化合物PA-8 T41005

Product Introduction
Bioactivity


英文名: PA-8

描述: PA-8是一种小分子的的 PACAP I 型(PAC1)受体拮抗剂，有 选择性、有效性和口服活性。PA-8抑制PACAP 诱导的CREB 在PAC1-受体上的磷酸化，但对VPAC11或VPAC2受体无抑制作用。PA-8也抑制pacap 诱导的体外cAMP 水平升高(IC50 = 2 nM)和体内鞘内注射后pacap 诱导的厌恶反应和机械异位性痛。

体外活性: In PAC1/CHO cells, PA-8 (10 pM to 10 nM; 30 minutes) dose dependently inhibits PACAP (1 nM)-induced CREB phosphorylation. In VPAC1/CHO and VPAC2/CHO cells, PACAP (1 nM) also induced CREB phosphorylation; however, PA-8 (10 pM to 10 nM) does not inhibit PACAP (1 nM)-induced CREB phosphorylation [1] .

体内活性: PA-8 (100 pmol/5 μL; intrathecal injection; once; male ddY mice) treatment inhibits PACAP-induced aversive responses and mechanical allodynia in vivo [1] . PA-8 (3-30 mg/kg, p.o.) treatment results in the dose-dependent attenuation of the second phase of formalin-induced nociceptive responses. PA-8 also inhibits c-fos upregulation in the ipsilateral dorsal horn of the spinal cord [2] . Animal Model: Male ddY mice (6 weeks old) injected with PACAP (100 pmol) [1] Dosage: 100 pmol/5 μL Administration: Intrathecal injection; once Result: Inhibited PACAP-induced aversive responses and mechanical allodynia in vivo.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 22.5 mg/mL (65.7 mM)


关键字: PA 8 | PA-8 | PA8

相关产品: PACAP 1-38 acetate | PACAP (6-38), human, ovine, rat acetate | PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt) | PACAP (1-27), human, ovine, rat acetate | PACAP (1-38), human, ovine, rat | PACAP-related Peptide (human) (trifluoroacetate salt) | PACAP-related Peptide (rat) (trifluoroacetate salt) | PAC1R antagonist 1 | PACAP-38 (31-38), human, mouse, rat acetate

相关库: Bioactive Compounds Library Max | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途