A TRPM8 antagonist
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AMTB

Item No. 25336

Technical Information
Formal Name
N-(3-aminopropyl)-2-[(3-methylphenyl)methoxy]-N-(2-thienylmethyl)-benzamide, monohydrochloride
CAS Number
926023-82-7
Molecular Formula
C23H26N2O2S • HCl
Formula Weight
Purity
≥98%
Formulation
A solid
DMSO: 100 mMWater: 100 mM
SMILES
O=C(N(CCCN)CC1=CC=CS1)C2=CC=CC=C2OCC3=CC(C)=CC=C3.Cl
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,6,12-13,16-17,24H2,1H3;1H
InChi Key
UDXGBANGPYONOK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    AMTB is an antagonist of transient receptor potential melastatin 8 (TRPM8).1 It inhibits calcium influx induced by the TRPM8 agonist icilin (Item No. 10137) with an IC50 value of 0.58 µM. AMTB (3 mg/kg) decreases the number of volume-induced bladder contractions in a rat model of noxious bladder distension. It also decreases the visceromotor reflex response to urinary bladder distension (ID50 = 2.42 mg/kg), indicating antinociceptive activity. AMTB inhibits the sodium channel (Nav) isoforms Nav1.1-1.8 (IC50s = 2-14.8 µM) and decreases viability of MDA-MB-231 and SK-BR-3 breast cancer cells (IC50s = ~23.7 and 17.3 µM, respectively) in a TRPM8-independent manner.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lashinger, E.S.R., Steiginga, M.S., Hieble, J.P., et alAMTB, a TRPM8 channel blocker: Evidence in rats for activity in overactive bladder and painful bladder syndrome. Am. J. Physiol. Renal Physiol. 295(3), F803-F810 (2008).

    2. Yapa, K.T.D.S., Deuis, J., Peters, A.A., et alAssessment of the TRPM8 inhibitor AMTB in breast cancer cells and its identification as an inhibitor of voltage gated sodium channels. Life Sci. 198, 128-135 (2018).