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| 10mg |
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| 25mg |
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| 50mg |
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TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
| ln Vitro |
TRPM8 Antagonist 2 (Compound 14) is a strong TRPM8 antagonist with an IC50 of 0.2 nM and is employed in the investigation of neuropathic pain syndromes. TRPM8 Antagonist 2 effectively suppresses the menthol-induced increase in intracellular Ca2+ levels in the Ca2+ fluorescence test of HEK293 stable cells expressing the channel subtype of the TRPM8 channel (IC50, 40 nM) [1].
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| ln Vivo |
Additionally, TRPM8 antagonist 2 (0.1 and 1 μg, subcutaneous injection) can lessen oxaliplatin (OXP)-induced simulated cold allodynia [1]. TRPM8 antagonist 2 (1, 10 and 30 mg/kg, subcutaneous injection) demonstrated significant dose-dependent analgesic activity and inhibited wet dog shock (WDS)-like cold hypersensitivity at 30 mg/kg.
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| References |
| Molecular Formula |
C26H26N2O2
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|---|---|
| Molecular Weight |
398.496846675873
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| Exact Mass |
398.2
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| Elemental Analysis |
C, 78.36; H, 6.58; N, 7.03; O, 8.03
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| CAS # |
259674-19-6
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| PubChem CID |
57055437
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
507
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COC(=O)[C@H](CC1=CNC2=CC=CC=C21)N(CC3=CC=CC=C3)CC4=CC=CC=C4
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| InChi Key |
HHVOOJDLCVOLKI-VWLOTQADSA-N
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| InChi Code |
InChI=1S/C26H26N2O2/c1-30-26(29)25(16-22-17-27-24-15-9-8-14-23(22)24)28(18-20-10-4-2-5-11-20)19-21-12-6-3-7-13-21/h2-15,17,25,27H,16,18-19H2,1H3/t25-/m0/s1
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| Chemical Name |
methyl (2S)-2-(dibenzylamino)-3-(1H-indol-3-yl)propanoate
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| Synonyms |
TRPM8 antagonist 2; HVN74196; HVN-74196; HVN 74196;
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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 : ~100 mg/mL (~250.94 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.67 mg/mL (6.70 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 26.7 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: ≥ 2.67 mg/mL (6.70 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 26.7 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: ≥ 2.67 mg/mL (6.70 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 | 2.5094 mL | 12.5471 mL | 25.0941 mL | |
| 5 mM | 0.5019 mL | 2.5094 mL | 5.0188 mL | |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5094 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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