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Capsazepine - 98%, high purity , CAS No.138977-28-3, Channel blocker of TRPM8;Channel blocker of TRPV1

  • Moligand™
  • ≥98%
Item Number
C126558
Grouped product items
SKUSizeAvailabilityPrice Qty
C126558-5mg
5mg
In stock
$56.90
C126558-10mg
10mg
In stock
$93.90
C126558-25mg
25mg
In stock
$211.90
C126558-50mg
50mg
In stock
$281.90
C126558-100mg
100mg
In stock
$450.90
C126558-250mg
250mg
In stock
$1,014.90

VR1 antagonist

Basic Description

Synonymscapsazepine|138977-28-3|N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide|capasazepine|capsazepin|N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-1,3,4,5-tetrahydro-2-benzazepine-2-carbothioamide|CHEMBL391997|LFW48MY
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsCapsazepine is a specific vanilloid receptor antagonist; synthetic analog of capsaicin.VR1 vanilloid receptor antagonist (IC 50 = 562 nM). Analgesic in vivo .
Storage TempStore at 2-8°C
Shipped InWet ice
GradeMoligand™
Action TypeCHANNEL BLOCKER
Mechanism of actionChannel blocker of TRPM8;Channel blocker of TRPV1
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, capsaicin; potent TRPV1 receptor antagonist with IC50 of 562 nM.
An antagonist of TRPV1 and activator of ENaC

Associated Targets

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C19 Tchem Cytochrome P450 2C19 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DRD1 Tclin D(1A) dopamine receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

POLB Tchem DNA polymerase beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EHMT2 Tchem Histone-lysine N-methyltransferase EHMT2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DUPD1 Tbio Dual specificity phosphatase DUPD1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CBX1 Tbio Chromobox protein homolog 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GMNN Tbio Geminin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RUNX1 Tbio Runt-related transcription factor 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RORC Tchem Nuclear receptor ROR-gamma 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

USP1 Tchem Ubiquitin carboxyl-terminal hydrolase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FTL Tbio Ferritin light chain 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HIF1A Tchem Hypoxia-inducible factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HSD17B10 Tchem 3-hydroxyacyl-CoA dehydrogenase type-2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KMT2A Tchem Histone-lysine N-methyltransferase 2A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FEN1 Tchem Flap endonuclease 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

THPO Tbio Thrombopoietin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TXNRD1 Tclin Thioredoxin reductase 1, cytoplasmic 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPV1 Tclin Transient receptor potential cation channel subfamily V member 1 23 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPA1 Tclin Transient receptor potential cation channel subfamily A member 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TSHR Tclin Thyrotropin receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HPGD Tchem 15-hydroxyprostaglandin dehydrogenase [NAD(+)] 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RGS4 Tchem Regulator of G-protein signaling 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ALOX12 Tchem Arachidonate 12-lipoxygenase, 12S-type 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

L3MBTL1 Tchem Lethal(3)malignant brain tumor-like protein 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

LMNA Tbio Prelamin-A/C 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ALOX15B Tchem Arachidonate 15-lipoxygenase B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ALOX15 Tchem Arachidonate 15-lipoxygenase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MPHOSPH8 Tbio M-phase phosphoprotein 8 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BLM Tchem Bloom syndrome protein 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BAZ2B Tchem Bromodomain adjacent to zinc finger domain protein 2B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPM8 Tclin Transient receptor potential cation channel subfamily M member 8 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TDP1 Tchem Tyrosyl-DNA phosphodiesterase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

APEX1 Tchem DNA-(apurinic or apyrimidinic site) lyase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ALDH1A1 Tchem Retinal dehydrogenase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPT Tclin Microtubule-associated protein tau 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GLS Tchem Glutaminase kidney isoform, mitochondrial 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

IDH1 Tclin Isocitrate dehydrogenase [NADP] cytoplasmic 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NPSR1 Tchem Neuropeptide S receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KDM4A Tchem Lysine-specific demethylase 4A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KDM4E Tchem Lysine-specific demethylase 4E 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

