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Search Results for " vanilloid receptor antagonist-1 "

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抑制剂 & 化合物

1

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。
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。
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。
T10176	TRPV antagonist 1	Others	Others
	TRPV antagonist 1 is an antagonist of transient receptor potential vanilloid (TRPV; IC50 < 250 nM).
T26663	AS1928370
	AS1928370 is an antagonist of transient receptor potential vanilloid 1 (TRPV1).
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).
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.
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.
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。
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...
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...
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。

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: T23322

Target: TRP/TRPV Channel

Cat.No: T29522

Synonym: ABT102,CHEMBL398338,ABT-102

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

TRPV antagonist 1

Cat.No: T10176

Target: Others

Cat.No: T26663

Cat.No: T68256

Cat.No: T15439

Target: TRP/TRPV Channel

Cat.No: T37668

Synonym: CAY10448

Cat.No: T41091

Cat.No: T75830

RN-9893 (hydrochloride)

Cat.No: T37321

Cat.No: T37732

Cat.No: T83701

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

Cat. No.	Product Name	Target	Signaling Pathways
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。

天然产物

Cat.No: TN1377

Synonym: Α-波菜甾醇,alpha-Spinasterol,菠甾醇

Target: COX, Antibacterial, TRP/TRPV Channel

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