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34

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T0383	Fenspiride hydrochloride Fenspiride HCl,Pneumorel,Fluiden,Decaspiride,盐酸芬司必利	Adrenergic Receptor; PDE; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
	Fenspiride hydrochloride (Decaspiride) 是一种口服活性的非甾体抗炎剂，是 H1-组胺受体的拮抗剂，可用于呼吸系统疾病的研究。
T16965	Symetine L 16726	Parasite	Microbiology/Virology
	Symetine（L 16726）是一种具有抗寄生虫活性的小分子化合物，可用于研究豚鼠阿米巴肝脓肿。
TP1358L	Peptide M acetate Peptide M acetate(110652-62-5 free base),Peptide M 醋酸盐	Others	Others
	Peptide M acetate 是一种合成多肽 (长度为 18 个氨基酸，对应于牛 S 抗原的氨基酸位置303-322: DTNLASSTIIKEGIDKTV)，能够在猴子和 Hartley 豚鼠以及 Lewis 大鼠中诱导实验性自身免疫性葡萄膜炎。
T31195	Dalcotidine KU 1257,KU-1257	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Dalcotidine (KU 1257) 是一种新型组胺H2受体拮抗剂，具有组胺H9受体拮抗活性和抗分泌作用，与豚鼠大脑皮层结合的Ki 值为0.040 对分离性豚鼠右心房组胺诱导的正变时反应的拮抗作用的KB 值为0.041。Dalcotidine 提高了溃疡愈合的质量，可能有助于降低溃疡的复发率和复发率。
T4535L	Etomoxir (R)-(+)-Etomoxir	Antioxidant; CPT	Metabolism; oxidation-reduction
	Etomoxir 是肉碱棕榈酰转移酶 1a （CPT-1a）抑制剂，通过抑制 CPT-1a 来抑制脂肪酸氧化，且抑制人、大鼠和豚鼠中棕榈酸酯的氧化。Etomoxir 对腺嘌呤核苷酸转位酶有抑制作用，可通过破坏CoA稳态来抑制巨噬细胞极化。
T68109	Moxipraquine	Antibiotic	Microbiology/Virology
	Moxipraquine 是一种新型的8-氨基喹诺酮类化合物，对克氏锥虫具有抗感染活性。Moxipraquine 能有效抑制寄生虫血症，但不能根除小鼠或豚鼠的感染。Moxipraquine 对重度利什曼原虫、墨西哥乳杆菌和巴西乳杆菌的实验性感染有效，但对巴西乳杆菌无效。
T23283	2-Methoxyidazoxan monohydrochloride RX 821002 hydrochloride	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	L-Albizziin (2-Methoxyidazoxan monohydrochloride) 是高效的 alpha 2r 肾上腺素受体选择性拮抗剂，对 imidazoline 拮抗作用很小或没有。它对 (豚鼠) alpha 2D 肾上腺素受体 (pKd9.7) 的亲和力明显高于 (兔子) alpha 2A 肾上腺素受体 (pKd8.2)。
T33647L	Nesosteine Lithium Nesosteine Lithium(84233-61-4 Free baes)
	Nesosteine Lithium 是一种新型的粘液调节剂，对豚鼠 Herxheimer 微休克具有抑制作用且抑制卵清蛋白诱导的组胺在致敏动物气管中的释放。Nesosteine Lithium 能够保护致敏动物免受卵清蛋白诱导的支气管痉挛但对组胺和乙酰胆碱诱导的支气管痉挛无效。
T15647	Tipelukast MN 001,KCA 757	Leukotriene Receptor	GPCR/G Protein
	Tipelukast (KCA 757) 是一种新型可口服的白三烯受体 (leukotriene receptor) 拮抗剂，是具有抗炎活性，可减少纤维化，下调 TIMP-1、1 型胶原蛋白。Tipelukast 可用于研究哮喘疾病。
T30110	AR 12456 AR12456,AR-12456
	AR-12456 is a Trapidil derivative that prevents serum hyperlipidemia in guinea pigs.
T27915	LY 302148 LY-302148,LY302148
	LY 302148 , a 5-HT1F receptor agonist, inhibits neurogenic dural inflammation in guinea pigs. It has potential for migraine therapeutics.
T23829	Btm 1042 Btm1042,Btm-1042
	Btm 1042 is an antispasmodic drug. It has been found to depress twitch responses in the ileum of guinea pigs.
T36772	11-deoxy Prostaglandin F1β 11-deoxy Prostaglandin F1β
