PA-9 是一种垂体腺苷酸环化酶激活多肽 (PACAP) I 型 (PAC1) 受体拮抗剂。PA-9 剂量依赖性地抑制 PACAP 诱导的 cAMP 升高，IC₅₀ 为 5.6 nM。PA-9 可用于研究神经性和/或炎症性疼痛。

PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC 50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain.

Solid

PAC1 receptor

PA-9 (10 pM to 10 nM; 30 minutes) dose dependently inhibits PACAP-induced (1 nM) CREB phosphorylation in the CHO cells expressing PAC1 receptors. has not independently confirmed the accuracy of these methods. They are for reference only.

PA-9 (100 pmol; co-injection with PACAP) attenuates the development of PACAP-induced (100 pmol/5 μL; intrathecal injection) aversive responses of mice.
PA-9 (100 pmol; co-injection with PACAP) significantly blocks the induction of PACAP-induced (100 pmol) mechanical allodynia.
PA-9 (100 pmol/5 μl; single intrathecal injection alone) does not induce aversive responses and mechanical allodynia of mice.
PA-9 is well accommodated in the subpocket formed by L80, F81, I83, G91, V92, P107, A112, and C113 of the PAC1 receptor, precipitating in hydrophobic interactions.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Takasaki I, et al. In Silico Screening Identified Novel Small-molecule Antagonists of PAC1 Receptor. J Pharmacol Exp Ther. 2018 Apr;365(1):1-8.

In Vitro: DMSO : 250 mg/mL (738.86 mM; Need ultrasonic)配制储备液