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29

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12137	N-(2-Hydroxypropyl)methacrylamide	Parasite	Microbiology/Virology
	N-(2-Hydroxypropyl)methacrylamide 用于合成共聚物，用于靶向递送内脏利什曼病中的抗寄生虫剂。
T5491	GSK3179106	c-RET	Apoptosis; Tyrosine Kinase/Adaptors
	GSK3179106 是选择性的、具有口服活性的RET 激酶抑制剂，对人和大鼠 RET 的 IC50 分别为 0.4 nM 和 0.2 nM。它能够减轻炎症后和应激引起的内脏超敏反应，对肠易激综合征具有潜在的应用价值。
T2525	Alosetron hydrochloride Lotronex,盐酸阿洛司琼,GR 68755C,GR 68755,GR 68755X	5-HT Receptor	GPCR/G Protein; Neuroscience
	Alosetron hydrochloride (GR 68755) 是一种高选择性的 5-HT3 受体拮抗剂，可减轻清醒或麻醉犬直肠扩张的内脏伤害性效应，具有抗炎活性，用于肠易激综合征的研究。它阻断 5HT3 介导的豚鼠肌间和粘膜下神经元的快速去极化，IC50约为 55 nM。
T39746	DNDI-6148
	DNDI-6148 is a novel preclinical candidate for the treatment of visceral leishmaniasis.
T0033	Miltefosine HePC,米替福新,Hexadecyl phosphocholine	Akt; HIV Protease; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Miltefosine (HePC) 是一种广谱抗微生物剂，是治疗内脏和皮肤利什曼病的药物。它是 CTP 磷酸胆碱胞苷基转移酶的抑制剂。
T33846	Oxyphenonium bromide Spasmophen,Oxifenon,奥芬溴铵,Oxyfenon,Atrenyl,Oxyphenon	Others	Others
	Oxyphenonium bromide (Oxyfenon) 具有抗胆碱能活性，可用于治疗胃和十二指肠溃疡以及缓解内脏痉挛的研究。
T7295	Miridesap Ro63-8695,CPHPC,GSK2315698	Others	Others
	Miridesap (GSK2315698) 是一种血清淀粉样蛋白 P 组分 (SAP) 的配体，能够利用肝脏清除导致循环 SAP 的快速消耗。它也可以明显减少脑脊液和内脏淀粉样蛋白沉积物中的 SAP。
T16448	PD173212	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	PD 173212是一种阻断 N-型电压敏感性钙通道 (N-type voltage sensitive calcium channel, Cav2.2)的阻滞剂。PD173212的腹腔注射给药(0.0017-1.7 μmol/kg)显著降低了2,4-二硝基苯磺酸(DNBS)诱导结肠炎小鼠的内脏超敏反应。
T39214L	LXE408 fumarate LXE408 fumarate (1799330-15-6 Free base)	Proteasome	Proteases/Proteasome; Ubiquitination
	LXE408 fumarate 是一种口服有效的，非竞争性的，动素体选择性蛋白酶体 (proteasome) 抑制剂。LXE408 fumarate 抑制 L. donovani 蛋白酶体 (IC50=0.04 μM) 和 L. donovani (EC50=0.04 μM)。LXE408 fumarate 具有较弱的透过血脑屏障能力。LXE408 fumarate 具有用于内脏利什曼病 (VL) 研究的潜力。
TP1057L	Phe-Met-Arg-Phe Like Peptide acetate Pqdpflrfamide acetate,Phe-Met-Arg-Phe Like Peptide acetate（98495-35-3 free base)	Others	Others
	Phe-Met-Arg-Phe Like Peptide acetate (Pqdpflrfamide acetate)(98495-35-3 free base) 是一种来自蜗牛 Helix aspersa 的内脏和躯体肌肉的 FMRF 样肽。 FMRF (Phe-Met-Arg-Phe) 是一种由 4 个氨基酸残基组成的神经肽肽。
T37427	(2R/S)-6-PNG 6-Prenylnaringenin,(±)-6-Prenylnaringenin	Calcium Channel; HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism
	(2R/S)-6-PNG (6-Prenylnaringenin) 是新型天然组蛋白脱乙酰酶抑制剂，具有抗癌抗肿瘤活性，可阻断T型钙通道可减轻小鼠的神经性和内脏疼痛。