	11-deoxy PGF1β is a synthetic analog of PGF1β. In contrast to PGF2α and PGF1α, 11-deoxy PGF1β exhibits vasodepressor and bronchodilator activities in guinea pigs at a dose of 500 μg/kg.
T68242	D-Mabuterol hydrochloride
	D-Mabuterol hydrochloride is a D isoform of Mabuterol, which is a selective β2 adrenoreceptor agonist. Mabuterol has been found to decrease the blood pressure in rats and increase heart rate and contractile force in guinea pigs. Mabuterol inhibited the positive inotropic effect of isoprenaline but has no effect on alpha-adrenergic, acetylcholine and histamine receptors.
T82424	Experimental allergic encephalitogenic peptide (human)
	Experimental allergic encephalitogenic peptide (human) 为EAE多肽类化合物，能够诱导豚鼠发生脑脊髓炎。
T28296	Parogrelil hydrochloride INDI-702,NM-702,NT-702,NM702,INDI702
	Parogrelil is a phosphodiesterase (PDE3/PDE5A) inhibitor potentially for the treatment of intermittent. Parogrelil suppress the asthmatic response in guinea pigs, with both bronchodilating and anti-inflammatory effects. Parogrelil improves reduced walking
T38266	Nirogacestat dihydrobromide
	Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs. Lanz et al (2010) Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. J.Pharmacol.Exp.Ther. 334 269 PMID:20363853
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.
T32770	Linsidomine CV 664
	Lincydomine is a smooth muscle relaxant, beneficial to the treatment of unstable angina pectoris, but also can open the respiratory tract of humans and guinea pigs.
T70106	F-050
	F-050 is a biochemical that has been shown to inhibit platelet aggregation induced by CaCl2, arachidonic acid, collagen, adenosine diphosphate (ADP) and thrombin in guinea pigs, rabbits and rats in vitro. F-050 may be useful in the treatment of thrombotic diseases.
T13331	WAY127093B racemate	PDE	Metabolism
	WAY127093B racemate 是WAY127093 B 的外消旋体。WAY127093B 是一种磷酸二酯酶IV 抑制剂，在大鼠和豚鼠中具有口服活性。
T67962	sulukast
	Sulukast 是一种有效的吸入白三烯拮抗剂，在豚鼠中被发现可有效预防白三烯和抗原诱导的支气管痉挛。
T69084	Mabuterol, (R)-
	Mabuterol, (R)- is a D isoform of Mabuterol, which is a selective β2 adrenoreceptor agonist. Mabuterol has been found to decrease the blood pressure in rats and increase heart rate and contractile force in guinea pigs. Mabuterol inhibited the positive inotropic effect of isoprenaline but has no effect on alpha-adrenergic, acetylcholine and histamine receptors.
T69085	Mabuterol, (S)-
	Mabuterol, (S)- is a D isoform of Mabuterol, which is a selective β2 adrenoreceptor agonist. Mabuterol has been found to decrease the blood pressure in rats and increase heart rate and contractile force in guinea pigs. Mabuterol inhibited the positive inotropic effect of isoprenaline but has no effect on alpha-adrenergic, acetylcholine and histamine receptors.
