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辣椒平, TRPM8 通道阻断剂;TRPV1 通道阻断剂

VR1拮抗剂
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货号 (SKU) 包装规格 是否现货 价格 数量
C126558-5mg
 5mg 现货 Stock Image
C126558-10mg
 10mg 现货 Stock Image
C126558-25mg
 25mg 现货 Stock Image
C126558-50mg
 50mg 现货 Stock Image
C126558-100mg
 100mg 期货 Stock Image
C126558-250mg
 250mg 现货 Stock Image
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Apoptosis (7108) TRP Channel (182) TRPM8 Channel blocker (15) TRPV1 Channel blocker (18) 神经元信号传导 (3320) 离子通道 (4087) 膜转运器/离子通道 (1829)
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基本描述

别名 辣椒平 | N-[2-(4-氯苯基)乙基]-1,3,4,5-四氢-7,8-二羟基-2H-2-苯并氮杂卓-2-硫代甲酰胺
英文别名 NCGC00015190-06 | ST50826300 | N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide | NCGC00015190-01 | SR-01000075437-1 | Tox21_500373 | BDBM20284 | HY-15640 | NCGC00015190-14 | Bio1_000883 | SMR001230854 | Tocri
规格或纯度 Moligand™, ≥98%
英文名称 Capsazepine
生化机理 辣椒素是一种特异性类香草素受体拮抗剂；是辣椒素的合成类似物，是 VR1 类香草素受体拮抗剂（IC 50 = 562 nM）。在体内具有镇痛作用。
储存温度 2-8°C储存
运输条件 冰袋运输
作用类型 通道阻滞剂
作用机制 TRPM8 通道阻断剂;TRPV1 通道阻断剂
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍

Capsazepine是TRPV1受体拮抗剂，IC50为562 nM。An antagonist of TRPV1 and activator of ENaC

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
纯度 ≥98%

关联靶点（人）

CYP2C19 Tchem 细胞色素 P450 2C19(Cytochrome P450 2C19) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
TRPV1 Tclin 瞬时受体电位阳离子通道亚家族V成员1(Transient receptor potential cation channel subfamily V member 1) (23 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
TRPM8 Tclin 瞬时受体电位阳离子通道亚家族M成员8(Transient receptor potential cation channel subfamily M member 8) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
TSHR Tclin Thyroid stimulating hormone receptor (29986 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
POLB Tchem DNA polymerase beta (23632 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TRPV1 Tclin Vanilloid receptor (8273 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ARSA Tbio Cerebroside-sulfatase (655 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ALOX15B Tchem Arachidonate 15-lipoxygenase, type II (7244 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ALDH1A1 Tchem Aldehyde dehydrogenase 1A1 (77053 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ALOX12 Tchem Arachidonate 12-lipoxygenase (3262 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NFKB1 Tclin Nuclear factor NF-kappa-B p105 subunit (1459 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ALOX15 Tchem Arachidonate 15-lipoxygenase (7108 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
U2OS (164939 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HEK293 (82097 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HepG2 (196354 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HeLa (62764 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FEN1 Tchem Flap endonuclease 1 (12055 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HIF1A Tchem Hypoxia-inducible factor 1 alpha (6027 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HSD17B10 Tchem Endoplasmic reticulum-associated amyloid beta-peptide-binding protein (20669 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KDM4A Tchem Lysine-specific demethylase 4A (52245 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
APEX1 Tchem DNA-(apurinic or apyrimidinic site) lyase (38016 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EHMT2 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (93046 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TDP1 Tchem Tyrosyl-DNA phosphodiesterase 1 (345557 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
L3MBTL1 Tchem Lethal(3)malignant brain tumor-like protein 1 (14536 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KDM4E Tchem Lysine-specific demethylase 4D-like (40243 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
LMNA Tbio Prelamin-A/C (36751 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BLM Tchem Bloom syndrome protein (4248 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HPGD Tchem 15-hydroxyprostaglandin dehydrogenase [NAD+] (24926 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
THPO Tbio Thrombopoietin (834 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GMNN Tbio Geminin (128009 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CBX1 Tbio Chromobox protein homolog 1 (92434 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ATAD5 Tbio ATPase family AAA domain-containing protein 5 (122566 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MPHOSPH8 Tbio M-phase phosphoprotein 8 (656 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
BAZ2B Tchem Bromodomain adjacent to zinc finger domain protein 2B (56204 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ATXN2 Tbio Ataxin-2 (54410 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
USP1 Tchem Ubiquitin carboxyl-terminal hydrolase 1 (22556 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RGS4 Tchem Regulator of G-protein signaling 4 (13867 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IDH1 Tclin Isocitrate dehydrogenase [NADP] cytoplasmic (40980 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MEN1 Tchem Menin/Histone-lysine N-methyltransferase MLL (48157 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
RUNX1 Tbio Runt-related transcription factor 1/Core-binding factor subunit beta (7867 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GLS Tchem Glutaminase kidney isoform, mitochondrial (16997 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TARDBP Tchem TAR DNA-binding protein 43 (40113 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HEK-293T (167025 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

