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CAS No. : 204067-01-6
MCE 国际站:PD176252
产品活性:PD176252 是一种有效的 BB1 和 BB2 拮抗剂,能够抑制人 BB1 和 BB2 受体和大鼠 BB1 和 BB2 受体活性,Ki 值分别为 0.17 nM,1 nM 和 0.66 nM,16 nM;PD176252 同时为 FPR1/FPR2 的激动剂,在 HL-60 细胞中,EC50 值分别为 0.31 和 0.66 μM。
研究领域:GPCR/G Protein
作用靶点:Bombesin Receptor
In Vitro: PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively. PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C at the human BB1 or BB2 receptors expressed in CHO cells, with the appKBs of 4.0 nM or 13 nM, and blocks bombesin-evoked increases in intracellular calcium levels in CHO cells stably expressing human BB1 or BB2 receptors, with appKBs of 2.3 nM and 36 nM, respectively. PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells. PD176252 activates Ca2+ mobilization in HL-60 cells transfected with human FPRs (EC50, 0.72 ± 0.21 μM). PD176252 inhibits little specific 125I-gastrin releasing peptide binding to NCI-H345 cells at 1 nM and suppresses almost all specific bindings at 1000 nM, with an IC50 of 30 nM. PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC50s of 7 and 5 μM.
In Vivo: PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice.
相关产品:Covalent Screening Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Anti-Cancer Compound Library | Covalent Screening Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | BA 1 | Bombesin | Litorin | RC-3095 TFA | BIM-26226 | ML-18 | MK-5046 | Ranatensin | Kuwanon G | (D-Phe6,Leu-NHEt13,des-Met14)-Bombesin (6-14) | BIM 23042 | Kuwanon H | PD 168368
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货号: HY-103286
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