T60419	Cyclic HPMPC
	Cyclic HPMPC 是有效的抗病毒剂，可以增加感染致死性牛痘苗病毒 (IHD 株) 小鼠的动脉氧饱和度水平。用 Cyclic HPMPC 治疗可改善先天性豚鼠巨细胞病毒 (GPCMV) 感染的结果并减少豚鼠模型中的病毒复制。
T36770	11-deoxy Prostaglandin E1 11-deoxy Prostaglandin E1
	11-deoxy Prostaglandin E1 是前列腺素 E1类似物，具有支气管扩张活性，可抑制组胺诱导的支气管收缩，引起离体豚鼠的气管条松弛。
T36771	11-deoxy Prostaglandin F1α 11-deoxy Prostaglandin F1α
	11-deoxy PGF1α is a synthetic analog of PGF1α. In whole animal studies, a dose of 32 mg/kg inhibited gastric acid secretion by 35%. 11-deoxy PGF1α is also known to cause rat uterine contractions at a dose 0.3 times that of PGF1α. It also exhibits vasopressor and bronchoconstrictor activities at about half the potency of PGF2α in guinea pigs.
T83924	(R)-(+)-Deoxyarbutin
	(R)-(+)-Deoxyarbutin 是 deoxyarbutin 的一个异构体，同时也是一种酪氨酸酶抑制剂。在 21 µM 的浓度下，它能够抑制酪氨酸酶的活性。(R)-(+)-Deoxyarbutin (1%) 能够使无毛的深色、中等和浅色皮肤豚鼠的皮肤变亮。
T70376	CHF-6366
	CHF-6366是一种高效的M3毒蕈碱拮抗剂和β2肾上腺素能受体激动剂，具有pKi值分别为10.4和11.4。同时，CHF-6366作为一种弱钙离子通道抑制剂，其IC50约为50μM。该化合物能够抑制豚鼠的支气管收缩，适用于慢性阻塞性肺疾病研究。
T69215	Ambrein
	Ambrein is a triterpene alcohol that is the chief constituent of ambergris, a secretion from the digestive system of the sperm whale, and has been suggested as the possible active component producing the supposed aphrodisiac effects of ambergris. It serves as the biological precursor for a number of aromatic derivatives such as ambroxan and is thought to possess fixative properties for other odorants. It has been shown to act as an analgesic and it has been proven to increase sexual behavior in ...
T37728	Methoctramine (hydrate)
	Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes).[1] It is selective for M2 over M1, M3, M4, and M5 receptors (IC50s = 92, 770, 260, and 217 nM, respectively). In vitro, methoctramine inhibits acetylcholine-induced reductions in isolated guinea pig tracheal tube contractions when used at a concentration of 1 μM.[2] In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholinein guinea pigs wit...
T36618	Rupatadine
	Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu...
T13421	(-)-Cevimeline hydrochloride hemihydrate (-)-SNI-2011,(-)-AF102B hydrochloride hemihydrate	ALK	Angiogenesis; Tyrosine Kinase/Adaptors
	(-)-Cevimeline hydrochloride hemihydrate ((-)-SNI-2011) 是一种新型mAChR 激动剂，是一种治疗干燥综合征口干症的候选治疗药物。
T13460	(+)-Cevimeline hydrochloride hemihydrate (+)-AF102B hydrochloride hemihydrate,(+)-SNI-2011	Others	Others
	(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011) 是一种有效的 mAChR 激动剂。

