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抑制剂&激动剂
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endothelin-2 , human

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  • 抑制剂&激动剂
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  • Endothelin-2 (49-69), human
    人内皮素2, Human endothelin-2, Endothelin-2, human, Endothelin-2 (human, canine)
    TP1174123562-20-9
    Endothelin-2 (49-69), human (Human endothelin-2) 是一种由 21 个氨基酸组成的血管活性肽。它可与 G 蛋白连接的跨膜受体,ET-RA 和ET-RB 结合。
    • ¥ 2690
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  • Endothelin-2 (49-69), human TFA
    Endothelin-2 (49-69) (human, canine) TFA,Human endothelin-2 TFA
    TP2143
    Endothelin-2 (49-69), human (TFA) is a 21-amino acid vasoactive peptide that binds to ET-RA and ET-RB.
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  • ETRB Antagonist 1
    T9621290815-30-4In house
    N-(6-chloro-5-(2-Methoxyphenoxy)-2-(pyridin-4-yl)pyriMidin-4-yl)-5-Met 抑制内皮素与CHO 细胞膜上人ETA 受体和人ETB 受体的的结合,IC50分别为268nM 和 1810nM。
    • ¥ 1300
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  • Nebentan
    T36007403604-85-3
    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 dependent manner,Ki values are 0.697 nM and 1.53 nM for human and rat endothelin ETA receptors, respectively. In contrast, YM598 exhibits low affinities for human and rat endothelin ETB receptors, with Ki values of 569 nM and 155 nM,respectively[1].In measurement of intracellular Ca2+ concentration, Nebentan concentration-dependently inhibits the increase in [Ca2+]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC50 values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively[1]. Nebentan (oral administration; 0.1-1 mg kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy[2].Nebentan (oral administration; 1 mg kg; 30 weeks) significantly ameliorates the poor survival rate of CHF rats, it markedly reduces the hypertrophy of both ventricles as well as pulmonary congestion[2]. [1]. Hironori Yuyama, et al. Pharmacological Characterization of YM598, an Orally Active and Highly Potent Selective Endothelin ET(A) Receptor Antagonist. Eur J Pharmacol. 2003 Sep 30;478(1):61-71. [2]. Akira Fujimori, et al. YM598, an Orally Active ET(A) Receptor Antagonist, Ameliorates the Progression of Cardiopulmonary Changes and Both-Side Heart Failure in Rats With Cor Pulmonale and Myocardial Infarction. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:S354-7.
    • ¥ 1992
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  • BQ-123 TFA
    T73877
    BQ-123 TFA 是一种高效、选择性内皮素 A(ETA)受体拮抗剂,IC50值为 7.3 nM,Ki 值为 25 nM。BQ-123 TFA 抑制内皮素-1 介导的人肺动脉平滑肌细胞增殖,降低高血压大鼠血压。
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  • [Ala2] Endothelin-3, human
    T763052243207-08-9
    [Ala2] Endothelin-3, human 为ET-3的线性类似物,其结构中的Cys残基被Ala所替代。ET-3是由人体横纹肌肉瘤细胞系产生,且仅在此细胞系中表达的一种具有血管活性的肽。在非肌肉来源的肉瘤细胞系中不表达。该肽能够作为旁分泌因子,促进内皮细胞迁移。
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