A-1165442 NEW
| Price | $364 | $1490 | $1940 |
| Package | 5mg | 25mg | 50mg |
| Supply Ability: | 10g |
| Update Time: | 2026-05-11 |
Product Details
| Product Name: A-1165442 | CAS No.: 1221443-94-2 |
| Supply Ability: 10g | Release date: 2026/05/11 |
Product Introduction
Bioactivity
| Name | A-1165442 |
| Description | A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM. |
| In vitro | A-1165442 is a potent, competitive antagonist of recombinant human TRPV1, evidenced by its IC50 value of 9 nM when activated by capsaicin and achieves a 62% block at 30 μM in acid-evoked responses, indicating incomplete blockade. It demonstrates exceptional selectivity, exceeding 100-fold over related TRP family members (TRPA1, TRPM8, TRPV2, TRPV3) and shows minimal cross-reactivity with other receptors and channels prevalent in peripheral sensory neurons, such as P2X2/3, Cav2.2, Nav channels, and KCNQ2/3. Furthermore, A-1165442 maintains limited cross-reactivity across a broad panel of 74 cell-surface receptors, ion channels, and enzymes at 10 μM, as assessed in a comprehensive screen (CEREP)[1]. |
| In vivo | A-1165442 demonstrates exceptional pharmacological selectivity, a favorable pharmacokinetic profile, and robust efficacy in mitigating osteoarthritis pain in rodents. Its oral administration effectively inhibits capsaicin-induced nocifensive behaviors in rats, achieving an ED50 of 9.5 μmol/kg, which corresponds to a plasma concentration of 420 ng/mL (970 nM). Furthermore, a single dose markedly enhances grip strength, with an ED50 of 35 μmol/kg observed one hour after administration. Notably, its analgesic potency increases with repeated doses. Importantly, administration of A-1165442 does not significantly alter core body temperature in conscious rats, maintaining this temperature-neutral effect in conscious dogs[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (231.56 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (7.64 mM), Sonication is recommended. |
| Keywords | TRPVChannel | TRPV Channel | TRPChannel | TRP Channel | human TRPV1 | A-1165442 | A1165442 | A 1165442 |
| Inhibitors Related | (+)-Camphor | Rosiglitazone | Caffeic Acid | Oleoyl Serotonin | (-)-Menthol | Camphor | Probenecid | Pregnenolone | Nonivamide | 1,4-Cineole | trans-Cinnamaldehyde | Methyl salicylate |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
You may like
-
CAS:96850-30-5
-
-
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
|
VIP1Y
|
Henan Boweixin Biotechnology Co., Ltd.
|
2026-05-29 | ||
| $100.00 |
VIP1Y
|
Rongchuang International
|
2026-06-04 | |
|
VIP6Y
|
RongNa Biotechnology Co.,Ltd
|
2026-06-24 |
United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, USA
INQUIRY