. It is thought to possibly be useful as a pharmacological obesity treatment. It is a tyrosine kinase antagonist that has also been found to inhibit tumor cell growth.
T38697	[Tyr(P)4] Angiotensin II
	[Tyr(P)4] Angiotensin II is a peptide that exerts a multitude of effects on vascular smooth muscle. These effects include the contraction of normal arteries, as well as the induction of hypertrophy or hyperplasia in cultured cells or diseased vessels.
T64266	KR-39038
	KR-39038 是一种口服具有活力的 GRK5 (G 蛋白偶联受体激酶 5) 抑制剂 (IC50: 0.02 μM)。KR-39038 能够抑制新生儿心肌细胞的 HDAC5 通路，明显抑制血管紧张素 II 诱导的细胞肥大，具有显著的抗心肌肥厚和改善心功能作用。KR-39038 能够用于进行心力衰竭的研究。
T3689L	Ruboxistaurin mesylate LY-333531,LY333531,LY 333531,LY-333531 Mesylate
	Ruboxistaurin is a PKC beta inhibitor. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/
T41232	GSK 2833503A
	GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.
T28005	MDL-100240
	MDL-100240 is a dual inhibitor of angiotensin-converting enzyme (ACE) and neprilysin with a balanced activity. MDL 100240 shows an impressive effectiveness both in preventing and in regressing hypertension-induced vascular remodeling and cardiac hypertrop
T81231	S6 peptide
	S6 peptide, 作为一种潜在重要的核纤维层蛋白激酶，参与了机械负荷诱发的心肌肥厚过程并可被多种生长因子所激活。
T69990	Ruboxistaurin mesylate monohydrate
	Ruboxistaurin mesylate monohydrate is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1/2 and Akt.
T70421	VCP746
	VCP-746 is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. VCP746 reduces hypertrophy in a rat neonatal cardiac myocyte model. VCP746 is a hybrid molecule consisting of an adenosine moiety linked to an adenosine A1 receptor (A1AR) allosteric modulator moiety. At the A1AR, VCP746 mediated cardioprotection in the absence of haemodynamic side effects such as bradycardia.
T60825	FC9402
	FC9402 是硫化物醌氧化还原酶 (SQOR) 的高效选择性抑制剂。FC9402 可调节心血管，减轻 TAC 诱导的心肌细胞肥大和左心室 (LV) 纤维化。
T71328	Theobromine-d6
	Theobromine-d6 is intended for use as an internal standard for the quantification of theobromine by GC- or LC-MS. Theobromine is a methylxanthine alkaloid and derivative of caffeine that has been found in cocoa beans and has diverse biological activities. It is an adenosine A1 receptor antagonist. Theobromine increases AMPK phosphorylation and inhibits adipocyte differentiation, ERK and JNK phosphorylation, and IL-6 and TNF-α production in 3T3-L1 preadipocytes cultured in differentiation medium....
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...
T37495	Angiotensin (1-7) (acetate)
	Angiotensin 1-7 (Ang-(1-7)) acetate 是RAS中的一种内源性七肽，具备心脏保护作用，主要表现为对心肌细胞的抗炎与抗纤维化活性。该化合物能抑制纯化的犬ACE活性（IC50=0.65 μM），通过降低ACE活性并促进一氧化氮释放，作为血管舒张调节的局部协同因子。此外，Angiotensin 1-7 acetate 可阻止血管紧张素Ⅱ诱发的平滑肌细胞增殖和肥大，同时对内皮细胞表现出抗血管生成和生长抑制作用。
T36007	Nebentan
	Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dep...
T35855	AAA
	AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension...

化合物

Mefentrifluconazole

Cat.No: T11991

Target: P450, Antifungal

Cat.No: T1498

Synonym: Veroxil,Noranat,吲达帕胺,Tertensif

Target: Potassium Channel

Cat.No: T5329

Target: Angiotensin-converting Enzyme (ACE)

Cat.No: T0267

Synonym: AD 810,唑尼沙胺,CI 912

Target: Calcium Channel, Sodium Channel, Carbonic Anhydrase

Tamsolusin Hydrochloride

Cat.No: T83965

Synonym: YM 12617,LY-253352

Target: Adrenergic Receptor

Cutamesine dihydrochloride

Cat.No: T3597

Synonym: AGY94806 dihydrochloride,库他美新二盐酸盐,SA4503 (dihydrochloride),SA4503 dihydrochloride

Target: Sigma receptor

Cat.No: T9818

Synonym: NGD8243,N-[4-(trifluoromethyl)phenyl]-7-[3-(trifluoromethyl)pyridin-2-yl]quinazolin-4-amine

Target: TRP/TRPV Channel

Cat.No: T31640

Synonym: SB-217242,SB 217242,SB217242

Target: Endothelin Receptor

Teduglutide acetate

Cat.No: T35337L

Target: Glucagon Receptor

Cat.No: T60165

Target: Monocarboxylate transporter

Cat.No: T24270

Synonym: KS-370-G,KS 370 G,Caffeic Acid Phenethyl Amide

Prazosin hydrochloride

Cat.No: T1050

Synonym: Prazosin hydrochloride,哌唑嗪盐酸盐,Prazosin HCl,cp-12299-1,Peripress,Vasoflex,盐酸哌唑嗪,Minipress