NFKB1 Tclin Nuclear factor NF-kappa-B p105 subunit 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Pubchem Sid488192405
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488192405
IUPAC Name N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-1,3,4,5-tetrahydro-2-benzazepine-2-carbothioamide
INCHI InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25)
InChi Key DRCMAZOSEIMCHM-UHFFFAOYSA-N
Canonical SMILES C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O
Isomeric SMILES C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O
WGK Germany 3
PubChem CID 2733484
Molecular Weight 376.9

Certificates

Certificate of Analysis(COA)

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20 results found

Lot NumberCertificate TypeDateItem
C2219280Certificate of AnalysisJan 04, 2024 C126558
H2330227Certificate of AnalysisJun 30, 2023 C126558
H2330182Certificate of AnalysisJun 30, 2023 C126558
H2330181Certificate of AnalysisJun 30, 2023 C126558
H2330180Certificate of AnalysisJun 30, 2023 C126558
E2306160Certificate of AnalysisMar 30, 2023 C126558
E2306167Certificate of AnalysisMar 30, 2023 C126558
E2306166Certificate of AnalysisMar 30, 2023 C126558
E2306165Certificate of AnalysisMar 30, 2023 C126558
E2306163Certificate of AnalysisMar 30, 2023 C126558
E2306162Certificate of AnalysisMar 30, 2023 C126558
E2306159Certificate of AnalysisMar 30, 2023 C126558
E2306157Certificate of AnalysisMar 30, 2023 C126558
E2306155Certificate of AnalysisMar 30, 2023 C126558
E2306154Certificate of AnalysisMar 30, 2023 C126558
E2306152Certificate of AnalysisMar 30, 2023 C126558
E2306151Certificate of AnalysisMar 30, 2023 C126558
A1908149Certificate of AnalysisSep 13, 2022 C126558
A2213055Certificate of AnalysisJan 26, 2022 C126558
C2219278Certificate of AnalysisDec 28, 2021 C126558

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Chemical and Physical Properties

Solubility25°C: DMSO
Refractive Index1.67
Boil Point(°C)581.13° C at 760 mmHg
Melt Point(°C)159-161°C

Safety and Hazards(GHS)

WGK Germany 3

Related Documents

References

1. Ryskamp DA, Witkovsky P, Barabas P, Huang W, Koehler C, Akimov NP, Lee SH, Chauhan S, Xing W, Rentería RC et al..  (2011)  The polymodal ion channel transient receptor potential vanilloid 4 modulates calcium flux, spiking rate, and apoptosis of mouse retinal ganglion cells..  J Neurosci,  31  (19): (7089-101).  [PMID:21562271]
2. Cahusac PM & Noyce R.  (2007)  A pharmacological study of slowly adapting mechanoreceptors responsive to cold thermal stimulation..  Neuroscience,  148  (2): (489-500).  [PMID:17683869]
3. Adinolfi B et al..  (2013)  Anticancer activity of anandamide in human cutaneous melanoma cells..  Eur J Pharmacol,  718  (1-3): (154-9).  [PMID:24041928]
4. Landucci E et al..  (2011)  CB1 receptors and post-ischemic brain damage: studies on the toxic and neuroprotective effects of cannabinoids in rat organotypic hippocampal slices..  Neuropharmacology,  60  (4): (674-82).  [PMID:21130785]
5. Yan J et al..  (2011)  Dural afferents express acid-sensing ion channels: a role for decreased meningeal pH in migraine headache..  Pain,  152  (106-13).  [PMID:20971560]
6. de Man JG et al..  (2008)  Functional study on TRPV1-mediated signalling in the mouse small intestine: involvement of tachykinin receptors..  Neurogastroenterol Motil,  20  (5): (546-56).  [PMID:18194153]
7. De Schepper HU et al..  (2008)  TRPV1 receptor signaling mediates afferent nerve sensitization during colitis-induced motility disorders in rats..  Am J Physiol Gastrointest Liver Physiol,  294  (G245-53).  [PMID:17991707]

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