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Search Results for " nk1 antagonist 1 "

23

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12233	NK-1 Antagonist 1 Rolapitant intermediate	Others	Others
	NK-1 Antagonist 1 is a NK-1 receptor antagonist.
T72224	NK1 receptor antagonist 2
	NK1receptor antagonist 2 是一种 NK1受体拮抗剂。NK1receptor antagonist 2 可用于耳鸣和听力损失的研究。
T13306L	Vapreotide acetate RC-160 acetate,醋酸伐普肽,BMY-41606 acetate	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Vapreotide acetate (BMY-41606 acetate) 是神经激肽-1 (NK1) 受体拮抗剂，IC50值为 330 nM。
T68068	Ezlopitant CJ 11974,CJ-11974,CJ11974	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Ezlopitant (CJ-11974) 是一种基于喹啉的原型 NK1受体拮抗剂 CP-96345的衍生物。
T6905	Netupitant Ro 67-31898/000,奈妥吡坦,CID 6451149	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Netupitant (CID 6451149) 是一种高效选择性、可口服的神经激肽 1 受体 (NK1) 拮抗剂，具有止吐作用，在 CHO 细胞中对 hNK1的 Ki 值为 0.95 nM。
T3716	Rolapitant 罗拉吡坦,SCH619734,罗拉匹坦	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Rolapitant (SCH619734) 是一种高效选择性具有口服活性的神经激肽 1 受体抑制剂，Ki 值为0.66 nM。
T3724	Rolapitant hydrochloride Rolapitant HCl,罗拉匹坦盐酸盐	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Rolapitant (SCH619734) hydrochloride 是一种高效选择性和具有口服活性的神经激肽 1 (NK1) 受体拮抗剂，Ki 值为 0.66 nM。Rolapitant hydrochloride (Rolapitant HCl) 不与 CYP3A4 产生互作。Rolapitant hydrochloride 在雪貂呕吐模型中显示出强效的中枢介导的止吐活性。
T28917	TAK-637 TAK 637
	TAK-637 is a tachykinin 1 (NK1) receptor antagonist.
T13306	Vapreotide BMY 41606,RC160	Others	Others
	Vapreotide is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).
T9471	Imnopitant
	Imnopitant 是 NK1 受体的拮抗剂。
T73705	Imnopitant dihydrochloride
	Imnopitant dihydrochloride 是一种神经激肽NK1受体拮抗剂。
T10688	Casopitant mesylate GW679769B	P450; Neurokinin receptor	GPCR/G Protein; Metabolism; Neuroscience
	Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of antiemetics.
T80031	[D-Pro2] Spantide I TFA	Neurokinin receptor	GPCR/G Protein; Neuroscience
	[D-Pro2] Spantide I TFA 为Spantide类似物，属于选择性NK1受体拮抗剂。
T71935	WIN 66306
	WIN 66306 is a cyclic heptapeptide antagonist of neurokinin-1 (NK1) and NK2 receptors originally isolated from A. flavipes. It binds to NK1 and NK2 receptors and inhibits contractions induced by substance P in isolated guinea pig ileum in a concentration-dependent manner.
T76406	[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11)
	[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) 为高效的神经激肽 NK1 拮抗剂，能够有效抑制金蛋白 P 物质 (GPSP) 与 P 物质 (SP) 的活性。
T78104	Fosnetupitant chloride monohydrochloride Pronetupitant chloride monohydrochloride	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Fosnetupitant chloride monohydrochloride（Pronetupitant chloride monohydrochloride）为NK1受体拮抗剂，对人NK1受体和NK3受体的pKi分别为9.5和6.1。它是奈妥匹坦的亚甲基磷酸酯前体。
T68371	Rolapitant hydrochloride hydrate
	Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of ...
T70456	Nolpitantium Free Base
	Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no eff...
T66676	SCH619734 SCH-619734
	Rolapitant Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity.
T75837	Spantide I TFA
	Spantide I TFA 是substance P 的类似物，是选择性的神经激肽-1 受体 (NK1receptor) 的拮抗剂，其对NK1和NK2受体的Ki 值分别为 230 nM 和8150 nM。Spantide I 可减少感染角膜的1型细胞因子和增强2型细胞因子IL-10，从而显著减少角膜穿孔。
T75881	GR 64349 TFA
	GR 64349为一种有效且高度选择性的神经激肽 2(NK2)受体肽类拮抗剂，具有在大鼠结肠中的EC50值仅为3.7 nM。相较于NK1和NK3受体，GR 64349展现出超过1000倍与300倍的选择性差异。
T38276	Benzomalvin C
	Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg/ml in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. It was isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.
T75880	GR 94800 TFA
	GR 94800 TFA 是有效的、选择性的神经激肽 2(NK2)受体的肽类拮抗剂，其对 NK2、NK1和 NK3受体的 pKB 值分别为 9.6、6.4 和 6.0。

化合物

NK-1 Antagonist 1

Cat.No: T12233

Synonym: Rolapitant intermediate

Target: Others

NK1 receptor antagonist 2

Cat.No: T72224

Vapreotide acetate

Cat.No: T13306L

Synonym: RC-160 acetate,醋酸伐普肽,BMY-41606 acetate

Target: Neurokinin receptor

Cat.No: T68068

Synonym: CJ 11974,CJ-11974,CJ11974

Target: Neurokinin receptor

Cat.No: T6905

Synonym: Ro 67-31898/000,奈妥吡坦,CID 6451149

Target: Neurokinin receptor

Cat.No: T3716

Synonym: 罗拉吡坦,SCH619734,罗拉匹坦

Target: Neurokinin receptor

Rolapitant hydrochloride

Cat.No: T3724

Synonym: Rolapitant HCl,罗拉匹坦盐酸盐

Target: Neurokinin receptor

Cat.No: T28917

Synonym: TAK 637

Cat.No: T13306

Synonym: BMY 41606,RC160

Target: Others

Cat.No: T9471

Imnopitant dihydrochloride

Cat.No: T73705

Casopitant mesylate

Cat.No: T10688

Synonym: GW679769B

Target: P450, Neurokinin receptor

[D-Pro2] Spantide I TFA

Cat.No: T80031

Target: Neurokinin receptor

Cat.No: T71935

[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11)

Cat.No: T76406

Fosnetupitant chloride monohydrochloride

Cat.No: T78104

Synonym: Pronetupitant chloride monohydrochloride

Target: Neurokinin receptor

Rolapitant hydrochloride hydrate

Cat.No: T68371

Nolpitantium Free Base

Cat.No: T70456

SCH619734 SCH-619734

Cat.No: T66676

Cat.No: T75837

Cat.No: T75881

Cat.No: T38276

Cat.No: T75880

Cat. No.	Product Name	Target	Signaling Pathways
T71833	Acetylaszonalenin
	Acetylaszonalenin is a fungal metabolite that has been found in A. flavipes.1 It acts as an antagonist of neurokinin-1 (NK1) receptors, inhibiting binding of substance P with a Ki value of 170 μM.
T38033	Benzomalvin B
	Benzomalvin B is a fungal metabolite originally isolated from Penicillium. It acts as an antagonist of neurokinin-1 (NK1) receptors, inhibiting binding of substance P by 24% in vitro when used at a concentration of 100 μg/ml.

天然产物

Acetylaszonalenin

Cat.No: T71833

Cat.No: T38033

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