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Search Results for " vanilloid "

48

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9247	Vanilloid receptor antagonist 1 4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile	TRP/TRPV Channel	Membrane transporter/Ion channel
	Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) 是香草酸受体的有效拮抗剂。
T83701	TRPV1-Tat TFA Transient Receptor Potential Vanilloid 1-Tat,736-745-Tat
	TRPV1-Tat是一种针对瞬时受体电位范烤苷1 (TRPV1) 的肽类拮抗剂。它由来自TRPV1的A-激酶锚蛋白(AKAP)结合域的736-745个氨基酸以及来自HIV Tat的细胞穿透肽序列组成。TRPV1-Tat (200 µM) 能够在使用初级小鼠背根神经节的整细胞膜片钳技术中抑制由热或棕榈酸酯12-肉豆蔻酸13-醋酸酯(PMA014)引起的电流。当以10或30 µM剂量给药时，它能增加大鼠后爪机械痛阈。
T6977	SB-366791 SB366791	TRP/TRPV Channel	Membrane transporter/Ion channel
	SB366791 是一种有效的 vanilloid receptor (VR1/TRPV1)选择性拮抗剂 (IC50=5.7 nM)。SB-366791 在炎症方面有研究价值。
T6848	GSK1016790A GSK101	Calcium Channel; TRP/TRPV Channel	Membrane transporter/Ion channel; Metabolism
	GSK1016790A (GSK101) 是选择性瞬时受体电位香草酸 4 通道激活剂，可引起 HEK 细胞中 Ca2+流入并升高细胞内 Ca2+。
T12306	OMDM-5	Cannabinoid Receptor; Endogenous Metabolite; TRP/TRPV Channel	GPCR/G Protein; Membrane transporter/Ion channel; Metabolism
	OMDM-5 是有效的、选择性的anandamide 细胞摄取抑制剂，Ki 为 4.8 μM。它是VR1 (TRPV1)激动剂，EC50为 75 nM，显示出对大麻素 1 型受体 (CB1) 的弱配体活性 (Ki=4.9 μM)。
T12302	OMDM-1 (Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide	Endogenous Metabolite	Metabolism
	OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) 是有效选择性的代谢稳定 anandamide 细胞摄取抑制剂，Ki=为2.4 μM。
T23106	Olvanil N-Vanillyloleamide,奥伐尼,N-Vannilyloleoylamide	TRP/TRPV Channel	Membrane transporter/Ion channel
	Olvanil (N-Vannilyloleoylamide) 是一种vanilloid 受体激动剂，EC50为0.7nM。
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。
T29522	ABT 102 ABT102,CHEMBL398338,ABT-102	TRP/TRPV Channel	Membrane transporter/Ion channel
	ABT 102 (CHEMBL398338) 是瞬时受体电位香草素 1 (TRPV1) 受体的选择性拮抗剂。
T13214L	TRPV4 agonist-1 free base OUN67600	TRP/TRPV Channel	Membrane transporter/Ion channel
	TRPV4 agonist-1 free base (OUN67600) 是有效的瞬时受体电位香草酸亚型 4 激动剂， hTRPV4 Ca2+实验中 EC50值为60 nM。
T14087	ABT-239	TRP/TRPV Channel	Membrane transporter/Ion channel
	ABT-239是一种新型、高效、非咪唑类H3R 拮抗剂，也是一种TRPV1拮抗剂。
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。
T37097	SET 2	TRP/TRPV Channel	Membrane transporter/Ion channel
	SET 2 是瞬时受体电位香草酸 2 型 (TRPV2) 的拮抗剂，IC50 为 0.46 μM。 SET 2 显示了对 TRPV1、TRPV3 和 TRPV4 的选择性。
T22360	MDR-652	TRP/TRPV Channel	Membrane transporter/Ion channel
	MDR-652是瞬时受体电位香草酸亚型 1 的选择性激动剂，对 hTRPV1 和 rTRPV1 的Ki 分别为 11.4 和 23.8 nM，EC50分别为 5.05 和 93 nM。MDR-652在缓解疼痛方面有研究的价值。
T23178	PPAHV	Others	Others
	vanilloid TRPV1 (VR1) receptor agonist
T26663	AS1928370
	AS1928370 is an antagonist of transient receptor potential vanilloid 1 (TRPV1).
T23721	AMG7905 AMG-7905,AMG 7905
	AMG7905 is a modulator of transient receptor potential vanilloid type 1.
T24237	JYL-79 JYL79,JYL 79
	JYL-79 is an agonist of the vanilloid receptor.
T10176	TRPV antagonist 1	Others	Others
	TRPV antagonist 1 is an antagonist of transient receptor potential vanilloid (TRPV; IC50 < 250 nM).
T16426	Asivatrep PAC-14028	Others	Others
	Asivatrep is an effective and selective transient receptor potential vanilloid type I antagonist.
T22527	6'-Iodoresiniferatoxin	Others	Others