T71716	Nav1.1-IN-B
	Nav1.1-IN-B is a selective NaV1.1 inhibitor which reduces visceral hypersensitivity.
TP1057	Phe-Met-Arg-Phe Like Peptide, Snail Helix aspersa Phe-Met-Arg-Phe Like Peptide
	Phe-Met-Arg-Phe-like peptide, derived from the visceral and somatic muscles of the snail Helix aspersa, is a neuropeptide known as FMRF (Phe-Met-Arg-Phe). This peptide comprises four amino acid residues[1].
T71308	DSP-6952
	DSP-6952 is a 5-HT4 receptor partial agonist, inhibiting visceral hypersensitivity and ameliorating gastrointestinal dysfunction.
T28346	PD-217014 HCl PD 217014,PD217014,PD-217,014,PD-217014
	PD-217014 is a GABA analog. It inhibits (3)H-gabapentin binding to alpha(2)delta subunit of voltage-gated calcium channels in a concentration-dependent manner (K(i) = 18 nmol/l). PD-217014 possesses visceral analgesic activity.
T12970L	Solabegron HCl GW-427,353,GW427353,GW-427353,GW 427,353,GW427,353
	Solabegron (GW-427,353), is a selective agonist of β3 adrenergic receptors. In addition, Solabegron has been shown to produce visceral analgesia by releasing somatostatin from fat cells.
T33637	Neostibosan Stibanilic acid,693B,Astaril,Ethylstibamine,p-Aminobenzenestibonic acid,Bayer 693
	Neostibosan is an arsenic-containing parasitic agent. Due to the activity of arsenic on visceral L/Ashmaniasis, one of the pentvalent antimony, which is less toxic, is synthesized and has potential activity on tumor cells.
T39214	LXE408 LXE408
	LXE408 is an orally active, kinetoplastid-selective proteasome inhibitor, exhibiting non-competitive inhibitory effects. It demonstrates an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. Moreover, LXE408 shows limited ability to traverse the blood-brain barrier. Hence, LXE408 holds promise for advancing research in the field of visceral leishmaniasis (VL).
T11661	INT-767	FXR; GPCR19	GPCR/G Protein; Metabolism
	INT-767 是一种高效的法尼类固醇 X 受体 (FXR)/TGR5 双激动剂，可预防 NASH 并促进内脏脂肪棕色脂肪生成和线粒体功能，可用于研究非酒精性脂肪性肝炎。
T35374L	(Ala13)-Apelin-13 acetate	Apelin receptor	GPCR/G Protein
	(Ala13)-Apelin-13 acetate，一种 APJ 拮抗剂，可调节CRF 诱导的增强的结肠运动、内脏敏感性和肠屏障。
T41183	Helianorphin-19
	Helianorphin-19 is a high affinity, potent and selective κ-opioid receptor (KOR) agonist (Ki = 25 nM; EC50= 45 nM). Helianorphin-19 exhibits approximately 200-fold selectivity for KOR over μ and δ-opioid receptors.In vivoHelianorphin-19 shows potent peripheral analgesic efficacy in a mouse model of visceral pain without affecting motor coordination/sedation.
