| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
TRPM8
|
|---|---|
| ln Vitro |
In tests involving heterologously produced TRP ion channels, Acoltremon (10 μM) exhibits TRPM8 agonism [1]. In DRG neurons, acoltremon (1 or 10 μM; 0-250 s) seems to be a very strong and selective TRPM8 channel agonist [1].
|
| ln Vivo |
In mice, acoltremon (ip; 10 mg/kg; once) produces analgesic effects by activating TRPM8 specifically [1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HEK293T Cell Tested Concentrations: 10 μM Incubation Duration: Experimental Results: Activates mouse TRPM8 (mTRPM8), but neither activates nor inhibits mTRPA1. Cell viability assay[1] Cell Types: Cultured Mouse DRG Neurons Tested Concentrations: 1 or 10 μM Incubation Duration: 0-250 s Experimental Results: Approximately 10% to 14% of cultured wild-type neurons were shown to respond to WS-12 . |
| Animal Protocol |
Animal/Disease Models: Trpm8–/– mice and capsaicin-injected mice [1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; 10 mg/kg; primary Experimental Results:significant analgesic effect in Trpm8-/ -The effect is lost in mice. In the rotarod test, mice demonstrated no change in latency decline. Reducing capsaicin-induced nociceptive behavior. |
| Toxicity/Toxicokinetics |
(1R,2S,5R)-N-(4-methoxyphenyl)-5-methyl-2-(1-methylethyl)-cyclohexaneformamide 2147 Scientific opinion on Fragrance Group Assessment 304 (FGE.304): From the Committee Regulation (EC) No 1565/2000 on Five Formamides in Group 30 of Chemistry (repealed by Committee Implementing Regulation (EU) No 872/2012) doi:10.2903/j.efsa.2012.2903 2012-10-12
(1R,2S,5R)-N-(4-methoxyphenyl)-5-methyl-2-(1-methylethyl)-cyclohexaneformamide 2524 Scientific opinion on Fragrance Group Assessment 304, Revision 1 (FGE.304Rev1): From Group 30 of Chemistry Four types of formamide were listed in Commission Regulation (EC) 1565/2000 (which was repealed by European Commission Implementing Regulation 872/2012) doi:10.2903/j.efsa.2014.3769 2014-07-22 |
| References | |
| Additional Infomation |
Acoltremon is being investigated in the clinical trial NCT05493111 (a long-term safety study evaluating the safety and systemic exposure of AR-15512). In the pivotal Phase 3 trial, TRYPTYR showed rapid promotion of natural tear production as early as day 1. TRYPTYR is a first-in-class TRPM8 receptor agonist that rapidly stimulates natural tear production in patients with dry eye syndrome (DED). Approximately 38 million people in the United States suffer from dry eye syndrome, but less than 10% of diagnosed patients receive prescription treatment.
|
| Molecular Formula |
C18H27NO2
|
|---|---|
| Molecular Weight |
289.419
|
| Exact Mass |
289.204
|
| Elemental Analysis |
C, 74.70; H, 9.40; N, 4.84; O, 11.06
|
| CAS # |
68489-09-8
|
| PubChem CID |
11266244
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.415
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
21
|
| Complexity |
334
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C[C@@H]1CC[C@H]([C@@H](C1)C(=O)NC2=CC=C(C=C2)OC)C(C)C
|
| InChi Key |
HNSGVPAAXJJOPQ-XOKHGSTOSA-N
|
| InChi Code |
InChI=1S/C18H27NO2/c1-12(2)16-10-5-13(3)11-17(16)18(20)19-14-6-8-15(21-4)9-7-14/h6-9,12-13,16-17H,5,10-11H2,1-4H3,(H,19,20)/t13-,16+,17-/m1/s1
|
| Chemical Name |
(1R,2S,5R)-N-(4-methoxyphenyl)-5-methyl-2-propan-2-ylcyclohexane-1-carboxamide
|
| Synonyms |
WS12; WS-12; (1R,2S,5R)-N-(4-methoxyphenyl)-5-methyl-2-(propan-2-yl)cyclohexane-1-carboxamide; Fema No. 4681; ...; Acoltremon; WS 12
|
| 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 : ~20 mg/mL (~69.11 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (6.91 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 20.0 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 | 3.4552 mL | 17.2759 mL | 34.5519 mL | |
| 5 mM | 0.6910 mL | 3.4552 mL | 6.9104 mL | |
| 10 mM | 0.3455 mL | 1.7276 mL | 3.4552 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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