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Search Results for " oral bioavailability "

115

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2086	ELN-441958 ELN 441958	Bradykinin Receptor	GPCR/G Protein
	ELN-441958是一种B1受体拮抗剂，能够抑制B1激动剂配体[3H] DAKD 与IMR-90细胞结合(Ki:0.26 nM)，相较于B2受体，它对B1受体的抑制作用具有更高的选择性，且比抑制μ阿片受体选择性高500多倍，比抑制δ阿片受体选择性高2000多倍。
T1770	GNE-9605	LRRK2	Autophagy
	GNE-9605 是一个高效，选择性和能脑渗透的LRRK2抑制剂，IC50为19 nM。
T13099	TC ASK 10	ASK; MAPK	Apoptosis; MAPK
	TC ASK 10 是选择性的，口服有效的细胞凋亡信号调节激酶 1 抑制剂，IC50为 14 nM。它对其他代表性激酶的抑制活性低于 50％，除 ASK2之外 (IC50为 0.51 μM)。
T10606	BRD0705	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	BRD0705 是一种具有旁系选择性的、口服具有活性的GSK3α抑制剂，其 IC50=66 nM，Kd=4.8 μM。它与 GSK3β (其 IC50=515 nM) 相比，对GSK3α的选择性更高 (8 倍)。它可用于研究急性髓细胞性白血病。
TQ0239	PF-06291874 Glucagon receptor antagonists-4	Glucagon Receptor	GPCR/G Protein
	PF-06291874 (Glucagon receptor antagonists-4) 是口服有活性的胰高血糖素受体非肽类拮抗剂。它正用于研究 2 型糖尿病。
T24493	Monoelaidin
	Monoelaidin is a poorly water-soluble drug enhancer of solubility and oral bioavailability.
T9173	HM-30181 mesylate monohydrate	P-gp	Membrane transporter/Ion channel; Neuroscience
	HM-30181 mesylate monohydrate 是一种口服 P-糖蛋白 (P-gp) 抑制剂，用于提高 P-gp 底物药物的口服生物利用度。
T69757	PDDC inhibitor
	PDDC is the first nSMase2 inhibitor that possesses both favorable pharmacodynamics and pharmacokinetic (PK) parameters, including substantial oral bioavailability, brain penetration, and significant inhibition of exosome release from the brain in vivo.
T7897	PK150	Others; Antibacterial	Microbiology/Virology; Others
	PK150 是一种 Sorafenib 类似物，具有抗菌活性。它抑制甲氧西林敏感金黄色葡萄球菌，耐甲氧西林金黄色葡萄球菌，万古霉素中介金黄色葡萄球菌的 MIC 分别为 0.3，0.3-1，0.3 µM。
T7614	Eniluracil GW776C85,5-Ethynyluracil	Others	Others
	Eniluracil (GW776C85) 是不可逆的二氢嘧啶脱氢酶(DPD)抑制剂，是一种尿嘧啶类似物，能够使 5-FU 的口服生物利用度提高到 100%，促进均匀吸收和可预测的毒性。
T8850	sbp-7455	Autophagy	Autophagy
	SBP-7455 是一种高亲和力，可口服的双重ULK1/ULK2自噬抑制剂，可有效抑制ULK1/2酶活性，可研究三阴性乳腺癌，在 ADP-Glo 分析中的IC50分别为 13 nM 和 476 nM。
T9692	Paltusotine	Somatostatin	GPCR/G Protein
	Paltusotine 是一种口服有效的，非肽选择性生长抑素 2 型受体激动剂。在长效生长抑素受体配体作用后，Paltusotine 仍可维持 GH 和 IGF-1 水平。
T26863	BMS-929075 BMS 929075,BMS929075	HCV Protease	Microbiology/Virology; Proteases/Proteasome
	BMS-929075是一种具有口服活性 HCV NS5B 复制酶 (HCV NS5B replicase) 手掌位点变构抑制剂，具有有效性、较高的口服生物利用度和药代动力学参数。BMS-929075 显示出细胞毒性。
TQ0039	(±)-Zanubrutinib (±)-BGB-3111	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	(±)-Zanubrutinib ((±)-BGB-3111) 是一种有效的口服Bruton’s 酪氨酸激酶(Btk)抑制剂，具有优越的口服生物利用度，可实现更高的暴露量和更完整的靶点抑制。
T15409	GNF179	Parasite	Microbiology/Virology
	GNF179 是8,8-二甲基 IP 类似物。它表现出对多药耐药菌株 W2 的效力，具有良好的体外代谢稳定性和体内口服生物相容性。
T3312	AM-2394 AM2394	Glucokinase	Metabolism
	AM-2394 是新型的 glucokinase 激活剂 (GKA)。它能够激活葡萄糖激酶 (GK)，EC50=60 nM。
T60538	SARS-CoV-2-IN-14 3',5-Dichlorosalicylanilide	SARS-CoV	Microbiology/Virology
	SARS-CoV-2-IN-14 是一种有效的、可口服的 SARS-CoV-2 抑制剂（IC50 ：0.39 μM），是一种氯硝柳胺类似物。SARS-CoV-2-IN-14在人血浆和肝 S9 酶测定中比氯硝柳胺稳定性更强。SARS-CoV-2-IN-14以口服的方式给药可以提高其生物利用度和半衰期。
T73447	NP10679
	NP10679 是一种选择性、pH 依赖性的GluN2B 亚基特异的 N-methyl-D-aspartate (NMDA) 受体抑制剂，具有较高的口服生物利用度和良好的脑穿透性。NP10679 在 pH 6.9 和 7.6 下，抑制 GluN2B 的IC50分别为 23 和 142 nM。NP10679 是histamine H1的拮抗剂和hERG 通道抑制剂，IC50分别为 73 和 620 nM。NP10679 是一种可逆的人肝脏CYP 酶抑制剂。
T26690	AVN-101	5-HT Receptor; Adrenergic Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	AVN-101 是一种非常有效的 5-HT7 受体拮抗剂 (Ki = 153 pM)。 AVN-101 还对组胺 H1 (Ki = 0.58 nM) 和肾上腺素能 α2A、α2B 和 α2C (Ki = 0.41-3.6 nM) 受体表现出相当高的亲和力。 AVN-101在中枢神经系统疾病动物模型中显示出良好的口服生物利用度和促进脑血屏障通透性、低毒性和合理的疗效。
T32005	GSK1842799 GSK 1842799
	GSK1842799 is a selective S1P1 receptor agonist with good oral bioavailability.
T70166	Indinavir monohydrate