	TRPV1 (VR1) vanilloid receptor partial agonist
T22586	Arvanil	Others	Others
	Cannabinoid CB1 and vanilloid TRPV1 (VR1) agonist
TP1934	L-R4W2
	Vanilloid TRPV1 (VR1) receptor antagonist peptide (IC50 ~ 0.1 μM); blocks Ca2+ currents in dorsal root ganglion neurons. Analgesic in vivo.
T68256	JNJ-38893777
	JNJ-38893777 is a potent and selective transient receptor potential vanilloid 1 (TRPV1) channel antagonist.
T15439	GSK3395879	TRP/TRPV Channel	Membrane transporter/Ion channel
	GSK3395879 is a selective and orally bioavailable antagonist of transient receptor potential vanilloid-4 (TRPV4) (IC50: 1 nM for hTRPV4).
T23723	AMG8163 AMG 8163,AMG-8163
	AMG8163 is an antagonist of vanilloid receptor TRPV1.
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.
T69785	GSK3527497
	GSK3527497 is a novel potent and selective inhibitor of transient receptor potential vanilloid-4 (TRPV4).
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.
T26386	4alpha-PDD 4α-Phorbol 12,13-didecanoate
	4alpha-PDD activates transient receptor potential vanilloid 4 (TRPV4) channels and is inactive for signaling through PKC.
T15434	GSK2798745	TRP/TRPV Channel	Membrane transporter/Ion channel
	GSK2798745 is an orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker (IC50s: 1.8 and 1.6 nM for hTRPV4 and rTRPV4). It is used in research for the treatment of pulmonary edema associated with congestive heart failure.
T76369	CEDAEVFKDSMVPGEK
	CEDAEVFKDSMVPGEK 为大鼠辣椒素受体亚型 1 (VR1) 的多肽序列片段，适用于探测 VR1 的存在、分布及分子形态。
T71563	10-oxo-12(Z)-Octadecenoic Acid
	10-oxo-12(Z)-Octadecenoic acid is a metabolite of linoleic acid and an activator of transient receptor potential vanilloid 1 (TRPV1) and selectively increases calcium levels in HEK293 cells expressing TRPV1.
T41091	JTS-653
	JTS-653 is a potent and selective in vitro and in vivo antagonist of transient receptor potential vanilloid 1 (TRPV1). It effectively attenuates chronic pain resistant to non-steroidal anti-inflammatory drugs.
T39293	Tivanisiran SYL1001,Tivanisiran
	Tivanisiran (SYL1001) is a siRNA developed specifically to inhibit the expression of transient receptor potential vanilloid 1 (TRPV1) to explore its implications in dry eye disease research.
T69784	GSK3527497 HCl
	GSK3527497 is a potent and selective inhibitor of Transient Receptor Potential Vanilloid‑4 (TRPV4) with IC50 = 12 nM) for the treatment of heart failure and respiratory diseases. GSK3527497 is a preclinical candidate suitable for oral and iv administration that is projected to inhibit TRPV4 effectively in patients from a low daily clinical dose.
T75830	L-R4W2 TFA
	L-R4W2 TFA，作为一种有效的香草酸受体1 (VR1，TRPV1) 拮抗剂，其IC50值达到0.1 μM，主要用于疼痛缓解的研究。
T71295	SOR-C13
	SOR-C13 is an inhibitor of transient receptor potential cation channel vanilloid family member 6 (TRPV6, CaT1 or CATL) with potential antineoplastic activity. TRPV6 calcium channel inhibitor SOR-C13 binds to TRPV6 and prevents the influx of calcium ions into TRPV6-expressing tumor cells. This inhibits the activation of nuclear factor of activated T-cell (NFAT) transcription complex which may result in an inhibition of calcium-dependent cancer cell proliferation and an induction of apoptosis in t...
T62543	JNc-440
