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23

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6015	Cathepsin Inhibitor 1	Cysteine Protease	Proteases/Proteasome
	Cathepsin inhibitor 1 是Cathepsin 的选择性抑制剂，能够抑制CatL(pIC50:7.9)、CatL2(pIC50:6.7)、CatS(pIC50:6.0)、CatK(pIC50:5.5)和CatB(pIC50:5.2)。
T9598	NCATS-SM1441

T70033	NCATS-SM1440
	NCATS-SM1440 is a Lactate Dehydrogenase Inhibitor with Optimized Cell Activity and Pharmacokinetic Properties.
T63663	NCATS-SM4487
	NCATS-SM4487 是高度选择性的 GALK1 抑制剂 (IC50: 0.05 μM)。
T15272	Febantel	Parasite	Microbiology/Virology
	Febantel 是一种用于家禽和家畜的蛔虫、绦虫感染的驱虫剂。
T21526	α-Guanidinoglutaric Acid	Others	Others
	α-Guanidinoglutaric Acid 存在于猫大脑皮层钴诱导的致癫痫病灶组织中。 α-Guanidinoglutaric Acid 诱导的癫痫发作与血清素功能异常有关，它们是由 5-HT 水平的降低引起的。
T7222	GS-441524 GS 441524 triphosphate	Others; SARS-CoV; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others
	GS-441524 是 Remdesivir 的主要活性代谢物，活性更优于 Remdesivir ，治疗患有自然发生的猫传染性腹膜炎的猫。
T36619	Aligeron	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Aligeron 是一种非选择性的prostaglandin (PG)拮抗剂，对PGF2α和PGE2诱导的猫血压下降有抑制作用，可用于抑制PGF2α诱导的小鼠腹泻和PGE2诱导的大鼠爪水肿。Aligeron 对血管并发症具有抗氧化保护作用。
TQ0145	(R)-(+)-Bay-K-8644 (R)-(+)-Bay K 8644	Calcium Channel; PPAR	DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism
	(R)-(+)-Bay-K-8644 是一种 Ca2+ 通道激动剂，是二氢吡啶激动剂，抑制 Ba2+电流 (IBa)，诱导猫的中枢性呼吸抑制，通过竞争性拮抗血栓素 A2-前列腺素 H2 受体抑制血小板活化。
TP2419	V-9-M Cholecystokinin nonapeptide V 9 M,Prepro CCK Fragment V-9-M,Val-pro-val-glu-ala-val-asp-pro-met,Cholecystokinin Precursor (24-32),V9M,V-9-M	Beta Amyloid	Neuroscience
	V-9-M Cholecystokinin nonapeptide (Prepro CCK Fragment V-9-M) 是胆囊收缩素(CCK)的前体化合物。胆囊收缩素(CCK)是一种刺激胆囊收缩和胰腺外分泌的脑肠肽，可从狗和猫的小肠中提取的，可以引起胆囊收缩。
T30629	Butoctamide semisuccinate M 2H,Butoctamide hydrogen succinate,M-2H,M2H
	Butoctamide semisuccinate enhances REM sleep in chronically prepared cats.
T30789	Cefovecin Sodium UK 287,074-02,UK-287,074-02,C13142,D01681,UK287,074-02
	Cefovecin Sodium(Convenia) is an antibiotic of the cephalosporin class, licensed for the treatment of skin infections in cats and dogs.
T36621	Prostaglandin F2β
	Prostaglandin F2β (PGF2β) is the 9β-hydroxy stereoisomer of PGF2α. It is much less active than PGF2α in antifertility and bronchoconstrictor activities. PGF2β exhibits bronchodilating activity in guinea pigs and cats and antagonizes the bronchoconstrictor activity of PGF2α.
T76011	Adrenomedullin (16-31), human TFA
	Adrenomedullin(16-31), human TFA 为人类肾上腺髓质素(hADM)之16至31氨基酸片段，对CGRP1受体显示高亲和力。该化合物在大鼠体内可提高全身血压，但对猫无效。
T41251	Taprostene
	Taprostene (CG-4203) 是一种合成的、化学稳定的前列环素 (PGI2) 类似物。Taprostene 对猫急性心肌缺血再灌注后内皮和心肌有保护作用。Taprostene 增强细胞保护作用，同时减少不必要的血液动力学影响。
T78185	Ac-PLVE-FMK Ac-Pro-Leu-Val-Glu(OMe)-CH2F	Others	Others
	Ac-PLVE-FMK（Ac-Pro-Leu-Val-Glu(OMe)-CH2F），一种四肽基m-FMK化合物，具有Cats抑制作用，常用于癌症研究。
T78316	Frunevetmab NV-02
	Frunevetmab (NV-02)为猫源化抗神经生长因子(NGF)单克隆抗体，具有20 pM的亲和常数(Kd)。该化合物能有效缓解猫骨关节炎(OA)的疼痛。
T38143	Elaidamide
	Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid of sleep-deprived cats.1 It inhibits rat microsomal epoxide hydrolase (mEH; Ki = 70 nM).2 Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2).3 In vivo, elaidamide (10 mg/animal) induces physiological sleep in rats.1References1. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-150...
T81275	Riboxin IDP
	Riboxin (IDP) 是一种抗缺氧及抗高血压活性的口服有效嘌呤衍生物次黄苷。该化合物对心律失常也具有治疗作用，能够干预Ouabain诱导的猫、兔子、小鼠的心脏节律障碍模型。此外，Riboxin还能保护动物不受γ辐射的损害。
T65396	Piperazine 2HCl
	Piperazine (2HCl) is gamma-aminobutyric acid (GABA) agonists and its major effects appear to be on the central nervous system. Piperazine was the anthelmintic with the greatest number of reports of toxicoses and suspected toxicoses in cats. Piperazine neurotoxicity in cats and dogs usually was manifested by muscle tremors, ataxia, and/or behavioral disturbances within 24 hours after estimated daily dose(s) between 20 and 110 mg/kg[1]. For di-substituted derivatives, ciprofloxacin was selected an...
T36565	Adrenomedullin (13-52) (human) (trifluoroacetate salt)
	Adrenomedullin (13-52) is a truncated form of adrenomedullin (1-52) . It induces nitric oxide-dependent relaxation of and inhibits release of angiotensin II and endothelin-1 from isolated rat aorta. In vivo, adrenomedullin (13-52) decreases mean arterial pressure (MAP) in spontaneously and renal hypertensive rats in a dose-dependent manner. Adrenomedullin (13-52) (10-3,000 ng per animal) reverses increases in lobar arterial pressure induced by U-46619 in a dose-dependent manner in cats but has n...
T35858	Adrenomedullin (22-52) (human) (trifluoroacetate salt)
	Adrenomedullin (22-52) is a C-terminal fragment of adrenomedullin (1-52) . In vitro, adrenomedullin (22-52) reduces basal corticosterone production in a mixture of rat adrenocortical and adrenomedulllary cells. It also reverses increases in ACTH-stimulated corticosterone production induced by adrenomedullin (1-52). Adrenomedulin (22-52) (0.5 and 5 μg/kg/min) has no effect on basal regional cerebral blood flow but reverses increases in regional cerebral blood flow induced by rat adrenomedullin in...
T36241	Arecaidine propargyl ester (hydrobromide)
	Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecai...

