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26

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1576	Iopamidol SQ-13396,Niopam,Iopamiron,Iopamiro,碘帕醇,B-15000,Isovue	Others	Others
	Iopamidol (SQ-13396) 是一种 benzenedicarboxamide 化合物。它具有放射性不透明介质、环境污染物和异种生物的作用。
T13675	Elacestrant dihydrochloride RAD1901 dihydrochloride	Estrogen/progestogen Receptor	Endocrinology/Hormones
	Elacestrant dihydrochloride (DA-DKRAD1901 dihydrochloride) 是一种具有口服活性的的选择性雌激素受体 (ER) 降解剂 (SERD)，能够作用于 ERα (IC50:48 nM) 和 ERβ (IC50:870 nM)。
T13674	Elacestrant 依拉司群,RAD1901	Estrogen Receptor/ERR; Estrogen/progestogen Receptor	Endocrinology/Hormones
	Elacestrant (RAD1901) 是一种具有口服活性的、选择性的雌激素受体 (ER) 降解剂 (SERD)，能够作用于 ERα (IC50:48 nM)和 ERβ (IC50:870 nM)。
T6249	Avagacestat BMS-708163	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	Avagacestat (BMS-708163) 是一种有效的γ-secretase 抑制剂，抑制 Aβ42 (IC50:0.27 nM) 和 Aβ40 (IC50:0.30 nM) 的产生。它同时抑制 Notch 胞内结构域 (NICD) (IC50:0.84 nM) 和 CYP2C19 (IC50:20 nM) 。它可用于阿尔兹海默症的研究。
TQ0238	Lanabecestat LY3314814,AZD3293	BACE	Neuroscience
	Lanabecestat (AZD3293) 是一种具有高效性和高渗透性、口服活性且可穿过血脑屏障的 BACE1 抑制剂（Ki：0.4 nM），Lanabecestat 可用于研究像阿尔茨海默症类的神经系统疾病。
T11175	Elenbecestat E2609	Beta-Secretase; BACE	Neuroscience
	Elenbecestat (E2609) 是一种高效、有口服活性的，能透过 CNS 的 BACE-1抑制剂，它有用于阿尔茨海默病 (AD) 的研究潜力。
T13253	Umibecestat CNP520	BACE	Neuroscience
	Umibecestat 是一种β-位点淀粉样前体蛋白裂解酶-1 (BACE-1) 抑制剂，对人 BACE-1 和小鼠 BACE-1 的 IC50 分别为 11 nM 和 10 nM，可用于阿尔茨海默病的研究。
T3633	Crenigacestat LY3039478	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	Crenigacestat (LY3039478) 是一种口服具有活性的Notch 和γ-secretase 的抑制剂，其在多种肿瘤细胞中的IC50为 ∼1nM。
T7011	Verubecestat MK-8931,维罗司他	Beta-Secretase; BACE	Neuroscience
	Verubecestat (MK-8931) 是一种高亲和力的、具有口服活性的BACE1和BACE2抑制剂，Ki 分别为 2.2 nM 和 0.38 nM。它可以有效降低 Aβ40，并具有潜力用于阿尔茨海默氏病。
T6125	Semagacestat LY450139,塞美司他	Beta Amyloid; Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	Semagacestat (LY450139) 是一种γ-secretase 抑制剂，抑制β-amyloid(Aβ42)，Aβ38和Aβ40，IC50分别为 10.9，12 和 12.1 nM，可用于研究阿尔茨海默病。
T6935	Nirogacestat PF-03084014,PF-3084014,PF03084014,PF 03084014	Apoptosis; Gamma-secretase	Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells
	Nirogacestat (PF 03084014) 是一种具有口服活性的，可逆的，非竞争性的，选择性γ-secretase 抑制剂，IC50为 6.2 nM。它抑制 Notch 信号通路，可研究 Notch 受体依赖性肿瘤。
T70800	Elenbecestat free base
	Elenbecestat,also known as E2609 is a BACE1 inhibitor. By inhibiting BACE, a key enzyme in the production of Aβ peptides, E2609 decreases the formation of these peptides which can aggregate into toxic oligomers and protofibrils and eventually form amyloid plaques in the brain. Elenbecestat has been shown to reduce Aβ levels in cerebrospinal fluid, was investigated in two global phase 3 studies in early AD.
T69664	Umibecestat HCl
	Umibecestat, also known as CNP-520, is a beta-secretase inhibitor and is a drug candidate for prevention trials in Alzheimer's disease. CNP520 has a selectivity, pharmacodynamics, and distribution profile suitable for AD prevention studies. CNP520 reduced brain and cerebrospinal fluid (CSF) Aβ in rats and dogs, and Aβ plaque deposition in APP-transgenic mice. CNP520 reduces Aβ load and neuroinflammation in APP‐transgenic mice
T125754	Cesternoside A
	Cesternoside A 是一种有用的有机化合物，可用于生命科学领域的相关研究。其产品编号为 T125754，CAS号为 153120-71-9。
T24924	Umibecestat HCl (1387560-01-1 free base) CNP 520,Umibecestat HCl,Umibecestat hydrochloride,CNP520,CNP-520
	Umibecestat is a beta-secretase inhibitor. CNP520 has a selectivity, pharmacodynamics, and distribution profile suitable for AD prevention studies.
T14338	Atabecestat JNJ-54861911	BACE	Neuroscience
	Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction and it is tolerated and displays a sustained pharmacokinetic (PK) and
T10014	(1α,1'S,4β)-Lanabecestat (1α,1'S,4β)-AZD3293	Others	Others
	(1α,1'S,4β)-Lanabecestat is a Beta site APP Cleaving Enzymel (BACE1) inhibitor, and has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively.
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
T23874	CESTRIN
	CESTRIN is a cellulose synthase trafficking probe that acts by inhibiting cellulose deposition and interferes with the trafficking of cellulose synthase complexes and their associated proteins KORRIGAN1 and POM2/CSI1.
T70807	Lanabecestat HCl
	Lanabecestat, also known as AZD3293 and LY3314814, is a potent, highly permeable, orally active, blood-brain barrier (BBB) penetrating, BACE1 inhibitor with unique slow off-rate kinetics. AZD3293 displayed significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ.
T11173	Elacestrant S enantiomer RAD1901 S enantiomer	Others	Others
	Elacestrant S enantiomer is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
T14525	Begacestat GSI-953	Beta Amyloid	Neuroscience
	Begacestat is a selective thiophene sulfonamide amyloid precursor protein gamma-secretase inhibitor (Aβ40,IC50=15 nM),and for the treatment of Alzheimer's disease.
T11173L	Elacestrant S enantiomer dihydrochloride RAD1901 S enantiomer dihydrochloride,RAD-1901 S enantiomer dihydrochloride,RAD 1901 S enantiomer dihydrochloride	Others	Others
	Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant S enantiomer dihydrochloride is an low activity enantiomer of elacestrant dihydrochloride.
T25610	Lanabecestat camsylate LY 3314814 camsylate,LY-3314814 camsylate,LY3314814 camsylate
	Lanabecestat camsylate is used as a BACE1 Inhibitor.
T70104	Verubecestat tosylate
	Verubecestat, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients.
T71899	Verubecestat TFA
	Verubecestat, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients.

