PA-8 free base · Synonyms: PA 8 · PA8

PA-8 is a potent, selective and orally active PACAP type I receptor antagonist.

For research use only. Not for human or veterinary use.

Target PACAP Receptor

Research area Neurological Disease Inflammation/Immunology

Purity >98% Stock Inquire

Data Sheet SDS COA

PA-8 structure

CAS No.: 878437-15-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 310.00	BP-02214-100mg	In stock	Get quote
250 mg	USD 615.00	BP-02214-250mg	In stock	Get quote
500 mg	USD 980.00	BP-02214-500mg	In stock	Get quote
1 g	USD 1,560.00	BP-02214-1g	In stock	Get quote
2 g	USD 2,510.00	BP-02214-2g	In stock	Get quote
3 g	USD 3,020.00	BP-02214-3g	In stock	Get quote

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Description

PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM[1][2].

Biological activity

In Vitro 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. In Vivo 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.

Identifiers

SMILES: O=C1C(C(C2=CC=C(OCC=C)C(OC)=C2)CC(N3)=O)=C3N=C(N)N1
InChIKey: DCSWTWUTSKSXOV-UHFFFAOYSA-N

Specifications

MW (average): 342.3492
Formula: C₁₇H₁₈N₄O₄
CAS No.: 878437-15-1
Physical state: Solid
Color: White to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

soluble in DMSO

Documents

References

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

[2]. Ichiro Takasaki, et al. The novel small-molecule antagonist of PAC1 receptor attenuates formalin-induced inflammatory pain behaviors in mice. J Pharmacol Sci. 2019 Feb;139(2):129-132.

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