	Indinavir monohydrate is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
T33763	NVP CXCR2 20 NVP-CXCR2 20,NVP CXCR2-20,NVP CXCR220
	NVP CXCR2 20 is an effective selective CXCR2 antagonist (IC50 = 40 nM) with oral bioavailability.
T10448	Bacampicillin	Others	Others
	Bacampicillin is an improved oral bioavailability penicillin antibiotic which is a prodrug of ampicillin.
T10448L	Bacampicillin hydrochloride	Others	Others
	Bacampicillin hydrochloride is an improved oral bioavailability penicillin antibiotic which is a prodrug of ampicillin.
T16755	RIPK-IN-4	TNF	Apoptosis
	RIPK-IN-4 is an effective and selective inhibitor of RIPK2. It also has excellent oral bioavailability (IC50: 3 nM).
T14500	BAY-1316957	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	BAY-1316957 is a highly potent and selective EP4 receptor antagonist. With an IC50 of 15.3 nM. Good oral bioavailability[1].
T18652	RTC-30	Others	Others
	RTC-30 is an optimized phenothiazine compound possessing potent anti-cancer properties. It is formulated with a hydroxylated linker (N) which enhances its oral bioavailability[1].
T70179	THIQ-40
	THIQ-40 is a novel potent erα antagonist and selective estrogen receptor degrader (serd), exhibiting good oral bioavailability, antitumor efficacy, and serd activity in vivo
T39935	TRPA1-IN-1 TRPA1-IN-1
	TRPA1-IN-1 is a potent, selective antagonist of the TRPA1 channel, demonstrating significant oral bioavailability as a small molecule.
T40280	JH-XVI-178
	JH-XVI-178 is a highly potent and selective CDK8/19 inhibitor with favorable pharmacokinetic attributes, including low clearance and moderate oral bioavailability.
T38990	MGS0274
	MGS0274, an ester-based lipophilic prodrug of the metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, demonstrates enhanced oral bioavailability and holds promise for schizophrenia research applications.
T39442	AM-8123
	AM-8123 is an APJ agonist with high oral bioavailability and potency. It effectively inhibits Forskolin-stimulated cAMP production and activates Gα proteins. This compound is valuable for cardiovascular disease research.
T27374	FR-181877 FR181877,FR 181877
	FR-181877, a nonprostanoid PGI2 agonist, inhibits ADP-induced aggregation of human platelets with an IC50 value of 0.081 microM and has high oral bioavailability (56%) with a long half-life (4.3 h) in rats.
T29151	WAY267464 HCl WAY267464,WAY-267464,WAY 267,464 dihydrochloride,WAY-267,464 dihydrochloride,WAY 267464 dihydrochloride,WAY 267464
	WAY267464 is a nonpeptide small-molecule OT agonists with anxiolytic activity. WAY267464 may be used for modulation of potency, selectivity over the structurally similar vasopressin receptors, CNS penetration, and oral bioavailability.
T38298	Tuberculosis inhibitor 3
	Tuberculosis inhibitor 3 (compound 2i) displays potent anti-TB activity (MIC < 0.016 μg/mL) against drug-sensitive/resistant MTB strains. Tuberculosis inhibitor 3 (compound 2i) shows acceptable PK profiles with oral bioavailability[1].
T11445	GNF179 (Metabolite) GNF179 Metabolite	Others	Others
	GNF179 Metabolite, the derivative of GNF179—an optimized 8,8-dimethyl IP analog—demonstrates significant potency (4.8 nM against the multidrug-resistant W2 strain) alongside in vitro metabolic stability and in vivo oral bioavailability.
T25234	CH5447240 CH 5447240,CH-5447240
	CH5447240 is an effective Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist for the treatment of Hypoparathyroidism. CH5447240 showed a potent in vitro hPTHR1 agonist effect (EC20: 3.0 nM; EC50: 12 nM). It showed 55% oral bioavailability and a signifi
T61637	Anti-inflammatory agent 8
