Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7656 |
Apelin-13
|
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Apelin-13 是存在于中枢和外周神经系统由13个氨基酸组成的多肽序列,是 G 蛋白偶联受体angiotensin II protein J (APJ) 的内源性配体,对 APJ 的 EC50 值为 0.37 nM。Apelin-13 具有扩张血管和降压活性,可用于研究 2 型糖尿病综合征。 | |||
T10843 |
CMF019
|
Apelin receptor | GPCR/G Protein |
CMF019 是一种有效的小分子 Apelin receptor (APJ) 激动剂,具有 G protein 偏向性。 CMF019 在人,大鼠和小鼠中与 APJ 结合的 pKi 值分别为 8.58、8.49 和 8.71。CMF-019 在啮齿动物中的有益于心血管。 Apelin 受体 (APJ) 是由内源性肽 apelin 激活的 G 蛋白偶联受体(GPCR)。 | |||
T14390L | (2R,3S)-Azelaprag | Apelin receptor | GPCR/G Protein |
(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide 是一种Apelin 受体激动剂,对Apelin 受体的EC50为0.012 µM。(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide 可用于治疗心力衰竭、动脉粥样硬化、肥胖、糖尿病、肌萎缩侧索硬化、冠心病、高血压、中风和心肌梗塞等疾病。 | |||
TP1260 |
[Pyr1]-Apelin-13
[pGlu1]-Apelin-13,人牛吡啶APELIN-13 |
Apelin receptor | GPCR/G Protein |
[Pyr1]-Apelin-13 ([pGlu1]-Apelin-13) 是一种高效的、内源性 apelin 受体选择性激动剂。 | |||
T14390 |
Azelaprag
AMG 986 |
Apelin receptor | GPCR/G Protein |
Azelaprag (AMG 986) 是一种有效的小分子 apelin 受体激动剂。Azelaprag 可用于治疗神经系统疾病、 心血管疾病。 | |||
TP2092L |
Apelin-17 (human, bovine) acetate
Apelin-17 (human, bovine) acetate(217082-57-0 free base) |
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
Apelin-17 (human, bovine) acetate(217082-57-0 free base) 是一种内源性 apelin 受体激动剂。有效抑制毛喉素刺激的 cAMP 积累 (pIC50 = 9.94)。 | |||
T39823L |
Apelin-12 acetate
Apelin-12 acetate (229961-08-4 Free base) |
Apelin receptor; p38 MAPK; JNK | GPCR/G Protein; MAPK |
Apelin-12 acetate 对 APJ 受体具有高亲和力。 Apelin-12 acetate 抑制凋亡相关 MAPKs 家族的 JNK 和 p38 MAPK 信号通路,从而为神经元提供保护。 | |||
T7847 |
Apelin-13 triTFA(217082-58-1(free base))
|
Others | Others |
Apelin-13 triTFA(217082-58-1(free base)) 是 APJ 受体的内源性配体,可激活该 G 蛋白偶联受体,EC50 值为 0.37 nM。 | |||
TP1922L1 |
ELA-11 (human) acetate(1784687-32-6 free base)
|
Apelin receptor; Arrestin | GPCR/G Protein |
ELA-11 (human) acetate(1784687-32-6 free base)是亲和力 apelin 受体激动剂 (Ki = 14 nM)。 ELA-32 的生物活性片段。在体外抑制毛喉素诱导的 cAMP 产生并刺激 β-arrestin 募集。 | |||
T10346 |
Apelin agonist 1
|
Others | Others |
Apelin agonist 1 is an oral selective apelin agonist AM-2995, an agonist of the APJ (APLNR, angiotensin receptor like-1) receptor. It may be used in the treatment of cardiovascular conditions. | |||
TP2001 |
MM 54
|
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Potent apelin receptor antagonist (Ki = 82 nM; IC50 = 93 nM). Antagonizes the inhibitory affect of [Pyr1]-Apelin-13 on forskolin-induced cAMP accumulation in CHO-K1-APJ cells. Recuces tumor expansion and lengthens survival time in a mouse xenograft model | |||
T39823 |
Apelin-12
|
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Apelin-12 is a highly potent C-terminal fragment of a polypeptide that exhibits a strong affinity towards the orphan receptor APJ. It plays a role in maintaining body fluid balance and regulating feeding control in the central nervous system. Additionally, Apelin-12 functions as an inhibitor of HIV-1 entry through the APJ receptor and demonstrates neuroprotective properties. | |||
T63669 |
APJ receptor agonist 6
|
||
APJ receptor agonist 6 是 APJ (apelin 受体) 的有效激动剂 (Ki: 0.059 μM)。APJ receptor agonist 6 能够作用于钙 (calcium) (EC50: 0.800 μM)、cAMP (EC50: 0.844 μM) 和 β-arrestin (EC50: 6.22 μM)。 | |||
T64305 |
APJ receptor agonist 7
|
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APJ receptor agonist 7 (化合物 37) 是一种口服具有活力的 APJ (apelin 受体) 激动剂 (Ki: 0.059 μM)。APJ receptor agonist 7 能够作用于钙 (EC50: 0.070 μM)、cAMP (EC50: 0.097 μM) 和 β-arrestin (EC50: 0.063 μM)。 | |||
TP2096 |
ELA-21 (human)
|
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High affinity apelin receptor agonist. Binds apelin receptors in left ventricle from normal and pulmonary arterial hypertensive (PAH) hearts (pKi values are 9.31 and 9.46, respectively). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP produc | |||