T63186	Cav 3.2 inhibitor 1
	Cav 3.2 inhibitor 1为T型钙离子通道(calcium channel)抑制剂，其与多巴胺受体(D2 receptor)的结合亲和力较低，主要应用于研究身体和内脏疼痛。
T78559	PDE7-IN-3
	PDE7-IN-3（例2）是一种具有潜在镇痛活性的PDE7磷酸二酯酶抑制剂，可用于探究炎性、神经性、内脏性及伤害性疼痛。
T63606	Cav 3.2 inhibitor 2
	Cav 3.2 inhibitor 2 是一种 Cav3.2 T-type Ca2+channels 的抑制剂，-80mV 恒定电位下，其IC50=0.09339 μM。Cav 3.2 inhibitor 2 对小鼠 T 通道依赖性的躯体和内脏疼痛表现出有效的抑制作用。Cav 3.2 inhibitor 2 能够用于研究顽固性疼痛。
T71476	Afegostat TFA
	Afegostat, aslo known as Isofagomine, and AT2101, was an experimental drug for the treatment of certain forms of Gaucher's disease. Isofagomine (IFG) is an acid β-glucosidase (GCase) active site inhibitor that acts as a pharmacological chaperone. FG inhibits GCase with K(i) ~30 nM for wild-type and mutant enzymes (N370S and V394L). Administration of IFG (30 mg/kg/day) to the mice homozygous for GCase mutations (V394L, D409H, or D409V) led to increased GCase activity in visceral tissues and brain...
T76127	Urocortin II, mouse
	Urocortin II, mouse 是一种选择性的 2 型促肾上腺皮质激素释放因子 (CRF2) 受体内源性多肽激动剂，对CRFR2和CRFR1的Ki 值分别为 0.66 nM 和 ﹥100 nM。Urocortin II, mouse 通过以 cAMP/PKA 和 Ca2+/CaMKII 依赖性方式激活 CRF2 受体。Urocortin II, mouse 在中枢神经系统的离散区域表达，并激活参与内脏感觉信息处理和调节自主神经外流的中枢神经元。
T65387	Paromomycin, sulfate (1:1)
	Paromomycin (Sulfate Salt) is an aminoglycoside that is active against Gram-negative and many Gram-positive bacteria as well as some protozoa and cestodes. Paromomycin in combination with sodium stibogluconate has proven to be effective in African and Indian VL (visceral leishmaniasis) and improves survival in African VL[3]. PS (Paromomycin Sulfate) is effective for elimination of B. coli without hematological side effects[4]. The activity of phosphoglucose isomerase was slightly inhibited by 10...
T83802	TNP-ATP sodium
	TNP-ATP是ATP的衍生物，同时是嘌呤P2Y1、P2X3和P2X2/3受体的拮抗剂（IC50s分别为6、0.9和7 nM，在表达人类受体的HEK293细胞中）。该化合物相对于嘌呤P2X2、P2X4和P2X7受体显示出选择性（IC50s分别为2、15.2和>30 µM，在表达人类受体的HEK293细胞中）。TNP-ATP能降低表达P2X3和P2X2/3受体的1321N1细胞中乙酸诱导的钙流量（IC50s分别为100和62 nM）。它还可以减轻小鼠模型中由乙酸诱发的痛性绞曲（ED50 = 6.35 µmol/kg）。在403 nm激发下，其发射最大峰值为547 nm，当结合于胰岛素降解酶（IDE）时，其相对荧光强度增加四倍，并且发射峰移至538 nm。
T36373	Urocortin II (mouse) (trifluoroacetate salt)
	Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF...