	Anti-inflammatory agent 8 (compound 13) designated as an anti-inflammatory agent 8, displays enhanced activity on the COX-2 enzyme compared to COX-1, with an IC50 value of 0.09 nM. Furthermore, anti-inflammatory agent 8 exhibits oral bioavailability [1].
T61076	Vildagliptin dihydrate
	Vildagliptin dihydrate (LAF237 dihydrate) is a powerful and stable dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating selectivity with an IC50 of 3.5 nM in human Caco-2 cells. This compound exhibits exceptional oral bioavailability and significant antihyperglycemic activity [1].
T74167	PCSK9-IN-3
	PCSK9-IN-3为新一代口服高效三环肽类PCSK9抑制剂，特征为新型化合物。
T11648	INCB 3284	Others	Others
	INCB 3284, a potent and selective human CCR2 antagonist with an oral bioavailability, is utilized in the study of acute liver failure. It effectively inhibits the binding of monocyte chemoattractant protein-1 (MCP-1) to hCCR2, demonstrating an IC50 of 3.7 nM.
T70420	PHA 543613 hydrochloride
	PHA-543613 hydrochloride acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatment for cognitive deficits in schizophrenia.
T68568	Encequidar, HCl
	Encequidar, also known as HM-30181, is an oral P-glycoprotein (P-gp) inhibitor developed to enhance the oral bioavailability of P-gp substrate drugs. Encequidar showed the highest potency (IC(50)=0.63nM) among several MDR1 inhibitors, including cycloporin A, XR9576, and GF120918, and effectively blocked transepithelial transport of paclitaxel in MDCK monolayers (IC(50)=35.4nM). Encequidar is currently under clinical trials.
T30491	BMS 183920 BMS-183920,BMS183920
	BMS-183920 is a diacid, potent angiotensin II receptor antagonist that improves Caco-2 cell permeability and in vivo oral absorption. The relative degree of hydrolysis (biological activation) and prodrug metabolism determines whether substantial improveme
T8795	met-kinase-in-2 1,6-Naphthyridin-4(1H)-one, 5-[[3-fluoro-4-[[7-(2-hydroxy-2-methylpropoxy)-4-quinolinyl]oxy]phenyl]amino]-3-phenyl-
	MET kinase-IN-2 是一种有效的选择性的,具有口服活性的 MET 激酶抑制剂,IC50 值为 7.4 nM。MET kinase-IN-2 具有抗肿瘤活性。
T3430L	(Rac)-PF-4136309（1341224-83-6 Free base) PF-04136309,INCB8761
	PF-4136309（INCB8761, PF-04136309）是一种高效、选择性的口服 CCR2 拮抗剂，具有良好的生物可利用性，其对人CCR2的IC50值为5.2 nM。
T27786	L-796568 dihydrochloride L 796568,L-796568,L796568
	L-796568, is a β3 adrenergic receptor agonist. L-796568 is a potent full beta(3) agonist (EC(50) = 3.6 nM, 94% activation) with >600-fold selectivity over the human beta(1) and beta(2) receptors, which also displays good oral bioavailability in several
T61480	NHE3-IN-3
	NHE3-IN-3 (Compound 1) is a potent inhibitor of the isoform 3 of the Na+/H+ exchanger (NHE3). It exhibits pIC50 values of 6.2 and 6.6 against human and rat NHE3, respectively. Furthermore, NHE3-IN-3 showcases exceptional oral bioavailability of 98% in Sprague–Dawley rats [1].
T61357	EP3 antagonist 3
	EP3 antagonist 3 (compound 2) is a highly effective and specific antagonist of the EP3 receptor. It displays significant oral bioavailability and exhibits a strong pKi value of 8.3. Furthermore, EP3 antagonist 3 possesses excellent pharmacokinetic characteristics, making it a suitable candidate for experimental investigations involving overactive bladder (OAB) research [1].
T61400	Anti-inflammatory agent 9
	Anti-inflammatory agent 9 (compound 28)Anti-inflammatory agent 9 (compound 28) is a benzimidazothiazole derivative derived from tilomisole. It exhibits a higher affinity for the COX-2 enzyme compared to COX-1, thereby demonstrating promising anti-inflammatory properties. Furthermore, it demonstrates oral bioavailability [1].

