| 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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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
AMTB HCl targets the TRPM8 (Transient Receptor Potential Melastatin 8) ion channel, acting as a potent and selective antagonist. It inhibits calcium influx induced by the TRPM8 agonist icilin with an IC50 value of 0.58 µM. In calcium influx assays, AMTB HCl demonstrates a pEC50 of 6.91, with no significant activity against TRPV4 (pEC50<4.6). By blocking TRPM8, it modulates cold and menthol sensing, making it a key tool for studying the channel's role in pain, inflammation, and sensory physiology.
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| ln Vitro |
Each NaV1 isoform's membrane potential alterations brought on by veratridine are blocked by AMTB hydrochloride (pIC50 range of NaV1.1-NaV1.8 is 4.83-5.69) [2]. AMTB hydrochloride decreases the migration of MDA-MB-231 cells (30 μM) and the number of viable cells in the SK-BR-3 and MDA-MB-231 breast cancer cell lines (30 and 100 μM) [2].
In vitro, AMTB HCl acts as a highly potent and selective TRPM8 channel blocker, effectively inhibiting TRPM8-mediated calcium influx with an IC50 of 0.58 µM. It shows a pEC50 of 6.91 in calcium influx assays and exhibits negligible activity against TRPV4 channels (pEC50<4.6). These properties confirm its specificity for TRPM8 over other TRP channels. The compound's in vitro activity is typically assessed using calcium imaging or electrophysiological techniques in cells heterologously expressing TRPM8. |
| ln Vivo |
In anesthetized rats, AMTB (3 mg/kg; i.v.) hydrochloride lowers the frequency, but not the amplitude, of volume-induced bladder contractions [1].
In vivo, AMTB HCl has demonstrated significant effects in animal models of pain and urinary dysfunction. For rats, AMTB (10 mg/kg) significantly attenuated reflex responses to noxious urinary bladder distension (UBD), reducing the visceromotor reflex (VMR) response and pressor response to 5.42% and 56.51% of the maximal response, respectively. These findings support its potential for treating pain and urinary diseases. Its in vivo efficacy highlights the therapeutic relevance of TRPM8 antagonism. |
| Enzyme Assay |
The in vitro receptor binding/functional assay for AMTB HCl typically involves measuring its ability to block TRPM8-mediated calcium influx. Cells heterologously expressing TRPM8 are loaded with a calcium-sensitive fluorescent dye and stimulated with a TRPM8 agonist such as icilin or menthol. The compound's ability to inhibit the agonist-induced calcium signal is measured, and the IC50 value is determined from concentration-response curves. These cell-free or cell-based assays provide a direct measure of its antagonistic potency.
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| Cell Assay |
In vitro cellular assays for AMTB HCl are commonly performed using cell lines that heterologously express the TRPM8 channel. Cells are pre-incubated with various concentrations of AMTB HCl and then stimulated with a TRPM8 agonist like icilin. The resulting changes in intracellular calcium levels are measured using fluorescence-based plate readers or imaging systems. These assays allow for the quantification of the compound's inhibitory potency (pEC50 or IC50) and its selectivity profile against other TRP channels.
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| Animal Protocol |
In vivo animal studies for AMTB HCl have been conducted in rat models to evaluate its effects on visceral pain and urinary function. In these studies, AMTB is typically administered systemically (e.g., 10 mg/kg), and reflex responses to noxious urinary bladder distension (UBD) are measured. Endpoints include the visceromotor reflex (VMR) response and pressor response, which are quantified as a percentage of the maximal response. These studies demonstrate the compound's in vivo efficacy in modulating TRPM8-mediated pathways.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for AMTB HCl are not extensively detailed in the available literature. As a small molecule antagonist, its pharmacokinetic properties are important for its in vivo efficacy. The compound is typically administered via injection in animal studies. Its pharmacokinetic profile, including parameters such as half-life and bioavailability, would be critical for its development as a therapeutic agent. However, these data are not provided in the search results.
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| Toxicity/Toxicokinetics |
Specific toxicity data for AMTB HCl are not extensively detailed in the available literature. As a research compound, its toxicity profile is not the primary focus of investigation. However, its use in animal models at doses such as 10 mg/kg suggests a manageable safety profile. Comprehensive toxicological studies would be required to establish its safety for therapeutic use. It is intended for research purposes only and is not for human use.
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| References |
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| Additional Infomation |
AMTB HCl is a selective TRPM8 channel blocker with a pEC50 of 6.91 in calcium influx assays and no activity against TRPV4 (pEC50<4.6). It inhibits icilin-induced calcium influx with an IC50 of 0.58 µM. In vivo, it attenuates reflex responses to noxious urinary bladder distension in rats. It is a research compound for studying pain, urinary diseases, and TRPM8 channel function. It is not approved for clinical use.
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| Molecular Formula |
C23H27CLN2O2S
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|---|---|
| Molecular Weight |
430.990683794022
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| Exact Mass |
430.148
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| CAS # |
926023-82-7
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| PubChem CID |
16095383
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| Appearance |
White to off-white solid powder
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| LogP |
6.129
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
29
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| Complexity |
476
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=CC=C1)COC2=CC=CC=C2C(=O)N(CCCN)CC3=CC=CS3.Cl
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| InChi Key |
UDXGBANGPYONOK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H26N2O2S.ClH/c1-18-7-4-8-19(15-18)17-27-22-11-3-2-10-21(22)23(26)25(13-6-12-24)16-20-9-5-14-28-20/h2-5,7-11,14-15H,6,12-13,16-17,24H2,1H31H
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| Chemical Name |
N-(3-Aminopropyl)-2-{[(3-methylphenyl) methyl]oxy}-N-(2-thienylmethyl)benzamide hydrochloride
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| Synonyms |
AMTB.
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~232.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.80 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 25.0 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: 2.5 mg/mL (5.80 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.80 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 | 2.3202 mL | 11.6012 mL | 23.2024 mL | |
| 5 mM | 0.4640 mL | 2.3202 mL | 4.6405 mL | |
| 10 mM | 0.2320 mL | 1.1601 mL | 2.3202 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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