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Search Results for " capsaicin "

32

抑制剂 & 化合物

13

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1109	(Z)-Capsaicin Zucapsaicin,Civamide,cis-Capsaicin,珠卡赛辛,(Z)-辣椒素	TRP/TRPV Channel; HSV	Membrane transporter/Ion channel; Microbiology/Virology
	(Z)-Capsaicin (Zucapsaicin) 是天然辣椒素的合成顺式异构体，用于治疗膝骨关节炎。它是一种可口服的 TRPV1激动剂，可研究神经性疼痛。
T16014	Mavatrep JNJ-39439335	TRP/TRPV Channel	Membrane transporter/Ion channel
	Mavatrep (JNJ-39439335) 是一种特异性的 TRPV1 拮抗剂，Ki 为 6.5 nM，可用于炎症性疼痛的研究。
T23322	SB 452533	TRP/TRPV Channel	Membrane transporter/Ion channel
	SB 452533 是TRPV1的选择性拮抗剂，pKb 为 7.8。
T39349	Vocacapsaicin hydrochloride CA-008 hydrochloride	TRP/TRPV Channel	Membrane transporter/Ion channel
	Vocacapsaicin hydrochloride (CA-008 hydrochloride) 是非阿片类 TRPV1 激动剂，是辣椒素的原料，可用于缓解疼痛。
T39348	Vocacapsaicin CA-008,Vocacapsaicin
	Vocacapsaicin (CA-008), a prodrug of Capsaicin and a first-in-class non-opioid TRPV1 agonist, offers significant and enduring pain relief.
T29522L	(S)-ABT 102	TRP/TRPV Channel	Membrane transporter/Ion channel
	N-[(1S)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea 是一种有效的TRPV1拮抗剂，其IC50为123 nM，可阻断capsaicin 对TRPV1的激活。
T6379	AMG 517 AMG517,N-[4-[[6-[4-(三氟甲基)苯基]-4-嘧啶基]氧基]-2-苯并噻唑基]乙酰胺,AMG-517	TRP/TRPV Channel	Membrane transporter/Ion channel
	AMG 517是一种有效的香草素受体-1 (TRPV1) 拮抗剂，IC50为0.5 nM。
T7102	BCTC N-(4-叔丁苯基)-4-(3-氯吡啶-2-基)哌嗪-1-甲酰胺	TRP/TRPV Channel	Membrane transporter/Ion channel
	BCTC 是有效的、特异性的瞬时受体阳离子通道M8(TRPM8)抑制剂。
T1356	4-Hydroxy-3-methoxybenzylamine hydrochloride 香兰素胺盐酸盐,N-Vanillylamine hydrochloride	Others	Others
	4-Hydroxy-3-methoxybenzylamine hydrochloride (N-Vanillylamine hydrochloride) 是一种生物碱，是capsaicin 生物合成的中间体。
T7189	AMG9810 (2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺	TRP/TRPV Channel	Membrane transporter/Ion channel
	AMG9810是高效的，竞争性的香草素受体1选择性拮抗剂，对人类和大鼠TRPV1的IC50分别为24.5 和 85.6 nM。
T4431	Olodanrigan PD-126055,EMA401	RAAS	Endocrinology/Hormones
	Olodanrigan (EMA401) 是具有口服活性、高选择性及外周受限的血管紧张素 Ⅱ 类型 2 受体(AT2R)拮抗剂。它的缓解疼痛的机制可能是：抑制增强的 AngII/AT2R 诱导的 p38 和 p42/p44 MAPK 激活，进而阻碍 DRG 神经元的过度兴奋性及 DRG 神经元的萌发。它可用于研究神经性疼痛。
T37610	AT-121	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	AT-121 是一种双重μ-阿片和神经肽受体部分激动剂（Kis 分别为 16.49 和 3.67 nM）。它能刺激[35S]GTPγS 与表达μ-阿片受体或神经肽受体的细胞膜结合（EC50s 分别为 19.6 和 34.7 nM）。AT-121（0.003-0.03 mg/kg）能以剂量依赖的方式降低辣椒素诱导的热异感，但不会增加恒河猴的搔抓活动。在恒河猴药物自我给药试验中，AT-121 每次注射剂量为 0.3 至 10 μg/kg，它缺乏强化作用（一种潜在的滥用标志），不能减少食物颗粒的强化作用。AT-121（0.01 或 0.03 毫克/千克）不会诱发恒河猴的超痛觉，超痛觉是产生耐受性的标志。AT-121 是一种安全、无成瘾性的缓解疼痛药，具有抗伤害和止痛作用。
T37668	CAY10448 CAY10448
	Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Capsaicin signals are transduced by a heat-activated ion channel, the vanilloid receptor 1 (VR1), or transient receptor potential vanilloid 1 (TRPV1). CAY10448 is an iodinated nonivamide, a potent capsaicin receptor antagonist with an IC50 value of approximately 10 nM.
T38277	8-methyl Nonanoic Acid 8-methyl Nonanoic Acid,Isocapric Acid
	Capsaicin, the chemical that imparts the spicy-hot quality of chili peppers, is produced by the fruits of plants belonging to the Capsicum family. 8-methyl Nonanoic acid is an immediate precursor of capsaicin as well as a by-product of capsaicin degradation.[1] Addition of 5 mM of 8-methyl nonanoic acid significantly increases the yield of capsaicin in both immobilized and freely suspended cells of C. frutescens. [2] Capsaicin has reported antimicrobial properties, however isocapric acid can ac...
T74742	TRPV1 activator-2
	TRPV1 activator-2 (compound 9)为辣椒素类似物，特异性与脂-水通道残基相互作用。
T68271	AZD1386
	AZD1386 is a TRPV1 antagonist. AZD1386 acts as a competitive antagonist at the channel's capsaicin binding site.
T23944	DA 5018 DA-5018,DA5018
	DA 5018 is a capsaicin derivative and is also a new non-narcotic analgesic. It has an antipruritic effect.
T37732	AMG 21629
