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Cat. No. | Product Name | Target | Signaling Pathways |
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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。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T68259 |
TUPS
|
||
TUPS is a selective soluble epoxide hydrolase inhibitor which protects against isoprenaline-induced cardiac hypertrophy. | |||
T28005 |
MDL-100240
|
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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 | |||
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. | |||
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. | |||
T81231 |
S6 peptide
|
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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。 | |||
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。 | |||
T35876 |
Chlorthalidone Impurity G
|
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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。 | |||
T35855 |
AAA
|
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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... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 |