ampC Beta-lactamase AmpC (62480 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Saccharomyces cerevisiae (19171 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasmodium falciparum (966862 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cavia porcellus (23802 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
lef Anthrax lethal factor (7585 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Npsr1 Neuropeptide S receptor (260 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Trpa1 Transient receptor potential cation channel subfamily A member 1 (1003 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Trpm8 Transient receptor potential cation channel subfamily M member 8 (889 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
pfk 6-phospho-1-fructokinase (7870 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Txnrd1 Thioredoxin reductase 1, cytoplasmic (45279 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ddn Putative uncharacterized protein (49 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TGR Thioredoxin glutathione reductase (28579 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapt Microtubule-associated protein tau (6 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rorc Nuclear receptor ROR-gamma (89407 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
fba Putative fructose-1,6-bisphosphate aldolase (15559 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ffp 4'-phosphopantetheinyl transferase ffp (24982 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
FTL Ferritin light chain (43324 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
nfo Endonuclease 4 (425 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 488192405
分子类型 小分子
IIUPAC Name N-[2-(4-chlorophenyl)ethyl]-7,8-dihydroxy-1,3,4,5-tetrahydro-2-benzazepine-2-carbothioamide
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
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
分子量 376.9
Reaxy-Rn 7047754
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7047754&ln=

化学和物理性质

溶解性 25°C: DMSO
密度 1.35
折光率 1.67
沸点 581.13° C at 760 mmHg
熔点 159-161°C
分子量 376.900 g/mol
XLogP3 3.900
氢键供体数Hydrogen Bond Donor Count 3
氢键受体数Hydrogen Bond Acceptor Count 3
可旋转键计数Rotatable Bond Count 3
精确质量Exact Mass 376.101 Da
单同位素质量Monoisotopic Mass 376.101 Da
拓扑极表面积Topological Polar Surface Area 87.800 Ų
重原子数Heavy Atom Count 25
形式电荷Formal Charge 0
复杂度Complexity 445.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性（GHS）

WGK Germany 3
个人防护装备 Eyeshields， Gloves， type N95 (US)， type P1 (EN143) respirator filter

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批号(Lot Number) 证书类型 货号
C2219280 分析证书 C126558
H2330180 分析证书 C126558
H2330182 分析证书 C126558
H2330227 分析证书 C126558
E2306160 分析证书 C126558
E2306163 分析证书 C126558
E2306166 分析证书 C126558
E2306167 分析证书 C126558
E2306159 分析证书 C126558
E2306151 分析证书 C126558
E2306154 分析证书 C126558
E2306155 分析证书 C126558
E2306157 分析证书 C126558
H2330181 分析证书 C126558
E2306162 分析证书 C126558
E2306165 分析证书 C126558
E2306152 分析证书 C126558
A1908149 分析证书 C126558
A2213055 分析证书 C126558
C2219278 分析证书 C126558

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引用文献

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]
8. Qin Yeyu, Xie Jing, Zheng Ruihe, Li Yuhang, Wang Haixia.  (2022)  Oleoylethanolamide as a New Therapeutic Strategy to Alleviate Doxorubicin-Induced Cardiotoxicity.  Frontiers in Pharmacology,  13  [PMID:35517792] [10.3389/fphar.2022.863322]
9. Di Wu, Ran Duan, Lan Tang, Dian Zhou, Zhen Zeng, Wen Wu, Jie Hu, Qiaomei Sun.  (2022)  In-vitro binding analysis and inhibitory effect of capsaicin on lipase.  LWT-FOOD SCIENCE AND TECHNOLOGY,  154  (112674).  [10.1016/j.lwt.2021.112674]
10. Kaiwen Lin, Zhongtao Wang, Erhao Wang, Xueer Zhang, Xiaofei Liu, Faming Feng, Xiaodan Yu, Guohui Yi, Yan Wang.  (2024)  Targeting TRPV1 signaling: Galangin improves ethanol-induced gastric mucosal injury.  JOURNAL OF ETHNOPHARMACOLOGY,  335  (118605).  [PMID:39047882] [10.1016/j.jep.2024.118605]

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