	Potent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant. Tamayo et al (2008) Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. J.Med.Chem. 51 2744 PMID:18386885 \|Gavva et al...
T74741	TRPV1 activator-1
	TRPV1 activator-1 (compound 8)，一种颈部结构经过改变的辣椒素类似物，特异性与T551残基相互作用。
T37086	PDDHV
	PDDHV is a resiniferatoxin-type phorboid vanilloid with capsaicin-like selectivity for the cloned rat transient receptor potential cation channel subfamily V member 1 (TRPV1), formerly known as vanilloid receptor 1. It induces Ca2+-uptake by rat dorsal root ganglion neurons with an EC50 value of 70 nM.
T61788	TRPV1 antagonist 3
	TRPV1 antagonist 3 (Compound 7q) is a highly potent antagonist of the TRPV1 receptor with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity towards its mode of action and is orally bioavailable (with a bioavailability of 60%). Additionally, it can penetrate the central nervous system [1].
T68904	GW-833972A free base
	GW833972 is a CB2 Agonist. GW 833972A inhibited capsaicin-induced depolarization of the human and guinea-pig and prostaglandin E(2) (PGE(2)) and hypertonic saline-induced depolarization of the guinea-pig isolated vagus nerve in vitro. GW 833972A also inhibited citric acid-induced cough but not plasma extravasation in the guinea-pig and this effect was blocked by a CB(2) receptor antagonist.
T21750	A 784168
	A-784168 是一种有效的、口服活性的香草素受体 1 型 (TRPV1) 抑制剂。香草素受体 1 型 (TRPV1) 是一种配体门控非选择性阳离子通道，被认为是各种疼痛刺激 (如内源性脂质、辣椒素、热和低 pH 值) 的重要整合剂。口服给药时，A-784168 具有良好的 CNS 渗透性。
T81787	MitTx-beta
	MitTx-beta为一多肽，源自得克萨斯珊瑚蛇(Micrurus tener tener)之毒液。与MitTx-α配对，组成复合物MitTx，此复合物激活ASIC1通道，存在于辣椒素敏感神经纤维上。
T33789	Oleoyl proline N-Oleoyl-l-proline
	Oleoyl proline is an N-acyl amine that can be detected in bovine brain extracts and D. melanogaster larvae using mass spectrometry. In a preclinical model of pain, mice lacking fatty acid amide hydrolase (FAAH KO) had decreased N-oleoyl proline levels in
T37670	CAY10568
	Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported. CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists sh...
T36101	Psychotridine
	Psychotridine is an alkaloid that has been found inP. forsterianaand has diverse biological activities.1,2,3It inhibits ADP-, collagen-, or thrombin-induced aggregation of washed isolated human platelets with IC50values of 1.4, 1.4, and 3.9 μM, respectively.1Psychotridine (2.5 or 5 μM) is cytotoxic to HTC rat hepatocellular carcinoma cells.2It reduces paw licking induced by capsaicin in mice when administered at doses of 0.5, 2.5, or 5 mg/kg.3 1.Beretz, A., Roth-Georger, A., Corre, G., et al.Pol...
T36064	N-Oleoyl Glutamine
	N-Oleoyl glutamine is an endogenous N-acyl amine.1,2It is both formed and degraded by peptidase M20 domain-containing 1 (PM20D1), a factor secreted by thermogenic adipose cells. N-Oleoyl glutamine (50 μM) induces mitochondrial uncoupling to increase respiration in C2C12 cells by 64%.3It inhibits capsaicin-induced calcium flux in HEK293A cells co-transfected with transient receptor potential vanilloid 1 (TRPV1) and red fluorescent protein (RFP).2N-Oleoyl glutamine (100 mg/kg) reduces the number o...
T37167	Reduced Haloperidol
	Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing ...
T78734	Sigma-1 receptor antagonist 5	Sigma receptor	GPCR/G Protein
	Sigma-1 receptor antagonist 5 (compound 12) 是一种 4-吡啶衍生物，既有镇痛活性也是 sigma 受体 (Ki=4.5 nM (σ1R)，10 nM (σ2R)) 及组胺 H3 (hH3R，Ki=7.7 nM，IC50=215 nM) 的拮抗剂。它能够抑制辣椒素引起的痛觉，并展现出对伤害性和神经性疼痛模型的显著疗效。
T71141	Fenspiride-d5
	Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from ...
T83732	Tat-CBD3A6K TFA
	Tat-CBD3A6K是一种肽类化合物，为N型电压门控钙通道Cav2.2以及collapsin response mediator protein 2 (CRMP2) 蛋白-蛋白相互作用抑制剂Tat-CBD3的衍生物。Tat-CBD3A6K (10 mg/kg) 能够阻止由d4T (stavudine)引发的大鼠抗逆转录病毒神经病痛模型中爪撤回阈值的下降，并减少同一大鼠分离的背根神经节(DRG)神经元的动作电位数量。通过硬膜途径给予Tat-CBD3A6K (30 µM/animal) 能够减少由萜类生物碱辣椒素引发的大鼠硬脑膜血流增加。

