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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7693 |
Thiorphan
|
Neprilysin | Metabolism |
Thiorphan 是选择性neprilysin 抑制剂 (IC50:6.9 nM) 。 | |||
T1176 |
Racecadotril
Acetorphan,消旋卡多曲 |
Neprilysin; Proteasome | Metabolism; Proteases/Proteasome; Ubiquitination |
Racecadotril (Acetorphan) 是一种中性内肽酶 (NEP) 抑制剂,具有止泻作用。Racecadotril 及其活性代谢物 Thiorphan 抑制小鼠脑中纯化的NEP 活性,Ki 分别为 4500 和 6.1 nM。 | |||
T2318 |
Sacubitril/Valsartan
Sacubitril mixture with Valsartan,沙库必曲/缬沙坦,Valsartan,Sacubitril,LCZ696 |
Apoptosis; RAAS; Neprilysin | Apoptosis; Endocrinology/Hormones; Metabolism |
Sacubitril/Valsartan (LCZ696),以1:1摩尔比由Valsartan(一种ARB)和Sacubitril(AHU377)组成,为创新口服血管紧张素受体-脑啡肽酶(ARN)双重抑制剂,旨在治疗高血压与心力衰竭。其作用机制包括抑制炎症、氧化应激及细胞凋亡,有助于改善糖尿病心肌病。 | |||
TQ0106 |
Sacubitrilat
LBQ-657 |
Neprilysin | Metabolism |
Sacubitrilat (LBQ-657) 是活性的脑啡肽酶 (NEP) 抑制剂。 | |||
T4574 |
Sacubitril
AHU 377,AHU377,沙库必曲,AHU-377 |
Neprilysin | Metabolism |
Sacubitril (AHU-377) 是一种有效的NEP 抑制剂,IC50=5 nM。它是研究心力衰竭药物 LCZ696 的组分之一。 | |||
T4200 |
Sacubitril hemicalcium salt
AHU-377 (hemicalcium salt),LCZ696中间体,AHU377 calcium salt |
Neprilysin | Metabolism |
Sacubitril hemicalcium salt (AHU377 calcium salt) 是一种有效的 NEP 抑制剂,IC50=5 nM。它是研究心力衰竭药物 LCZ696 的组分之一。 | |||
TP2045 |
CH 275
|
||
Potent somatostatin receptor 1 (sst1) agonist; displays selectivity for sst1 (IC50 values are 30.9 nM, 345 nM, > 1 μM, > 10 μM and > 10μM for human sst1, sst3, sst4, sst2 and sst5 respectively). Attenuates somatostatin release in the rat nucleus accumbens | |||
T19114L |
Sacubitril-(2S,4S)-Isomer
(2S,4S)-Sacubitril,LCZ 696杂质C |
Others | Others |
Sacubitril-(2S,4S)-Isomer ((2S,4S)-Sacubitril) 是 Sacubitril 的异构体,它是一种脑啡肽酶抑制剂。 | |||
T19112L |
Sacubitril Enantiomer
2R,4S-Sacubitril,LCZ 696杂质A,ahu377 isomer 2 |
Others | Others |
Sacubitril Enantiomer (ahu377 isomer 2) 是 Sacubitril 的对映体,它是一种脑啡肽酶抑制剂。 | |||
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 | |||
T19112 |
2R,4S-Sacubitril
LCZ 696杂质A,Sacubitril Enantiomer,ahu377 isomer 2 |
Others | Others |
2R,4S-Sacubitril (Sacubitril Enantiomer) 是 Sacubitri 杂质。其中 Sacubitril 与缬沙坦联合使用,表现出抗心力衰竭的活性。 | |||
T25316 |
Dexecadotril
Retorphan |
||
Dexecadotril is a powerful and selective neprilysin inhibitor. It behaves as a prodrug of the enantiomer of thiorphan. | |||
T4574L |
Sacubitril sodium
AHU377,AHU-377,LCZ696,AHU 377 |
||
Sacubitril is an angiotensin receptor neprilysin inhibitor being studied for use in combination with valsartan for heart failure. Sacubitril is a prodrug that is activated to LBQ657 by de-ethylation via esterases. | |||
T13125 | TD-0212 | Others | Others |
TD-0212 is an orally active dual pharmacology antagonist of angiotensin II type 1 receptor (AT1) and inhibitor of neprilysin (NEP)(pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP). | |||
T13125L | TD-0212 TFA | Others | Others |
TD-0212 TFA is an orally active dual pharmacology antagonist of angiotensin II type 1 receptor (AT1) and inhibitor of neprilysin (NEP)(pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP). | |||
T71118 | NEP-28 | ||
NEP-28 is an AR agonist. NEP28 is a new SARM exhibiting high selectivity for androgen receptor. NEP28 showed tissue-selective effect equivalent to or higher than existing SARMs. In addition, the administration of NEP28 increased the activity of neprilysin, a known Aβ-degrading enzyme. | |||
T71145 |
Racecadotril-d5
|
||
Racecadotril-d5 is intended for use as an internal standard for the quantification of racecadotril by GC- or LC-MS. Racecadotril is a prodrug form of the neprilysin (NEP) inhibitor thiorphan. In vivo, racecadotril reduces or prevents castor oil-induced diarrhea without delaying intestinal transit in rats when administered at doses of 80 or 100 mg/kg, respectively. It also decreases the duration of diarrhea and increases body weight gain in a neonatal gnotobiotic pig model of human rotavirus-indu... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6627 |
Phosphoramidon Disodium
Phosphoramidon Disodium Salt,磷酰胺二钠 |
RAAS; Neprilysin; Others | Endocrinology/Hormones; Metabolism; Others |
Phosphoramidon Disodium (Phosphoramidon Disodium Salt) Salt 是一种金属蛋白酶 (metalloprotease) 抑制剂 。Phosphoramidon Disodium Salt 抑制内皮素转化酶 (ECE) ,中性肽内切酶 (NEP) 和血管紧张素转换酶 (ACE) 的IC50分别为 3.5 ,0.034 和 78 μM。 |