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26

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TP2453	Conotoxin GII alpha-Conotoxin G II
	Conotoxin GII is a highly toxic peptide.
TP2158L1	TRV-120027 acetate (1234510-46-3 free base)	RAAS; Arrestin	Endocrinology/Hormones; GPCR/G Protein
	TRV-120027 acetate (1234510-46-3 free base) 是 1 型血管紧张素 II 受体（AT1 受体）的 β-arrestin-1 偏向激动剂，可与 ß-arrestins 结合，同时阻断 G 蛋白信号传导。
TP1787L	PKG Substrate acetate（81187-14-6 free base)	PKA	Tyrosine Kinase/Adaptors
	PKG Substrate acetate（81187-14-6 free base) 是 cGMP 依赖性蛋白激酶 (PKG) 的选择性底物。PKG Substrate 是蛋白激酶 G (PKG) 的选择性底物，PKG Iα (Km = 59 µM) 优于 PKG II (Km = 305)微米）。
TP2158	TRV-120027 TFA TRV-120027 TFA (1234510-46-3 free base)	RAAS; Arrestin	Endocrinology/Hormones; GPCR/G Protein
	TRV-120027 TFA 是一种血管紧张素 II 介导的血管收缩抑制剂，可增加心肌细胞的收缩力。它是一种偏向 β-arrestin-1 的 AT1R 激动剂，可与 ß-arrestins 结合，同时阻断 G 蛋白信号传导。它通过阳离子通道亚家族 C3 (TRPC3) 偶联诱导急性儿茶酚胺分泌，并促进在质膜上形成由 AT1R-β-arrestin-1-TRPC3-PLCγ 组成的大分子复合物。
T7656	Apelin-13
	Apelin-13 是存在于中枢和外周神经系统由13个氨基酸组成的多肽序列，是 G 蛋白偶联受体angiotensin II protein J (APJ) 的内源性配体，对 APJ 的 EC50 值为 0.37 nM。Apelin-13 具有扩张血管和降压活性，可用于研究 2 型糖尿病综合征。
T36968	ARN-21934	Topoisomerase	DNA Damage/DNA Repair
	ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂，具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM，ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。
T81789	Miromavimab M777-16-3
	Miromavimab (M777-16-3)为针对狂犬病毒ERAGP外域表位G-II的单克隆抗体(mAb)。
T63304	Topoisomerase II inhibitor 9
	Topoisomerase II inhibitor 9 是 Topo II 抑制剂 (IC50: 0.97 μM)，也是 DNA 嵌入剂 (IC50: 43.51 μM)，能够在 G2/M 期阻滞 Hep G‐2 细胞周期，诱导细胞凋亡 (apoptosis)。
T76196	TRV055 hydrochloride
	TRV055 hydrochloride，G 蛋白-偏向激动剂，作为AT1R的Gq-偏向配体，有效激发细胞内Gq介导信号传导。
T75962	Urotensin II, mouse acetate
	Urotensin II, mouse acetate，是孤儿G蛋白偶联受体（GPR14或SENR）的一种内源性配体，具有显著的血管收缩活性并在中枢神经系统中发挥重要功能。
T75961	Urotensin II, mouse TFA
	Urotensin II, mouse TFA 为孤儿G蛋白偶联受体GPR14或SENR的内源性配体，具有强效血管收缩作用，并在中枢神经系统中发挥重要角色。
TP1787	PKG Substrate
	PKG Substrate is a selective substrate for cGMP-dependent protein kinase (PKG).PKG Substrate is a selective substrate for protein kinase G (PKG) with a strong preference for PKG Iα (Km = 59 µM) over PKG II (Km = 305 µM).
T35459	Glycyl H-1152 hydrochloride
	Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits bett...
T26868	BMS-986118 BMS 986118
	BMS-986118 is a full agonist of GPR40, is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cells that has been a target of significant recent therapeutic interest for type II diabetes. Activation of GPR40 by partial a
T68207	Elsamitrucin
	Elsamitrucin is a heterocyclic antineoplastic antibiotic isolated from the bacterium Actinomycete strain J907-21. Elsamitrucin intercalates into DNA at guanine-cytosine (G-C)-rich sequences and inhibits topoisomerase I and II, resulting in single-strand breaks and inhibition of DNA replication. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
T37665	Endosulfan I
	Endosulfan I is an organochlorine insecticide and a stereoisomer of endosulfan II . It is active against a variety of insects, including bollworms (LD50 = 0.63 mg/g). Endosulfan I binds to GABA receptors in rat brain membranes with an IC50 value of 30 nM and is toxic to rats (LD50 = 18 mg/kg).
T64266	KR-39038
	KR-39038 是一种口服具有活力的 GRK5 (G 蛋白偶联受体激酶 5) 抑制剂 (IC50: 0.02 μM)。KR-39038 能够抑制新生儿心肌细胞的 HDAC5 通路，明显抑制血管紧张素 II 诱导的细胞肥大，具有显著的抗心肌肥厚和改善心功能作用。KR-39038 能够用于进行心力衰竭的研究。
T74142	Angiotensin II human TFA
	Angiotensin II human (Angiotensin II) TFA 作为肾素/血管紧张素系统中关键的生物活性肽，扮演着血管收缩剂的角色并在调节人体血压中发挥中心作用。其主要通过与 G 蛋白偶联受体 (GPCRs)、血管紧张素 II 1型受体 (AT1R) 和血管紧张素 II 2型受体 (AT2R) 的相互作用来介导效应，包括刺激交感神经系统、增加醛固酮的生物合成和肾脏功能。此外，Angiotensin II human TFA 促进血管平滑肌细胞的生长和 I 型及 III 型胶原在成纤维细胞中的合成，导致血管壁与心肌增厚及纤维化，并诱导细胞凋亡。还通过LOX-1依赖的氧化还原敏感路径诱导内皮细胞中的毛细血管形成。
T36729	Urotensin II (goby) (trifluoroacetate salt)
	Urotensin II is a peptide vasoconstrictor and agonist of the urotensin (UT) receptor (Ki= 2.06 nM for the human recombinant receptor expressed in HEK293 cells).1It stimulates intracellular calcium mobilization in HEK293 cells expressing human and rat UT (EC50s = 0.47 and 0.78 nM, respectively) but decreases intracellular calcium concentration in goby (G. mirabilis) enterocytes when used at a concentration of 500 nM.2Urotensin II (20 mU/ml) stimulates active sodium and chloride absorption across ...
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...
TP1816	Urotensin II, mouse
	Jump to search UTS2 Identifiers Aliases UTS2, PRO1068, U-II, UCN2, UII, urotensin 2 External IDs OMIM: 604097 MGI: 1346329 HomoloGene: 4939 GeneCards: UTS2 hide Gene location (Human) Chr. Chromosome 1 (human)[1] Band 1p36.23 Start 7,843,083 bp[1] En
T70222	Ethonafide
	Ethonafide is an anthracene-containing derivative of amonafide that belongs to the azonafide series of anticancer agents. The lack of cross-resistance in multidrug-resistant cancer cell lines and the absence of a quinone and hydroquinone moiety make ethonafide a potentially less cardiotoxic replacement for existing anthracene-containing anticancer agents. Ethonafide was cytotoxic against three human prostate cancer cell lines at nanomolar concentrations. Ethonafide was found to be better tolerat...
T35814	Urocortin III (human) (trifluoroacetate salt)
	Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively)....
T35855	AAA
	AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension...
T37847	Zonisamide-13C2,15N Zonisamide-13C2,15N
	Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...
T37794	Rec 15/2615 (hydrochloride)
	Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50...