化合物

N-(2-Hydroxypropyl)methacrylamide

Cat.No: T12137

Target: Parasite

Cat.No: T5491

Target: c-RET

Alosetron hydrochloride

Cat.No: T2525

Synonym: Lotronex,盐酸阿洛司琼,GR 68755C,GR 68755,GR 68755X

Target: 5-HT Receptor

Cat.No: T39746

Cat.No: T0033

Synonym: HePC,米替福新,Hexadecyl phosphocholine

Target: Akt, HIV Protease, PKC

Oxyphenonium bromide

Cat.No: T33846

Synonym: Spasmophen,Oxifenon,奥芬溴铵,Oxyfenon,Atrenyl,Oxyphenon

Target: Others

Cat.No: T7295

Synonym: Ro63-8695,CPHPC,GSK2315698

Target: Others

Cat.No: T16448

Target: Calcium Channel

LXE408 fumarate

Cat.No: T39214L

Synonym: LXE408 fumarate (1799330-15-6 Free base)

Target: Proteasome

Phe-Met-Arg-Phe Like Peptide acetate

Cat.No: TP1057L

Synonym: Pqdpflrfamide acetate,Phe-Met-Arg-Phe Like Peptide acetate（98495-35-3 free base)

Target: Others

Cat.No: T37427

Synonym: 6-Prenylnaringenin,(±)-6-Prenylnaringenin

Target: Calcium Channel, HDAC

Cat.No: T71716

Phe-Met-Arg-Phe Like Peptide, Snail Helix aspersa

Cat.No: TP1057

Synonym: Phe-Met-Arg-Phe Like Peptide

Cat.No: T71308

Cat.No: T28346

Synonym: PD 217014,PD217014,PD-217,014,PD-217014

Cat.No: T12970L

Synonym: GW-427,353,GW427353,GW-427353,GW 427,353,GW427,353

Cat.No: T33637

Synonym: Stibanilic acid,693B,Astaril,Ethylstibamine,p-Aminobenzenestibonic acid,Bayer 693

Cat.No: T39214

Synonym: LXE408

Cat.No: T11661

Target: FXR, GPCR19

(Ala13)-Apelin-13 acetate

Cat.No: T35374L

Target: Apelin receptor

Helianorphin-19

Cat.No: T41183

Cav 3.2 inhibitor 1

Cat.No: T63186

Cat.No: T78559

Cav 3.2 inhibitor 2

Cat.No: T63606

Cat.No: T71476

Urocortin II, mouse

Cat.No: T76127

Paromomycin, sulfate (1:1)

Cat.No: T65387

Cat.No: T83802

Urocortin II (mouse) (trifluoroacetate salt)

Cat.No: T36373

Cat. No.	Product Name	Target	Signaling Pathways
T20225	Dicentrine, (-)- L-Dicentrine,荷包牡丹碱,NSC 251699,NSC251699,NSC-251699	Others	Others
	Dicentrine, (-)- (NSC-251699) 是一种在几种植物物种中发现的非卟啉生物碱，在小鼠内脏痛的急性模型中显示出显著的镇痛活性。
TN6791	Palvanil Hexadecanamide	TRP/TRPV Channel	Membrane transporter/Ion channel
	Palvanil (Hexadecanamide) 是一种快速脱敏的 TRPV1 激动剂。它可能是治疗 IBS 的有前途的药物，因为它可以调节肠道蠕动并减轻内脏疼痛。
T2P2923	Stearic acid 硬脂酸,Isostearic acid,Octadecanoic acid,Cetylacetic acid	Phosphatase; Endogenous Metabolite	Metabolism
	Stearic acid (Cetylacetic acid) 是长链饱和脂肪酸，存在于许多动植物油脂中。
TN3568	Calceolarioside A	Calcium Channel; Antifection	Membrane transporter/Ion channel; Metabolism; Microbiology/Virology
	Calceolarioside A shows potent activity against visceral leishmaniasis. It can induce a dose-related aggregant effect on rabbit platelets, which may be partly related to a calcium-dependent mechanism. Calceolarioside A also has potent antioxidative activi

天然产物

Dicentrine, (-)-

Cat.No: T20225

Synonym: L-Dicentrine,荷包牡丹碱,NSC 251699,NSC251699,NSC-251699

Target: Others

Cat.No: TN6791

Synonym: Hexadecanamide

Target: TRP/TRPV Channel

Cat.No: T2P2923

Synonym: 硬脂酸,Isostearic acid,Octadecanoic acid,Cetylacetic acid

Target: Phosphatase, Endogenous Metabolite

Calceolarioside A

Cat.No: TN3568

Target: Calcium Channel, Antifection

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