Cat. No. | Product Name | Target | Signaling Pathways |
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TP1902L1 |
G-Protein antagonist peptide acetate
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Adrenergic Receptor | GPCR/G Protein; Neuroscience |
G-Protein antagonist peptide acetate 是一种 substance P 相关肽,可抑制 G 蛋白与其受体的结合。G-Protein antagonist peptide acetate 竞争性和可逆性地抑制毒蕈碱型乙酰胆碱受体 M2 (M2 muscarinic receptor) 对 Gi 或 Go 的激活,并通过 β-肾上腺素受体抑制 Gs 的激活。 | |||
TP1902 |
G-Protein antagonist peptide
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Substance P-related peptide that inhibits binding of G proteins to their receptors. Competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors. | |||
T35794 |
Kisspeptin-54 (human) (trifluoroacetate salt)
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Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-5... | |||
T36722 |
Deltorphin II (trifluoroacetate salt)
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Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid... | |||
T83697 |
PAMP-12 (human, mouse, rat, porcine, bovine) TFA
Proadrenomedullin N-terminal 12 Peptide,PAMP (9-20) |
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Proadrenomedullin N-terminal 12 peptide (PAMP-12) 是一种内源性肽段,源自人体肾上腺髓质,对应人类PAMP-20的9-20氨基酸,涉及降低血压。它是MAS相关G蛋白偶联受体家族成员X2 (MRGPRX2) 的激动剂。在表达人MRGPRX2的CHO细胞中,PAMP-12抑制forskolin诱导的cAMP积累(EC50 = 57.2 nM),特异性诱导表达MRGPRX2的CHO细胞的钙离子动员(EC50 = 41 nM),而在表达MRGPRX1、MRGPRX3或MRGPRX4的细胞中则无此效应(在1 µM浓度下)。PAMP-12还能作为烟碱型乙酰胆碱受体(nAChRs)的拮抗剂,抑制carbachol诱导的儿茶酚胺释放(IC50 = 1.3 µM)及钙和钠的流入(IC50分别为0.39 µM和0.87 µM),但不抑制组胺诱导的儿茶酚胺释放或钙和钠的流入(IC50 >1 µM),在初级牛肾上腺嗜铬细胞中有此表现。当以10至50 nmol/kg剂量给予正常血压大鼠时,PAMP-12能降低平均动脉血压。 | |||
T36717 |
RWJ-56110 dihydrochloride
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RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell ap... |