化合物

Cathepsin Inhibitor 1

Cat.No: T6015

Target: Cysteine Protease

Cat.No: T9598

Cat.No: T70033

Cat.No: T63663

Cat.No: T15272

Target: Parasite

α-Guanidinoglutaric Acid

Cat.No: T21526

Target: Others

Cat.No: T7222

Synonym: GS 441524 triphosphate

Target: Others, SARS-CoV, DNA/RNA Synthesis

Cat.No: T36619

Target: Prostaglandin Receptor

(R)-(+)-Bay-K-8644

Cat.No: TQ0145

Synonym: (R)-(+)-Bay K 8644

Target: Calcium Channel, PPAR

V-9-M Cholecystokinin nonapeptide

Cat.No: TP2419

Synonym: V 9 M,Prepro CCK Fragment V-9-M,Val-pro-val-glu-ala-val-asp-pro-met,Cholecystokinin Precursor (24-32),V9M,V-9-M

Target: Beta Amyloid

Butoctamide semisuccinate

Cat.No: T30629

Synonym: M 2H,Butoctamide hydrogen succinate,M-2H,M2H

Cefovecin Sodium

Cat.No: T30789

Synonym: UK 287,074-02,UK-287,074-02,C13142,D01681,UK287,074-02

Prostaglandin F2β

Cat.No: T36621

Adrenomedullin (16-31), human TFA

Cat.No: T76011

Cat.No: T41251

Cat.No: T78185

Synonym: Ac-Pro-Leu-Val-Glu(OMe)-CH2F

Target: Others

Cat.No: T78316

Synonym: NV-02

Cat.No: T38143

Cat.No: T81275

Synonym: IDP

Piperazine 2HCl

Cat.No: T65396

Adrenomedullin (13-52) (human) (trifluoroacetate salt)

Cat.No: T36565

Adrenomedullin (22-52) (human) (trifluoroacetate salt)

Cat.No: T35858

Arecaidine propargyl ester (hydrobromide)

Cat.No: T36241

Cat. No.	Product Name	Target	Signaling Pathways
T1157	Moxidectin milbemycin B,CL301423,莫昔克丁,莫西菌素	GluCls; Antibiotic; Parasite	Microbiology/Virology
	Moxidectin (CL301423) 是可用于预防和控制心丝虫和蛔虫的一种驱虫剂。
T6S0033	Crotonoside 巴豆苷；异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE	Others; FLT; HDAC	Angiogenesis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Others; Tyrosine Kinase/Adaptors
	Crotonoside (Isoguanosine) 是从中草药巴豆中分离出来的一种天然产物。它抑制 FLT3 和 HDAC3/6，有治疗急性髓性白血病 (AML)的研究潜力。

天然产物

Cat.No: T1157

Synonym: milbemycin B,CL301423,莫昔克丁,莫西菌素

Target: GluCls, Antibiotic, Parasite

Cat.No: T6S0033

Synonym: 巴豆苷；异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE

Target: Others, FLT, HDAC

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