	JNc-440 是一种有效的抗高血压剂。JNc-440 能够提高内皮细胞瞬时受体电位香草酸亚型 4 (TRPV4) 和钙离子激活钾通道 3 (KCa2.3) 的相互作用。JNc-440 也可以提高小鼠血管扩张，具有降压活性。
T37321	RN-9893 (hydrochloride)
	RN-9893 is an antagonist of transient receptor potential vanilloid 4 (TRPV4; IC50s = 0.42 and 0.66 μM, respectively, for the human and rat receptors).1 It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = 10, >30, and 30 μM, respectively). RN-9893 reduces rat TRPV4 activity induced by 4α-phorbol 12,13-didecanoate or hypotonicity (IC50s = 0.57 and 2.1 μM, respectively, in cell free assays). \|1. Wei, Z.L., Nguyen, M.T., O'Mahony, D.J., et al. Identification of orally-bioavailable antago...
T35921	N-Oleoyl Valine
	N-Oleoyl valine is an endogenous N-acyl amine that acts as an antagonist at the transient receptor potential vanilloid type 3 (TRPV3) receptor, which is involved in thermoregulation. N-Oleoyl valine is increased in mice following cold exposure for up to at least 16 days. Acute lung injury in mice increases the concentration of N-Oleoyl valine in lung tissue. N-acyl amines also promote mitochondrial uncoupling.
T37092	20-HEPE
	20-HEPE is a metabolite of eicosapentaenoic acid that is formed via ω-oxidation of EPA by cytochrome P450 (CYP) ω-oxidases, including human CYP4F3B. It activates peroxisome proliferator-activated receptor α (PPARα) in COS-7 cells expressing a luciferase reporter when used at a concentration of 10 μM. 20-HEPE also activates murine transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro but lacks antinociceptive activity in rats.
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...
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。
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...
T38028	(R)-(+)-Docosahexaenyl-1'-Hydroxy-2'-Propylamide
	N-Acyl ethanolamines (NAEs) have diverse biological actions that are strongly affected by the associated acyl group. Docosahexaenoyl ethanolamide (DHEA) has potential signaling roles in cancer, inflammation, and neurological development and functioning. At least some of DHEA's effects are mediated through cannabinoid (CB) receptors, while some NAEs also act as vanilloid receptor agonists and voltage-gated K+ channel blockers. (R)-(+)-Docosahexaenyl-1'-hydroxy-2'-propylamide is a homolog of DHEA,...
T35918	N-Arachidonoyl Taurine
	N-Arachidonoyl taurine is an arachidonoyl amino acid. It is oxygenated by 12(S)- and 15(S)-lipoxygenase and is converted to 12-HETE-taurine (12-HETE-T) in murine resident peritoneal macrophages. N-Arachidonoyl taurine is an activator of the transient receptor potential vanilloid (TRPV) channels TRPV1 and TRPV4 (EC50s = 28 and 21 μM, respectively). It increases calcium flux in HIT-T15 pancreatic β-cells and INS-1 rat islet cells when used at a concentration of 10 μM and increases insulin secretio...
T83728	Tat-AKAP79 (326-336) TFA Tat-A-kinase Anchor Protein 79 (326-336)
	Tat-AKAP79 (326-336) 是一种肽，由HIV-1 Tat蛋白质转导域与对应于A-kinase anchor protein 79 (AKAP79) 326至336残基的11个氨基酸肽链相连组成。在200 µM浓度下，能抑制蛋白激酶A (PKA) 或PKC激活诱导的瞬时受体电位钒通道1 (TRPV1) 在分离的大鼠背根神经节 (DRG) 神经元中的敏感化。在体内，Tat-AKAP79 (326-336) 抑制小鼠由甲醛或phorbol 12-myristate 13-acetate (PMA014) 引发的伤害性行为。它还延长了小鼠对辐射热刺激爪子撤回的潜伏期，并在卡拉胶诱导的炎症性疼痛小鼠模型中增加了爪子撤回的机械阈力。