化合物

Fenspiride hydrochloride

Cat.No: T0383

Synonym: Fenspiride HCl,Pneumorel,Fluiden,Decaspiride,盐酸芬司必利

Target: Adrenergic Receptor, PDE, Histamine Receptor

Cat.No: T16965

Synonym: L 16726

Target: Parasite

Peptide M acetate

Cat.No: TP1358L

Synonym: Peptide M acetate(110652-62-5 free base),Peptide M 醋酸盐

Target: Others

Cat.No: T31195

Synonym: KU 1257,KU-1257

Target: Histamine Receptor

Cat.No: T4535L

Synonym: (R)-(+)-Etomoxir

Target: Antioxidant, CPT

Cat.No: T68109

Target: Antibiotic

2-Methoxyidazoxan monohydrochloride

Cat.No: T23283

Synonym: RX 821002 hydrochloride

Target: Adrenergic Receptor

Nesosteine Lithium

Cat.No: T33647L

Synonym: Nesosteine Lithium(84233-61-4 Free baes)

Cat.No: T15647

Synonym: MN 001,KCA 757

Target: Leukotriene Receptor

Cat.No: T30110

Synonym: AR12456,AR-12456

Cat.No: T27915

Synonym: LY-302148,LY302148

Cat.No: T23829

Synonym: Btm1042,Btm-1042

11-deoxy Prostaglandin F1β

Cat.No: T36772

Synonym: 11-deoxy Prostaglandin F1β

D-Mabuterol hydrochloride

Cat.No: T68242

Experimental allergic encephalitogenic peptide (human)

Cat.No: T82424

Parogrelil hydrochloride

Cat.No: T28296

Synonym: INDI-702,NM-702,NT-702,NM702,INDI702

Nirogacestat dihydrobromide

Cat.No: T38266

Prostaglandin F2β

Cat.No: T36621

Cat.No: T32770

Synonym: CV 664

Cat.No: T70106

WAY127093B racemate

Cat.No: T13331

Target: PDE

Cat.No: T67962

Mabuterol, (R)-

Cat.No: T69084

Mabuterol, (S)-

Cat.No: T69085

Cat.No: T60419

11-deoxy Prostaglandin E1

Cat.No: T36770

Synonym: 11-deoxy Prostaglandin E1

11-deoxy Prostaglandin F1α

Cat.No: T36771

Synonym: 11-deoxy Prostaglandin F1α

(R)-(+)-Deoxyarbutin

Cat.No: T83924

Cat.No: T70376

Cat.No: T69215

Methoctramine (hydrate)

Cat.No: T37728

Cat.No: T36618

(-)-Cevimeline hydrochloride hemihydrate

Cat.No: T13421

Synonym: (-)-SNI-2011,(-)-AF102B hydrochloride hemihydrate

Target: ALK

(+)-Cevimeline hydrochloride hemihydrate

Cat.No: T13460

Synonym: (+)-AF102B hydrochloride hemihydrate,(+)-SNI-2011

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
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。
T4953	Neotuberostemonine	NOS	Immunology/Inflammation
	Neotuberostemonine 是一种结核分枝杆菌根中主要的止咳生物碱，能够阻碍巨噬细胞的募集和活化，从而减轻博来霉素 (Bleomycin) 诱导的肺纤维化。
T2S2215	Crebanine	Apoptosis; Others; Akt	Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling
	Crebanine 是来自于韦诺萨千金藤的一种生物碱，通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性，还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。
TN4041	Eupatoriopicrin	Others	Others
	Eupatoriopicrin shows anti-trypanosomal activity and cytotoxicity against Trypanosoma brucei rhodesiense. Eupatoriopicrin-induced DNA damage may play a role in the observed cytotoxicity, it shows a weak sensitizing capacity in guinea pigs.
TN4465	Luvangetin	COX; Prostaglandin Receptor; Antifection	GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience
	Luvangetin may have anti-inflammatory activity, it can inhibit NO and PGE2 production in LPS-stimulated BV2 cells. Luvangetin shows significant protection against pylorus-ligated and aspirin-induced gastric ulcers in rats and cold restraint stress-induced

天然产物

Cat.No: T6S0033

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

Target: Others, FLT, HDAC

Neotuberostemonine

Cat.No: T4953

Target: NOS

Cat.No: T2S2215

Target: Apoptosis, Others, Akt

Eupatoriopicrin

Cat.No: TN4041

Target: Others

Cat.No: TN4465

Target: COX, Prostaglandin Receptor, Antifection

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