| CapsazepineTRPV1 ion channel activator |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.02%
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| Cas No. | 138977-28-3 | SDF | Download SDF |
| Chemical Name | N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-1,3,4,5-tetrahydro-2-benzazepine-2-carbothioamide | ||
| Canonical SMILES | C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O | ||
| Formula | C19H21ClN2O2S | M.Wt | 376.9 |
| Solubility | ≥22 mg/mL in DMSO with gentle warming, ≥18.85 mg/mL in EtOH with gentle warming, <2.58 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Capsazepine is a competitive antagonist of vanilloid (capsaicin) receptor with IC50 value of 562 nM.[1]
Capsazepine is a synthetic analogue of capsaicin, which activates the TRPV1 ion channel, thereby, blocks the painful sensation of heat caused by capsaicin. Capsazepine blocked voltage-activated calcium currents in adult rat dorsal root ganglion neurons with EC50 value of 7.7±1.4 μM.[2] Capsazepine was also able to block the response of TRPM8 to menthol (IC50=18±1.1 μM).[3] Capsazepine also inhibited nicotinic acetylcholine receptors in rat trigeminal ganglia at 10μM.[4] In human colon cancer cells, capsazepine treatment activated caspase -8, –9, and -3, induced death receptors (DRs) DR5 and DR4, then sensitized the cells to TRAIL-induced apoptosis.[5] Capsazepine is thought to be a tool to study the TRPV1 ion channel.
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