化合物

Cat.No: TP2453

Synonym: alpha-Conotoxin G II

TRV-120027 acetate (1234510-46-3 free base)

Cat.No: TP2158L1

Target: RAAS, Arrestin

PKG Substrate acetate（81187-14-6 free base)

Cat.No: TP1787L

Target: PKA

Cat.No: TP2158

Synonym: TRV-120027 TFA (1234510-46-3 free base)

Target: RAAS, Arrestin

Cat.No: T7656

Cat.No: T36968

Target: Topoisomerase

Cat.No: T81789

Synonym: M777-16-3

Topoisomerase II inhibitor 9

Cat.No: T63304

TRV055 hydrochloride

Cat.No: T76196

Urotensin II, mouse acetate

Cat.No: T75962

Urotensin II, mouse TFA

Cat.No: T75961

Cat.No: TP1787

Glycyl H-1152 hydrochloride

Cat.No: T35459

Cat.No: T26868

Synonym: BMS 986118

Cat.No: T68207

Cat.No: T37665

Cat.No: T64266

Angiotensin II human TFA

Cat.No: T74142

Urotensin II (goby) (trifluoroacetate salt)

Cat.No: T36729

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

Urotensin II, mouse

Cat.No: TP1816

Cat.No: T70222

Urocortin III (human) (trifluoroacetate salt)

Cat.No: T35814

Cat.No: T35855

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Rec 15/2615 (hydrochloride)

Cat.No: T37794

Cat. No.	Product Name	Target	Signaling Pathways
T31993	Grayanotoxin II G-II,Deacetylanhydroandromedotoxin,delta(sup 10 (18))-Andromedenol
	Grayanotoxins are a group of closely related neurotoxins named after Leucothoe grayana. Extract from leaves of Ericaceae.
TN7109	Prosaikogenin G	RAAS	Endocrinology/Hormones
	Prosaikogenin G 是一种从柴胡的根中分离出的化合物，是 Saikosaponin d 在胃肠道中的衍生物。Prosaikogenin G 对 Angiotensin II 诱导的大鼠系膜细胞增殖具有明显的抑制作用，同时对肾脏有保护作用。
T3S1612	kuwanon G 桑黄酮G,Moracenin B,桑黄酮 G,Kuwanone G	Phosphatase; Antibacterial; Bombesin Receptor; AChR; AChE; Glucosidase	GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience
	Kuwanon G (Moracenin B) 是一种从桑树中得到的黄酮类蛙皮素受体拮抗剂，具有杀菌作用。
TN3557	Cabraleadiol	ATPase; Antifection	Membrane transporter/Ion channel; Microbiology/Virology
	Cabraleadiol displays antimycobacterial activity against Mycobacterium tuberculosis, it also is weakly cytotoxic to a breast cancer (BC) cell line. Cabraleadiol inhibits photosystem II (PS II) and induces the appearance of small G band which is related wi

天然产物

Grayanotoxin II

Cat.No: T31993

Synonym: G-II,Deacetylanhydroandromedotoxin,delta(sup 10 (18))-Andromedenol

Prosaikogenin G

Cat.No: TN7109

Target: RAAS

Cat.No: T3S1612

Synonym: 桑黄酮G,Moracenin B,桑黄酮 G,Kuwanone G

Target: Phosphatase, Antibacterial, Bombesin Receptor, AChR, AChE, Glucosidase

Cat.No: TN3557

Target: ATPase, Antifection

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