化合物

Vanilloid receptor antagonist 1

Cat.No: T9247

Synonym: 4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile

Target: TRP/TRPV Channel

Cat.No: T83701

Synonym: Transient Receptor Potential Vanilloid 1-Tat,736-745-Tat

Cat.No: T6977

Synonym: SB366791

Target: TRP/TRPV Channel

Cat.No: T6848

Synonym: GSK101

Target: Calcium Channel, TRP/TRPV Channel

Cat.No: T12306

Target: Cannabinoid Receptor, Endogenous Metabolite, TRP/TRPV Channel

Cat.No: T12302

Synonym: (Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide

Target: Endogenous Metabolite

Cat.No: T23106

Synonym: N-Vanillyloleamide,奥伐尼,N-Vannilyloleoylamide

Target: TRP/TRPV Channel

Cat.No: T23322

Target: TRP/TRPV Channel

Cat.No: T29522

Synonym: ABT102,CHEMBL398338,ABT-102

Target: TRP/TRPV Channel

TRPV4 agonist-1 free base

Cat.No: T13214L

Synonym: OUN67600

Target: TRP/TRPV Channel

Cat.No: T14087

Target: TRP/TRPV Channel

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: T37097

Target: TRP/TRPV Channel

Cat.No: T22360

Target: TRP/TRPV Channel

Cat.No: T23178

Target: Others

Cat.No: T26663

Cat.No: T23721

Synonym: AMG-7905,AMG 7905

Cat.No: T24237

Synonym: JYL79,JYL 79

TRPV antagonist 1

Cat.No: T10176

Target: Others

Cat.No: T16426

Synonym: PAC-14028

Target: Others

6'-Iodoresiniferatoxin

Cat.No: T22527

Target: Others

Cat.No: T22586

Target: Others

Cat.No: TP1934

Cat.No: T68256

Cat.No: T15439

Target: TRP/TRPV Channel

Cat.No: T23723

Synonym: AMG 8163,AMG-8163

Cat.No: T37668

Synonym: CAY10448

Cat.No: T69785

Cat.No: T37086

Cat.No: T26386

Synonym: 4α-Phorbol 12,13-didecanoate

Cat.No: T15434

Target: TRP/TRPV Channel

CEDAEVFKDSMVPGEK

Cat.No: T76369

10-oxo-12(Z)-Octadecenoic Acid

Cat.No: T71563

Cat.No: T41091

Cat.No: T39293

Synonym: SYL1001,Tivanisiran

Cat.No: T69784

Cat.No: T75830

Cat.No: T71295

Cat.No: T62543

RN-9893 (hydrochloride)

Cat.No: T37321

N-Oleoyl Valine

Cat.No: T35921

Cat.No: T37092

Cat.No: T37732

Cat.No: T21750

N-Oleoyl Glutamine

Cat.No: T36064

(R)-(+)-Docosahexaenyl-1'-Hydroxy-2'-Propylamide

Cat.No: T38028

N-Arachidonoyl Taurine

Cat.No: T35918

Tat-AKAP79 (326-336) TFA

Cat.No: T83728

Synonym: Tat-A-kinase Anchor Protein 79 (326-336)

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。
TN1377	α-Spinasterol Α-波菜甾醇,alpha-Spinasterol,菠甾醇	COX; Antibacterial; TRP/TRPV Channel	Immunology/Inflammation; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
	α-Spinasterol 是一种从Spinacia oleracea 分离的瞬时受体电位香草酸 1 拮抗剂，具有抗菌、抗炎、抗抑郁、抗氧化和抗伤害作用。它抑制COX-1和COX-2活性，IC50值分别为 16.17 μM 和 7.76 μM。
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。

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

Cat.No: TN1377

Synonym: Α-波菜甾醇,alpha-Spinasterol,菠甾醇

Target: COX, Antibacterial, TRP/TRPV Channel

Dihydrocapsaicin

Cat.No: T2163

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

Target: Others, TRP/TRPV Channel

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