Target: Potassium Channel, MRP, Adrenergic Receptor, ABC, Autophagy

Cat.No: T11807

Target: Others, Histone Acetyltransferase, STAT

Methyl retinoate

Cat.No: T77599

Synonym: Retinoic acid, methyl ester

Target: Others

Nebentan potassium

Cat.No: T36008

Cat.No: T68259

[Sar1, Ile8]-Angiotensin II TFA

Cat.No: TP1224

Synonym: Angiotensin 2 TFA,AngiotensinII TFA

Cat.No: T24594

Tyrphostin AG17

Cat.No: T68822

[Tyr(P)4] Angiotensin II

Cat.No: T38697

Cat.No: T64266

Ruboxistaurin mesylate

Cat.No: T3689L

Synonym: LY-333531,LY333531,LY 333531,LY-333531 Mesylate

Cat.No: T41232

Cat.No: T28005

Cat.No: T81231

Ruboxistaurin mesylate monohydrate

Cat.No: T69990

Cat.No: T70421

Cat.No: T60825

Cat.No: T71328

Chlorthalidone Impurity G

Cat.No: T35876

Angiotensin (1-7) (acetate)

Cat.No: T37495

Cat.No: T36007

Cat.No: T35855

Cat. No.	Product Name	Target	Signaling Pathways
TN6490	Regaloside C	Others	Others
	Regaloside C 是一种从百合属的中分离出来的甘油葡糖苷，具有抗炎作用。
TN1039	Tamarixetin 柽柳黄素,4'-O-Methyl Quercetin	Endogenous Metabolite; Immunology/Inflammation related	Immunology/Inflammation; Metabolism
	Tamarixetin (4'-O-Methyl Quercetin) 是一种槲皮素的天然类黄酮衍生物，具有抗氧化、抗炎作用，能够防止心肌肥厚。
T3408	Syringin Lilacin,Syringoside,eleutheroside-b,Methoxyconiferine,紫丁香苷	NOS; Autophagy	Autophagy; Immunology/Inflammation
	Syringin (eleutheroside-b) 是欧丁香中的一种苯丙素类天然产物，通过抑制自噬来防止压力超载引起的心肌肥厚，具有抗肿瘤、抗增殖、抗骨质疏松、免疫调节和血小板聚集抑制作用。
T19687	Phenylethyl isothiocyanate JC 5411,2-苯基乙基异硫代氰酸酯,JC5411,JC-5411	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Phenylethyl isothiocyanate (JC5411) 是一种 HDAC 抑制剂。它有可能用于治疗良性前列腺肥大。
T2803	Monocrotaline 野百合碱,Crotaline	TGF-beta/Smad	Stem Cells
	Monocrotaline (Crotaline) 是一种吡咯里西啶生物碱，从猪屎豆植物的种子中提取得到，可诱导啮齿动物产生肺动脉高血压。
T6S1418	Praeruptorin C	Antioxidant; Calcium Channel	Membrane transporter/Ion channel; Metabolism; oxidation-reduction
	Praeruptorin C 是白花前胡中的一种主要成分，是钙拮抗剂，pD2′值为 5.7。
T6S1740	Nardosinone 苷松新酮,甘松新酮	Others	Others
	Nardosinone 是一个 dbcAMP 和 staurosporine 的神经生成作用增强剂，分离自Nardostachys chinensis 中。Nardosinone 可能成为一种有用的药理学工具，不仅可用于研究神经生长因子 (NGF) 的作用机理，而且可用于研究神经毒性物质的作用机理。
T12576	Pterosin B	Others	Others
	Pterosin B is an salt-inducible kinase 3 (Sik3) signaling inhibitor. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis by inhibiting Sik3.
TN4164	Grandifloroside	TNF	Apoptosis
	Grandifloroside shows good antioxidative and potent anti-inflammatory activities, it also exhibits potent inhibitory activity against TNF-α and 5α-reductase, suggests that it might be developed as a source of potent anti-oxidative and anti-inflammatory ag

天然产物

Cat.No: TN6490

Target: Others

Cat.No: TN1039

Synonym: 柽柳黄素,4'-O-Methyl Quercetin

Target: Endogenous Metabolite, Immunology/Inflammation related

Cat.No: T3408

Synonym: Lilacin,Syringoside,eleutheroside-b,Methoxyconiferine,紫丁香苷

Target: NOS, Autophagy

Phenylethyl isothiocyanate

Cat.No: T19687

Synonym: JC 5411,2-苯基乙基异硫代氰酸酯,JC5411,JC-5411

Target: HDAC

Cat.No: T2803

Synonym: 野百合碱,Crotaline

Target: TGF-beta/Smad

Cat.No: T6S1418

Target: Antioxidant, Calcium Channel

Cat.No: T6S1740

Synonym: 苷松新酮,甘松新酮

Target: Others

Cat.No: T12576

Target: Others

Grandifloroside

Cat.No: TN4164

Target: TNF

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