Shopping Cart
- Remove All
Your shopping cart is currently empty
PA-8
Catalog No. T41005Cas No. 878437-15-1
PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors. PA-8 also inhibited PacAP-induced elevation of cAMP levels in vitro (IC50 = 2 nM) and PacAP-induced aversive response and mechanical atopic pain after intrathecal injection in vivo.
PA-8
Catalog No. T41005Cas No. 878437-15-1
PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors. PA-8 also inhibited PacAP-induced elevation of cAMP levels in vitro (IC50 = 2 nM) and PacAP-induced aversive response and mechanical atopic pain after intrathecal injection in vivo.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $39 | In Stock | |
| 10 mg | $72 | In Stock | |
| 25 mg | $155 | In Stock | |
| 50 mg | $272 | In Stock | |
| 100 mg | $478 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $43 | In Stock |
Bulk & Custom
Add to Cart
Questions
View MoreInhibitors Related to "PA-8"
PACAP-38 (31-38), human, mouse, rat acetate
PACAP-38 (31-38), human, mouse, rat acetate(138764-85-9 Free base)
TP1618L
PACAP-38 (31-38), human, mouse, rat acetate is an activator of PAC1 receptor. PACAP-38 (31-38), human, mouse, rat acetate demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production and can
- $137
Size
QTY
PACAP (1-27), human, ovine, rat acetate
PACAP 1-27 acetate, PACAP (1-27), human, ovine, rat acetate(127317-03-7 free base)
TP1070L
PACAP (1-27), human, ovine, rat acetate (PACAP 1-27 acetate) is a novel neuropeptides originally isolated from bovine hypothalamus, also found in humans and rats.
- $153
Size
QTY
PACAP 1-38 acetate
TP1878L
PACAP 1-38 acetate is a pituitary adenylate cyclase activating polypeptide (PACAP) analogue. PACAP 1-38 acetate binds to PACAP type I receptor(IC50 = 4 nM) and PACAP type II VIP2 receptor(IC50 = 1 nM) but not to PACAP type II, VIP1 receptor.
- $163
Size
QTY
PACAP (1-38), human, ovine, rat
Pituitary Adenylate Cyclase Activating Polypeptide 38, PACAP 1-38
TP1878137061-48-4
PACAP (1-38), human, ovine, rat (Pituitary Adenylate Cyclase Activating Polypeptide 38), is a neuropeptide comprising 38 amino acid residues.
- $143
Size
QTY
PAC1R antagonist 1
T781052305204-24-2
PAC1R antagonist 1 is an orally active PAC1 receptor antagonist that inhibits abnormal pain induced by pituitary adenylate cyclase-activating polypeptide (PACAP) and nerve damage, and may be used in the study of neoplasms and immune-related disorders.
- $149
Size
QTY
PACAP (6-38), human, ovine, rat acetate
TP1722L
PACAP (6-38), human, ovine, rat acetate is a potent PACAP receptor antagonist with IC50s of 30, 600, and 40 nM for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively.
- $89
Size
QTY
PACAP-related Peptide (rat) (trifluoroacetate salt)
T37435
PACAP-related peptide (PRP) is an endogenous 29-amino acid peptide that belongs to the secretin/glucagon superfamily of peptides, which includes secretin , glucagon , glucagon-like peptide-1 , GLP-2 , and pituitary adenylate cyclase-activating polypeptide . It is expressed in rat hypothalamus as well as within the nerves of the median eminence, the anterior pituitary, bed nucleus of the stria terminalis, cerebellum, cerebral cortex, and amygdala. PRP is also expressed in vaginal, uterine cervical, uterine horn, fallopian tube, and ovarian tissues from the rat female genital tract and is present in extracts of male testis tissue.
- $505
Size
QTY
PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt)
T36427
Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.
- $445
Size
QTY
PACAP-related Peptide (human) (trifluoroacetate salt)
T36428
PACAP-related peptide (PRP) is an endogenous 29-amino acid peptide that belongs to the secretin/glucagon superfamily of peptides, which includes secretin , glucagon , glucagon-like peptide-1 , GLP-2 , and pituitary adenylate cyclase-activating polypeptide . It is expressed in normal human pancreas and adrenal gland tissue and in some tumors that produce vasoactive intestinal peptide (VIP). PRP (1-29) is secreted by CHO-K1 cells that express human recombinant preproPACAP.
- $891
Size
QTY
Select Batch
Purity:97.64%
Contact us for more batch information
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors. PA-8 also inhibited PacAP-induced elevation of cAMP levels in vitro (IC50 = 2 nM) and PacAP-induced aversive response and mechanical atopic pain after intrathecal injection in vivo. |
| Targets&IC50 | cAMP:2 nM |
| 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 induces CREB phosphorylation; however, PA-8 (10 pM to 10 nM) does not inhibit this effect [1]. |
| In vivo | Treatment with PA-8 (100 pmol/5 μL; via intrathecal injection; single dose; in male ddY mice) effectively suppresses PACAP-induced aversive reactions and mechanical allodynia in vivo [1]. Additionally, oral administration of PA-8 (3-30 mg/kg) leads to a dose-dependent reduction in the second phase of formalin-induced pain responses. PA-8 also significantly reduces c-fos expression in the spinal cord's ipsilateral dorsal horn [2]. This showcases PA-8's potential in mitigating nociceptive behaviors and neuronal activation in a PACAP-administered male ddY mouse model (6 weeks old; 100 pmol PACAP) [1], confirming its analgesic and anti-allodynic effects in vivo. |
| Molecular Weight | 342.35 |
| Formula | C17H18N4O4 |
| Cas No. | 878437-15-1 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 22.5 mg/mL (65.7 mM), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
| |||||||||||||||||||||||||||||||
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Preview
Related Tags: buy PA-8 | purchase PA-8 | PA-8 cost | order PA-8 | PA-8 chemical structure | PA-8 in vivo | PA-8 in vitro | PA-8 formula | PA-8 molecular weight
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.