化合物

(Z)-Capsaicin

Cat.No: T1109

Synonym: Zucapsaicin,Civamide,cis-Capsaicin,珠卡赛辛,(Z)-辣椒素

Target: TRP/TRPV Channel, HSV

Cat.No: T16014

Synonym: JNJ-39439335

Target: TRP/TRPV Channel

Cat.No: T23322

Target: TRP/TRPV Channel

Vocacapsaicin hydrochloride

Cat.No: T39349

Synonym: CA-008 hydrochloride

Target: TRP/TRPV Channel

Cat.No: T39348

Synonym: CA-008,Vocacapsaicin

Cat.No: T29522L

Target: TRP/TRPV Channel

Cat.No: T6379

Synonym: AMG517,N-[4-[[6-[4-(三氟甲基)苯基]-4-嘧啶基]氧基]-2-苯并噻唑基]乙酰胺,AMG-517

Target: TRP/TRPV Channel

Cat.No: T7102

Synonym: N-(4-叔丁苯基)-4-(3-氯吡啶-2-基)哌嗪-1-甲酰胺

Target: TRP/TRPV Channel

4-Hydroxy-3-methoxybenzylamine hydrochloride

Cat.No: T1356

Synonym: 香兰素胺盐酸盐,N-Vanillylamine hydrochloride

Target: Others

Cat.No: T7189

Synonym: (2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺

Target: TRP/TRPV Channel

Cat.No: T4431

Synonym: PD-126055,EMA401

Target: RAAS

Cat.No: T37610

Target: Opioid Receptor

Cat.No: T37668

Synonym: CAY10448

8-methyl Nonanoic Acid

Cat.No: T38277

Synonym: 8-methyl Nonanoic Acid,Isocapric Acid

TRPV1 activator-2

Cat.No: T74742

Cat.No: T68271

Cat.No: T23944

Synonym: DA-5018,DA5018

Cat.No: T37732

TRPV1 activator-1

Cat.No: T74741

Cat.No: T37086

TRPV1 antagonist 3

Cat.No: T61788

GW-833972A free base

Cat.No: T68904

Cat.No: T21750

Cat.No: T81787

Cat.No: T33789

Synonym: N-Oleoyl-l-proline

Cat.No: T37670

Cat.No: T36101

N-Oleoyl Glutamine

Cat.No: T36064

Reduced Haloperidol

Cat.No: T37167

Sigma-1 receptor antagonist 5

Cat.No: T78734

Target: Sigma receptor

Cat.No: T71141

Tat-CBD3A6K TFA

Cat.No: T83732

Cat. No.	Product Name	Target	Signaling Pathways
T1062	Capsaicin Qutenza,8-Methyl-N-vanillyl-trans-6-nonenamide,天然辣椒素,Vanilloid,辣椒素,(E)-Capsaicin,Zostrix	Apoptosis; TRP/TRPV Channel; Autophagy	Apoptosis; Autophagy; Membrane transporter/Ion channel
	Capsaicin ((E)-Capsaicin) 属于天然产物，提取自辣椒，是一种 TRPV1 激动剂 (EC50=0.29 μM)。Capsaicin 具有抗肿瘤、抗炎、抗氧化、神经保护等活性。
T39018	Capsaicin β-D-glucopyranoside
	Capsaicin β-D-glucopyranoside, a glucoside converted by Capsaicin, is the bioactive compound found in chili peppers responsible for their characteristic pungent flavor.
T3421	Nordihydrocapsaicin	Others	Others
	Nordihydrocapsaicin is an analog and congener of capsaicin, belonging to the capsaicinoid class of compounds found in Capsicum chili peppers.
T2163	Dihydrocapsaicin CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide	Others; TRP/TRPV Channel	Membrane transporter/Ion channel; Others
	Dihydrocapsaicin (CCRIS1589) 是一种天然来源的辣椒素，是TRPV1的选择性激动剂，同时可以增加 p-Akt 水平。它可以增强低温诱导的神经保护。
TN1739	Homodihydrocapsaicin I 高二氢辣椒素,高二氢辣椒素I	Others	Others
	Homodihydrocapsaicin I 是一种辣椒素，分离自辣椒果实中。
