Product Details
| Product Name:
AZ8838 |
CAS No.:
2100285-41-2 |
| Supply Ability:
10g |
Release date:
2025/10/27 |
Product Introduction
Bioactivity
| Name | AZ8838 |
| Description | AZ8838 is an effective, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pK i of 6.4 for hPAR2 [1]. |
| In vitro | AZ8838 demonstrates potent antagonistic activity by binding to an occluded pocket, significantly inhibiting SLIGRL-NH2 in Ca2+ assays with a pIC50 of 5.70 ± 0.02. It also shows a consistent potency trend in reducing IP1 production (pIC50 = 5.84 ± 0.02) and effectively attenuates peptide-induced phosphorylation of ERK1/2 (pIC50 = 5.7 ± 0.1) alongside β-arrestin-2 recruitment (pIC50 = 6.1 ± 0.1). |
| In vivo | AZ8838 (10 mg/kg; p.o.; 2 h prior) demonstrated anti-inflammatory effects in a rat paw oedema model induced by the PAR2 agonist 2f-LIGRLO-NH2 [1]. Utilizing Wistar rats in an acute oedema model, a single oral dose was administered 2 hours before induction, resulting in a 60% reduction in paw swelling. The compound effectively inhibited the activation of mast cells induced by 2f-LIGRLO-NH2, reduced the number of tryptase-positive (AA1+ve) intact mast cells in the paw, and blocked histamine release. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Inhibitors Related | FSLLRY-NH2 TFA(245329-02-6 free base) | LRGILS-NH2 acetate | Protease-Activated Receptor-1, PAR-1 Agonist acetate | PAR-2 Activating Peptide acetate | ML-354 | Atopaxar | Vorapaxar sulfate | Trypsin | Vorapaxar | AY 77 | PAR-2-IN-1 | VKGILS-NH2 Acetate |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States