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Submit ReviewPA 8 is a PAC1 receptor antagonist. Inhibits PACAP-induced CREB phosphorylation in PAC1, but not VPAC1 or VPAC2, expressing cells. Also inhibits PACAP-induced increases in cAMP levels in vitro (IC50 = 2 nM) and PACAP-induced aversive responses and mechanical allodynia following intrathecal injection in vivo.
PA 8 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 342.35 |
公式 | C17H18N4O4 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 878437-15-1 |
PubChem ID | 6485327 |
InChI Key | DCSWTWUTSKSXOV-UHFFFAOYSA-N |
Smiles | COC1=C(C=CC(C2CC(NC3=C2C(N=C(N3)N)=O)=O)=C1)OCC=C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 17.12 | 50 |
以下数据基于产品分子量 342.35。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 5.84 mL | 29.21 mL | 58.42 mL |
2.5 mM | 1.17 mL | 5.84 mL | 11.68 mL |
5 mM | 0.58 mL | 2.92 mL | 5.84 mL |
25 mM | 0.12 mL | 0.58 mL | 1.17 mL |
参考文献是支持产品生物活性的出版物。
Takasaki et al (2018) In silico screening identified novel small-molecule antagonists of PAC1 receptor. J.Pharmacol.Exp.Ther. 365 1 PMID: 29363578
If you know of a relevant reference for PA 8, please let us know.
关键词: PA 8, PA 8 supplier, PA8, Pituitary, adenylate, cyclase-activating, polypeptide, PACAP, receptors, antagonists, antagonism, PAC1, analgesics, analgesia, Receptors, 6657, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PA 8 的部分引用包括:
Varodayan et al (2020) PACAP regulation of central amygdala GABAergic synapses is altered by restraint stress. Neuropharmacology 168 PMID: 31476352
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