AMTB HCl is a novel and potent TRPM8 channel blocker effective for pain and urinary diseases. For rats, AMTB (10 mg/kg) significantly attenuated reflex responses to noxious urinary bladder distension (UBD) to 5.42 and 56.51% of the maximal visceromotor reflex (VMR) response and pressor response, respectively. The ID50 value on VMR response was 2.42 +/- 0.46 mg/kg. AMTB can act on the bladder afferent pathway to attenuate the bladder micturition reflex and nociceptive reflex responses in the rat.

Physicochemical Properties

Molecular Formula	C23H27CLN2O2S
Molecular Weight	430.990683794022
Exact Mass	430.148
CAS #	926023-82-7
PubChem CID	16095383
Appearance	White to off-white solid powder
LogP	6.129
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	9
Heavy Atom Count	29
Complexity	476
Defined Atom Stereocenter Count	0
InChi Key	UDXGBANGPYONOK-UHFFFAOYSA-N
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
Chemical Name	N-(3-Aminopropyl)-2-{[(3-methylphenyl) methyl]oxy}-N-(2-thienylmethyl)benzamide hydrochloride
Synonyms	AMTB.
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 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)

Biological Activity

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].
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].
References	[1]. AMTB, a TRPM8 channel blocker: evidence in rats for activity in overactive bladder and painful bladder syndrome. Am J Physiol Renal Physiol. 2008;295(3):F803-F810. [2]. Assessment of the TRPM8 inhibitor AMTB in breast cancer cells and its identification as an inhibitor of voltage gated sodium channels. Life Sci. 2018;198:128-135.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~232.02 mM)

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. 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. 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 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	2.3202 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.