T61330 |
ML233
|
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ML233 is a potent non-peptide apelin receptor agonist (EC50 = 3.7 μM) that exhibits more than 21-fold selectivity over the closely related angiotensin 1 receptor (AT1) (>79 μM) [1]. | |||
TP2092 |
Apelin-17(human, bovine)
Apelin-17 (human, bovine) |
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Endogenous apelin receptor agonist. Potently inhibits forskolin-stimulated cAMP accumulation (pIC50 = 9.94). | |||
TP1424 |
Apelin-13 TFA (217082-58-1 free base)
Apelin-13 TFA |
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Apelin-13 is an endogenous ligand of APJ receptor, and the EC 50 value of activated G protein coupled receptor is 0.37 nM. | |||
T75785 |
Apelin-17(human, bovine) TFA
|
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Apelin-17(human, bovine) TFA 是一种内源性孤儿 G 蛋白偶联受体 APJ 激动剂。Apelin-17(human, bovine) TFA 与在 HEK 293 细胞中表达的人 APJ 受体结合 (pIC50)。Apelin-17(human, bovine) TFA 阻断 HIV-1和 HIV-2毒株进入表达 APJ 的 NP-2/CD4 细胞。 | |||
T75783 |
Apelin-36(human) TFA
|
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Apelin-36(human) TFA 是一种内源性孤儿 G 蛋白偶联受体 APJ 激动剂,EC50为 20 nM。Apelin-36(human) TFA 对 HEK 293 细胞表达的人 APJ 受体有很高的亲和力 (pIC50=8.61)。Apelin-36(human) TFA 与两种主要的生物活性有关:心血管和代谢。Apelin-36(human) TFA 抑制 HIV-1和 HIV-2进入表达 APJ 的 NP2/CD4细胞。 | |||
TP1922 |
ELA-11(human)
ELA-11 (human) |
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High affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro. | |||
T39813 |
APJ receptor agonist 1
|
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APJ receptor agonist 1, a potent biphenyl acid derivative, acts as an agonist (EC50 of 0.093 nM and 0.12 nM for human and rat APJ receptors, respectively) for the APJ receptor (APJ-R). It exhibits significant in vitro potency towards apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 holds promise for heart failure research. | |||
TP1923 |
Elabela(19-32)
ELA-14 (human) |
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Potent apelin (APJ) receptor agonist (Ki = 0.93 nM). Bioactive fragment of ELA-32. Activates Gαi1 pathway and β-arrestin-2 recruitment. Reduces arterial pressure in rat hearts. Active in vivo. | |||
T39587 |
APJ receptor agonist 4
|
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APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease. | |||
T75784 |
Apelin-36(rat, mouse) TFA
|
||
Apelin-36(rat, mouse) TFA 是一种内源性孤儿 G 蛋白偶联受体 APJ 激动剂。Apelin-36(rat, mouse) TFA 与 APJ 受体结合,IC50为 5.4 nM,显著抑制 cAMP 的产生,EC50为 0.52 nM。Apelin-36(rat, mouse) TFA 阻断 HIV-1和 HIV-2毒株进入表达 APJ 的 NP-2/CD4 细胞。 | |||
T76044 |
Elabela(19-32) TFA
|
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Elabela(19-32) TFA 是ELABELA(ELA)与apelin受体(APJ)结合的活性片段,能激活Gαi1和β-arrestin-2信号通路,EC50值分别为8.6 nM和166 nM。该化合物可诱导受体内在化,降低动脉压,并对心脏具有正性肌力作用。 | |||
T63153 | APJ receptor agonist 5 | ||
APJ receptor agonist 5 (compound 3) 是一种有效的、口服具有活力的 apelin 受体 (APJ) 激动剂 (EC50: 0.4 nM)。APJ receptor agonist 5 在啮齿动物心力衰竭 (HF) 模型中具有出色的药代动力学特征,在临床前毒理学研究中也具有可接受的安全性。APJ receptor agonist 5 能够改善心脏功能,可用于 HF 疾病的研究。 | |||
T76053 |
ELA-11(human) TFA
|
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ELA-11(human) TFA is a high affinityapelin receptoragonist (Ki=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro. | |||
TP2097 |
ELA-32(human)
ELA-32 (human) |
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Potent, high affinity apelin receptor agonist (IC50 = 0.27 nM; Kd = 0.51 nM). Exhibits no binding GPR15 and GPR25. Activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. Also potentiates the T | |||
T76052 |
ELA-32(human) TFA
|
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ELA-32(human) TFA is a potent, high affinityapelin receptoragonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells. |