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AZ8838

Catalog No.GC65312

AZ8838은 hPAR2에 대해 pKi가 6.4인 강력하고 경쟁적이며 알로스테릭하며 경구 활성인 PAR2의 비펩타이드성 소분자 길항제입니다.

Products are for research use only. Not for human use. We do not sell to patients.

AZ8838 Chemical Structure

Cas No.: 2100285-41-2

Size 가격 재고 수량
5mg
US$351.00
재고 있음
10mg
US$585.00
재고 있음
25mg
US$1,125.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2[1].

AZ8838 binds in an occluded pocket[1].AZ8838 is a potent antagonist against SLIGRL-NH2 in the Ca2+ assay with a pIC50 of 5.70 ± 0.02[1].AZ8838 shows a potency trend when inhibiting IP1 production (pIC50 = 5.84 ± 0.02)[1].AZ8838 attenuates both peptide-induced phosphorylation of ERK1/2 (pIC50 = 5.7 ± 0.1) and β-arrestin-2 recruitment (pIC50 = 6.1 ± 0.1)[1].

AZ8838 (10 mg/kg; p.o.; 2 h prior) is anti-inflammatory in a PAR2 agonist-induced rat paw oedema model[1].

[1]. Kennedy AJ, et al. Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition. Commun Biol. 2020 Dec 17;3(1):782.

Chemical Properties

Cas No. 2100285-41-2 SDF Download SDF
Formula C13H15FN2O M.Wt 234.27
Solubility Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 4.2686 mL 21.3429 mL 42.6858 mL
5 mM 0.8537 mL 4.2686 mL 8.5372 mL
10 mM 0.4269 mL 2.1343 mL 4.2686 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

리뷰

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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