| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Animal Protocol |
Systemic administration: A-836339 was dissolved in 5% DMSO/95% PEG-400 (v/v) and administered intraperitoneally (i.p.) at a volume of 2 mL/kg, 30 minutes before behavioral testing. For antagonist studies, SR144528 or rimonabant were administered i.p. 15 minutes before A-836339. Naloxone was administered i.p. 20 minutes before A-836339. [3]
Local administration (intra-DRG and intrathecal): A-836339 was dissolved in 10% DMSO/90% hydroxyl-β-cyclodextrin (30%, w/w) in water (v/v) and administered at an injection volume of 10 μL, 30 minutes before behavioral testing. For intra-DRG administration, the catheter tip was positioned 1–2 mm dorsal to the exposed L5 DRG; for intrathecal administration, the catheter tip was advanced 8.5 cm caudally to the lumbar enlargement (L4-L6). [3] Intraplantar administration: A-836339 was dissolved in the same vehicle and administered into the intra-plantar surface of the hind paw at a volume of 50 μL, 30 minutes before testing. [3] CFA inflammatory pain model: Chronic inflammatory pain was induced by intraplantar injection of 150 μL of 50% CFA emulsion in PBS. Thermal hyperalgesia was assessed 48 hours post-CFA using a Hargreaves-type apparatus, with a cutoff of 20.48 seconds. Paw withdrawal latency was measured 30 minutes after drug administration. [3] SNL neuropathic pain model: L5 and L6 spinal nerves were ligated unilaterally. Mechanical allodynia was assessed 7–14 days post-surgery using von Frey filaments with the up-down method. Paw withdrawal threshold was measured 30 minutes after drug administration. [3] CCI neuropathic pain model: The right sciatic nerve was loosely ligated with four chromic gut ties. Mechanical allodynia was assessed 2–3 weeks post-surgery using von Frey filaments. [3] |
|---|---|
| References |
|
| Molecular Formula |
C16H26N2O2S
|
|---|---|
| Molecular Weight |
310.456
|
| Exact Mass |
310.171
|
| CAS # |
959746-77-1
|
| PubChem CID |
17754357
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
388.4±44.0 °C at 760 mmHg
|
| Flash Point |
188.7±28.4 °C
|
| Vapour Pressure |
0.0±0.9 mmHg at 25°C
|
| Index of Refraction |
1.561
|
| LogP |
3.88
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
21
|
| Complexity |
506
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JKGIMVBQKSRTGX-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H26N2O2S/c1-10-11(2)21-14(18(10)8-9-20-7)17-13(19)12-15(3,4)16(12,5)6/h12H,8-9H2,1-7H3
|
| Chemical Name |
N-[3-(2-methoxyethyl)-4,5-dimethyl-1,3-thiazol-2-ylidene]-2,2,3,3-tetramethylcyclopropane-1-carboxamide
|
| Synonyms |
A-836339 A836339 A 836339 A 836,339 A836,339A-836,339
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~12 mg/mL (~38.65 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.71 mg/mL (2.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 7.1 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.71 mg/mL (2.29 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 7.1 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. View More
Solubility in Formulation 3: ≥ 0.71 mg/mL (2.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2210 mL | 16.1051 mL | 32.2103 mL | |
| 5 mM | 0.6442 mL | 3.2210 mL | 6.4421 mL | |
| 10 mM | 0.3221 mL | 1.6105 mL | 3.2210 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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