化合物

Cat.No: T1576

Synonym: SQ-13396,Niopam,Iopamiron,Iopamiro,碘帕醇,B-15000,Isovue

Target: Others

Elacestrant dihydrochloride

Cat.No: T13675

Synonym: RAD1901 dihydrochloride

Target: Estrogen/progestogen Receptor

Cat.No: T13674

Synonym: 依拉司群,RAD1901

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor

Cat.No: T6249

Synonym: BMS-708163

Target: Gamma-secretase

Cat.No: TQ0238

Synonym: LY3314814,AZD3293

Target: BACE

Cat.No: T11175

Synonym: E2609

Target: Beta-Secretase, BACE

Cat.No: T13253

Synonym: CNP520

Target: BACE

Cat.No: T3633

Synonym: LY3039478

Target: Gamma-secretase

Cat.No: T7011

Synonym: MK-8931,维罗司他

Target: Beta-Secretase, BACE

Cat.No: T6125

Synonym: LY450139,塞美司他

Target: Beta Amyloid, Gamma-secretase

Cat.No: T6935

Synonym: PF-03084014,PF-3084014,PF03084014,PF 03084014

Target: Apoptosis, Gamma-secretase

Elenbecestat free base

Cat.No: T70800

Umibecestat HCl

Cat.No: T69664

Cesternoside A

Cat.No: T125754

Umibecestat HCl (1387560-01-1 free base)

Cat.No: T24924

Synonym: CNP 520,Umibecestat HCl,Umibecestat hydrochloride,CNP520,CNP-520

Cat.No: T14338

Synonym: JNJ-54861911

Target: BACE

(1α,1'S,4β)-Lanabecestat

Cat.No: T10014

Synonym: (1α,1'S,4β)-AZD3293

Target: Others

Nirogacestat dihydrobromide

Cat.No: T38266

Cat.No: T23874

Lanabecestat HCl

Cat.No: T70807

Elacestrant S enantiomer

Cat.No: T11173

Synonym: RAD1901 S enantiomer

Target: Others

Cat.No: T14525

Synonym: GSI-953

Target: Beta Amyloid

Elacestrant S enantiomer dihydrochloride

Cat.No: T11173L

Synonym: RAD1901 S enantiomer dihydrochloride,RAD-1901 S enantiomer dihydrochloride,RAD 1901 S enantiomer dihydrochloride

Target: Others

Lanabecestat camsylate

Cat.No: T25610

Synonym: LY 3314814 camsylate,LY-3314814 camsylate,LY3314814 camsylate

Verubecestat tosylate

Cat.No: T70104

Verubecestat TFA

Cat.No: T71899

Cat. No.	Product Name	Target	Signaling Pathways
T75465	Mycestericin G
	Mycestericin G 是一种鞘氨醇样真菌代谢产物，具有免疫抑制活性。
T81735	Mycestericin C
	Mycestericin C, 分离自 Mycelia sterilia ATCC 20349 的培养液, 能在小鼠同种异体混合淋巴细胞反应中抑制淋巴细胞的增殖。

天然产物

Cat.No: T75465

Cat.No: T81735

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