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17

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T0099	Tolterodine tartrate Detrol LA,PNU-200583E,Kabi-2234,酒石酸托特罗定	AChR	Neuroscience
	Tolterodine tartrate (PNU-200583E) 是毒蕈碱受体的有效拮抗剂。它在体内显示出对膀胱和唾液腺的选择性。
T4579	Pentagastrin 五肽胃泌素,ICI-50123	Others; cholecystokinin	GPCR/G Protein; Others
	Pentagastrin (ICI-50123) 是一种选择性的胆囊收缩素 B(CCKB) 受体激动剂，IC50=11 nM。它能够增强胃粘膜对酸的防御机制，并保护胃粘膜免受损伤。
T38089	2F-Peracetyl-Fucose 1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos	Others	Others
	2F-Peracetyl-Fucose (1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) 是一种有效的岩藻糖基转移酶 (FUT)抑制剂，在体外炎症模型中抑制唾液酸化和岩藻糖基化。
T8832	Eledoisin trifluoroacetate (69-25-0 free base) Eledoisin trifluoroacetate	Others	Others
	Eledoisin trifluoroacetate (69-25-0 free base) 是从某些小章鱼（Eledone spp.，Mollusca）的后唾液腺中提取或合成获得的肽。它的作用类似于 P 物质的作用；它是一种有效的血管扩张剂，可增加毛细血管的通透性。
T25913L	P-113 acetate	HIV Protease; Antibacterial; Antibiotic	Microbiology/Virology; Proteases/Proteasome
	P-113 acetate 是一种源自人类唾液蛋白组氨酸 5 的抗菌肽 (AMP)，在患有口腔念珠菌病的牙龈炎和人类免疫缺陷病毒 (HIV) 患者中显示出良好的安全性和有效性。
T9417L	gamma-preprotachykinin amide (72-92) acetate gamma-preprotachykinin amide (72-92) acetate (114882-65-4 Free base)	Others	Others
	gamma-preprotachykinin amide (72-92) acetate 是一种 21 个氨基酸的肽，属于速激肽 (TK) 家族，在其 C 末端序列中包括神经激肽 A (NKA)。它对中枢 NK-2 受体的亲和力高于 NKA；它对 NK-1 受体的亲和力较低，但是，它有效地刺激唾液分泌，这是由 NK-1 受体激活介导的。
T21119	Cevimeline AF-102B,西维美林,FKS 508,SNI 2011,HSDB 7286
	Cevimeline, a parasympathomimetic and muscarinic agonist, affects M1 and M3 receptors. Cevimeline has been shown to treat dry mouth and Sj gren's syndrome. It is also used to reduce Xerostomia symptoms and increase salivary flow in head and neck cancer survivors after radiotherapy.
T20131	Cevimeline hydrochloride 盐酸西维美林,Cevimeline HCl,Evoxac
	Cevimeline HCl is an agonist of cholinergic that binds to muscarinic receptors. Muscarinic agonists in sufficient dosage can enhance the secretion of exocrine glands, such as salivary and sweat glands.
TP1741	Histatin 5
	Histatin 5 inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively. Histatin 5 is a human basic salivary peptide with strong fungicidal properties in vitro.
T78627	Chinese gallotannin	Others	Others
	Chinese gallotannin，一种非特异性α-amylase抑制剂，对人唾液α-淀粉酶具有较强的抑制作用，其Ki值为0.82 μg/mL。此化合物可用于糖尿病研究。
T16547	PK14105	Others	Others
	PK14105 has been evaluated biologically as a potential radioligand for positron emission tomography (PET) studies targeting peripheral benzodiazepine binding sites (PBBS) receptors. When administered to rats with unilaterally lesioned striata, PK14105 was observed to quickly cross the blood-brain barrier, displaying significant radioactivity retention in the lesioned striatum, in contrast to the unlesioned striatum or cerebellar vermis. Additionally, PK14105 has the capability to inhibit recepto...
T82217	Helospectin I
	Helospectin I属于血管活性肠肽(VIP)家族的一种神经肽，能够引起血管扩张，具有抗高血压效果，可用于降低血压。该化合物最早是从Heloderma suspectum蜥蜴的唾液腺毒液中分离得到。
T37834	G3-CNP
	G3-CNP is a colorimetric substrate for α-amylases.1Upon hydrolysis by α-amylases, 2-chloro-4-nitrophenol is released which can be quantified by colorimetric detection at 405 nm as a measure of enzyme activity. G3-CNP has been used to characterize the activity of human pancreatic or salivary amylase.
T76467	Acetyl-Adhesin (1025-1044) amide
	Acetyl-Adhesin (1025-1044) amide，为变形链球菌细胞表面粘连蛋白20肽段，充当抗菌肽，特异性阻止粘连素同唾液受体结合，避免变形链球菌再定植。
T82216	Helospectin II
	Helospectin II，一种属于血管活性肠肽（VIP）家族的神经肽，具备血管扩张作用及抗高血压活性，能够降低血压。该化合物最初从蜥蜴Heloderma suspectum的唾液腺毒液中分离得到。
T83715	Histatin 3 TFA Hst-3
	Histatin 3, 一种唾液抗菌肽，对C. albicans具有活性（LC50 = 9.2 µM）。在12 µM浓度下，还能在无细胞测定中诱导肌动蛋白聚合。
T83689	Histatin 8 TFA Hst-8
	Histatin 8是一种唾液抗微生物肽，是histatin 3和histatin 5的蛋白水解片段。针对A. baumannii（包括对colistin敏感或耐药的菌株）在32 µg/ml浓度下显示活性。Histatin 8也对C. albicans和C. tropicalis显示活性（MICs分别为1和5 mg/ml）。

