A2AR-antagonist-1 NEW
| Price | $1520 | $1980 | $2500 |
| Package | 25mg | 50mg | 100mg |
| Supply Ability: | 10g |
| Update Time: | 2026-05-11 |
Product Details
| Product Name: A2AR-antagonist-1 | CAS No.: 2922920-71-4 |
| Supply Ability: 10g | Release date: 2026/05/11 |
Product Introduction
Bioactivity
| Name | A2AR-antagonist-1 |
| Description | A2AR-antagonist-1 (compound 38), an orally active adenosine A2A receptor antagonist with an IC50 value of 29 nM, demonstrates anti-tumor properties and stability in mouse liver microsomes (t1/2 = 86.1 min). Additionally, it activates T cells by inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and promoting expression of effector molecules (GZMB, IFNG, and IL-2) [1]. |
| In vitro | A2AR-antagonist-1 (0.001-10 μM; 30 minutes) reduces NECA-induced phosphorylation of ERK levels in HEK293-A2AR cells [1]. At concentrations of 0.1-10 μM over 5 hours, this compound inhibits NECA-induced expression of immune molecules and increases the expression of effector molecules in Jurkat T cells (human immortalized T lymphocyte line) [1]. Furthermore, A2AR-antagonist-1 (0.1-10 μM; 48 hours) restores the impaired cytotoxic function of OT-I mouse splenocytes (OT-I CTL) against MC38-OVA cells and enhances in vitro T cell activation and effector functions [1]. |
| In vivo | A2AR-antagonist-1 (100 mg/kg; oral administration; once daily for 23 days) demonstrated remarkable antitumor activity in C57BL/6 mice carrying MC38 colon carcinoma cells [1]. Pharmacokinetic analysis in mice [1] revealed the following: Route Dose (mg/kg) C max (ng/mL) AUC 0-last (ng·h/mL) AUC 0-t (ng·h/mL) t 1/2 (h) F (%) for intravenous (i.v.) administration at 2 mg/kg resulted in a C max of 2584 ng/mL, AUC 0-last of 5577 ng·h/mL, AUC 0-t of 5565 ng·h/mL, and a half-life (t 1/2) of 0.93 h, while oral (p.o.) administration at 10 mg/kg achieved a C max of 8823 ng/mL, AUC 0-last of 24008 ng·h/mL, AUC 0-t of 24003 ng·h/mL, t 1/2 of 2.35 h, and bioavailability (F) of 86.1%. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| Keywords | AdenosineReceptor | Adenosine Receptor |
| Inhibitors Related | Xanthine | Theophylline monohydrate | Diphylline | Adenosine monophosphate | Acefylline | Sulcatone | Adenosine 5'-monophosphate monohydrate | Inosine | Theobromine | Adenosine 5'-monophosphate disodium salt | Theophylline | Doxofylline |
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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