| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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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].
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|---|---|
| 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].
|
| 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. |
| References |
| Molecular Formula |
C19H23N5O3
|
|---|---|
| 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)
|
|---|---|
| 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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