化合物

Tolterodine tartrate

Cat.No: T0099

Synonym: Detrol LA,PNU-200583E,Kabi-2234,酒石酸托特罗定

Target: AChR

Cat.No: T4579

Synonym: 五肽胃泌素,ICI-50123

Target: Others, cholecystokinin

2F-Peracetyl-Fucose

Cat.No: T38089

Synonym: 1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos

Target: Others

Eledoisin trifluoroacetate (69-25-0 free base)

Cat.No: T8832

Synonym: Eledoisin trifluoroacetate

Target: Others

Cat.No: T25913L

Target: HIV Protease, Antibacterial, Antibiotic

gamma-preprotachykinin amide (72-92) acetate

Cat.No: T9417L

Synonym: gamma-preprotachykinin amide (72-92) acetate (114882-65-4 Free base)

Target: Others

Cat.No: T21119

Synonym: AF-102B,西维美林,FKS 508,SNI 2011,HSDB 7286

Cevimeline hydrochloride

Cat.No: T20131

Synonym: 盐酸西维美林,Cevimeline HCl,Evoxac

Cat.No: TP1741

Chinese gallotannin

Cat.No: T78627

Target: Others

Cat.No: T16547

Target: Others

Cat.No: T82217

Cat.No: T37834

Acetyl-Adhesin (1025-1044) amide

Cat.No: T76467

Cat.No: T82216

Cat.No: T83715

Synonym: Hst-3

Cat.No: T83689

Synonym: Hst-8

Cat. No.	Product Name	Target	Signaling Pathways
T0962	L-Hyoscyamine Daturine,Hyoscyamine,L-莨菪碱,L-天仙子胺	AChR	Neuroscience
	L-Hyoscyamine (Daturine) 是从山莨菪中提取的一种托烷生物碱，是竞争性的毒蕈碱受体拮抗剂。它是 Atropine 的左旋异构体。
T4S1619	L-Hyoscyamine sulfate Hyoscyamine sulfate hydrate,Levsin Sulfate,Hyoscyamine Sulphate,硫酸天仙子胺水合物,L-莨菪碱硫酸盐	AChR	Neuroscience
	L-Hyoscyamine sulfate (Levsin Sulfate) 是来自山莨菪的一种托烷生物碱，是竞争性的毒蕈碱受体拮抗剂。它是 Atropine 的左旋异构体。

天然产物

Cat.No: T0962

Synonym: Daturine,Hyoscyamine,L-莨菪碱,L-天仙子胺

Target: AChR

L-Hyoscyamine sulfate

Cat.No: T4S1619

Synonym: Hyoscyamine sulfate hydrate,Levsin Sulfate,Hyoscyamine Sulphate,硫酸天仙子胺水合物,L-莨菪碱硫酸盐

Target: AChR

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