T82187	Homocapsaicin II
	Homocapsaicin II, 提取自Capsicum annuum L果实，为一种辣椒素类化合物。
T5S1389	Escin IB 七叶皂苷B,七叶皂苷 IB	5-HT Receptor; NO Synthase	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Escin IB 是一种皂苷，分离自马栗子种子的皮和胚乳中，能够抑制 pancreatic lipase 的活性。
T7177	Capsazepine	Apoptosis; TRP/TRPV Channel	Apoptosis; Membrane transporter/Ion channel
	Capsazepine 是一种 TRPV1 受体的拮抗剂， IC50值为 562 nM。它可阻断由激活 TRPV1 离子通道的辣椒素引起的热痛感，是辣椒素拮抗剂。
T1321	Nonivamide Nonanoic acid vanillylamide,Pelargonic acid vanillylamide,辣椒素,Vanillyl-N-nonylamide,Pseudocapsaicin	TRP/TRPV Channel	Membrane transporter/Ion channel
	Nonivamide (Nonanoic acid vanillylamide) 具有激动活性，在静态毒性检测中，4d-EC50为 5.1 mg/L。
TN2429	Capsiate	Antioxidant; TRP/TRPV Channel	Membrane transporter/Ion channel; oxidation-reduction
	Capsiate 是一种具有口服活性的 TRPV1 激动剂，是非刺激性辣椒素类似物，可作为抗过敏剂，具有抗炎、抗氧、降糖和抑制血管生成活性。
T4513	Vanillyl butyl ether 4-(Butoxymethyl)-2-methoxyphenol,香兰醇丁醚,Butyl vanillyl ether,香草醇丁醚	Others	Others
	Vanillyl butyl ether (Butyl vanillyl ether) 是香草特有风味和香气的来源。它是辣椒素类似物，对人体有感官刺激作用。它是环保且无毒的物质。它是烷氧基取代的苄基衍生物，主要用作调味剂。
TL0018	Lobelin	AChR; Antifection	Microbiology/Virology; Neuroscience
	Inhalation challenge with capsaicin and rapid intravenous injection of Lobelin and alinamin indicated that peripheral c-fiber receptors were involved in the induction of coughing.
TN4440	Limonexic acid	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Limonexic acid shows antinociceptive actions , it produces dose-related inhibition of glutamate- and capsaicin-induced pain. Limonexic acid can effectively protect hepatocyte against CCl4-induced injury.

天然产物

Cat.No: T1062

Synonym: Qutenza,8-Methyl-N-vanillyl-trans-6-nonenamide,天然辣椒素,Vanilloid,辣椒素,(E)-Capsaicin,Zostrix

Target: Apoptosis, TRP/TRPV Channel, Autophagy

Capsaicin β-D-glucopyranoside

Cat.No: T39018

Nordihydrocapsaicin

Cat.No: T3421

Target: Others

Dihydrocapsaicin

Cat.No: T2163

Synonym: CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide

Target: Others, TRP/TRPV Channel

Homodihydrocapsaicin I

Cat.No: TN1739

Synonym: 高二氢辣椒素,高二氢辣椒素I

Target: Others

Homocapsaicin II

Cat.No: T82187

Cat.No: T5S1389

Synonym: 七叶皂苷B,七叶皂苷 IB

Target: 5-HT Receptor, NO Synthase

Cat.No: T7177

Target: Apoptosis, TRP/TRPV Channel

Cat.No: T1321

Synonym: Nonanoic acid vanillylamide,Pelargonic acid vanillylamide,辣椒素,Vanillyl-N-nonylamide,Pseudocapsaicin

Target: TRP/TRPV Channel

Cat.No: TN2429

Target: Antioxidant, TRP/TRPV Channel

Vanillyl butyl ether

Cat.No: T4513

Synonym: 4-(Butoxymethyl)-2-methoxyphenol,香兰醇丁醚,Butyl vanillyl ether,香草醇丁醚

Target: Others

Cat.No: TL0018

Target: AChR, Antifection

Cat.No: TN4440

Target: GABA Receptor

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