| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
TCS-5861528 targets the transient receptor potential ankyrin 1 (TRPA1) channel, a non-selective cation channel involved in pain, inflammation, and sensory transduction. By blocking TRPA1, the compound antagonizes AITC- and 4-HNE-evoked calcium influx through the channel. It attenuates diabetic hypersensitivity in an in vivo rat model.
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| ln Vitro |
At dosages up to 100 μM, Chembridge-5861528 (TCS 5861528) does not display TRPV1 channel antagonism or agonism against TRPA1 or TRPV1 channels [1].
In vitro, TCS-5861528 is a TRPA1 channel blocker with IC50 values of 14.3 μM and 18.7 μM for antagonizing AITC- and 4-HNE-evoked TRPA1 responses, respectively. Its activity is assessed by measuring calcium flux in cells expressing TRPA1 channels upon activation by AITC or 4-HNE. |
| ln Vivo |
In a streptozocin-induced diabetic rat model, Chembridge-5861528 (TCS 5861528) (30 mg/kg; intraperitoneally; twice daily for one week) greatly reduces the development of mechanical hypersensitivity [1]. The effects of capsaicin on blood flow are attenuated in a dose-related manner by Chembridge-5861528 (3 and 10 μg/rat; once) [2].
In vivo, TCS-5861528 attenuates diabetic hypersensitivity in an in vivo rat model. By blocking TRPA1 channels, the compound reduces pain and hypersensitivity in diabetic conditions. It has potential applications in the study and treatment of pain and inflammatory conditions where TRPA1 plays a role. |
| Enzyme Assay |
In vitro receptor binding/functional assays for TCS-5861528 measure its inhibition of TRPA1-mediated calcium influx. Cells expressing TRPA1 channels are treated with serial dilutions of the compound, and calcium flux is measured using fluorescent calcium indicators upon activation by AITC or 4-HNE. IC50 values of 14.3 μM and 18.7 μM are determined for AITC and 4-HNE, respectively.
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| Cell Assay |
In vitro cell-based assays for TCS-5861528 use cells expressing TRPA1 channels. Cells are treated with serial dilutions of the compound, and TRPA1-mediated calcium influx is measured using fluorescent calcium indicators. The IC50 for inhibition of TRPA1 activation is calculated from dose-response curves. Cell viability is assessed in parallel.
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| Animal Protocol |
Animal/Disease Models: Male Hannover-Wistar rat, streptozotocin-induced diabetes model [1]
Doses: 30 mg/kg Route of Administration: intraperitoneal (ip) injection twice (two times) daily for one week Experimental Results: Paw pressure test demonstrated mechanical hypersensitivity Development was Dramatically attenuated (F1,80= 31.4, P < 0.0001). Animal/Disease Models: Male Hannover-Wistar rat (220-260 g), capsaicin-induced neurogenic inflammation model [2] Doses: 0, 3, 10 μg/rat Route of Administration: Sheath 20 minutes before injection of capsaicin Intra-injection Experimental Results: Dramatically diminished blood flow 10μg. In vivo animal models for TCS-5861528 include rat models of diabetic hypersensitivity. The compound is administered via appropriate routes, and its effects on pain behavior, hypersensitivity, and sensory function are evaluated. Pharmacodynamic studies measure TRPA1 antagonism and pain relief in response to compound treatment. |
| ADME/Pharmacokinetics |
TCS-5861528 has a molecular formula of C19H23N5O3 and a molecular weight of 369.42 g/mol. It is also known as Chembridge-5861528 and has the chemical name N-(4-(sec-Butyl)phenyl)-2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)acetamide. The compound has a purity of ≥98% and is soluble in DMSO at 76 mg/mL.
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| Toxicity/Toxicokinetics |
The toxicity profile of TCS-5861528 is characterized in preclinical safety studies. As a TRPA1 channel blocker, the compound may affect pain sensation and inflammation. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
TCS-5861528 (Chembridge-5861528) is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx with IC50 values of 14.3 μM and 18.7 μM, respectively. It attenuates diabetic hypersensitivity in an in vivo rat model. TCS-5861528 is also known as Chembridge-5861528 and is intended for laboratory research use only.
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| Molecular Formula |
C19H23N5O3
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|---|---|
| Molecular Weight |
369.41762
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| Exact Mass |
369.18
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| CAS # |
332117-28-9
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| PubChem CID |
2873523
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| Appearance |
White to off-white solid powder
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| LogP |
1.658
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
590
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZUTUWJYMCADJHD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H23N5O3/c1-5-12(2)13-6-8-14(9-7-13)21-15(25)10-24-11-20-17-16(24)18(26)23(4)19(27)22(17)3/h6-9,11-12H,5,10H2,1-4H3,(H,21,25)
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| Chemical Name |
N-(4-butan-2-ylphenyl)-2-(1,3-dimethyl-2,6-dioxopurin-7-yl)acetamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~120 mg/mL (~324.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (8.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (8.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7069 mL | 13.5347 mL | 27.0695 mL | |
| 5 mM | 0.5414 mL | 2.7069 mL | 5.4139 mL | |
| 10 mM | 0.2707 mL | 1.3535 mL | 2.7069 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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