化合物

Cat.No: T2086

Synonym: ELN 441958

Target: Bradykinin Receptor

Cat.No: T1770

Target: LRRK2

Cat.No: T13099

Target: ASK, MAPK

Cat.No: T10606

Target: GSK-3

Cat.No: TQ0239

Synonym: Glucagon receptor antagonists-4

Target: Glucagon Receptor

Cat.No: T24493

HM-30181 mesylate monohydrate

Cat.No: T9173

Target: P-gp

Cat.No: T69757

Cat.No: T7897

Target: Others, Antibacterial

Cat.No: T7614

Synonym: GW776C85,5-Ethynyluracil

Target: Others

Cat.No: T8850

Target: Autophagy

Cat.No: T9692

Target: Somatostatin

Cat.No: T26863

Synonym: BMS 929075,BMS929075

Target: HCV Protease

(±)-Zanubrutinib

Cat.No: TQ0039

Synonym: (±)-BGB-3111

Target: BTK

Cat.No: T15409

Target: Parasite

Cat.No: T3312

Synonym: AM2394

Target: Glucokinase

SARS-CoV-2-IN-14

Cat.No: T60538

Synonym: 3',5-Dichlorosalicylanilide

Target: SARS-CoV

Cat.No: T73447

Cat.No: T26690

Target: 5-HT Receptor, Adrenergic Receptor, Histamine Receptor

Cat.No: T32005

Synonym: GSK 1842799

Indinavir monohydrate

Cat.No: T70166

Cat.No: T33763

Synonym: NVP-CXCR2 20,NVP CXCR2-20,NVP CXCR220

Cat.No: T10448

Target: Others

Bacampicillin hydrochloride

Cat.No: T10448L

Target: Others

Cat.No: T16755

Target: TNF

Cat.No: T14500

Target: Prostaglandin Receptor

Cat.No: T18652

Target: Others

Cat.No: T70179

Cat.No: T39935

Synonym: TRPA1-IN-1

Cat.No: T40280

Cat.No: T38990

Cat.No: T39442

Cat.No: T27374

Synonym: FR181877,FR 181877

Cat.No: T29151

Synonym: WAY267464,WAY-267464,WAY 267,464 dihydrochloride,WAY-267,464 dihydrochloride,WAY 267464 dihydrochloride,WAY 267464

Tuberculosis inhibitor 3

Cat.No: T38298

GNF179 (Metabolite)

Cat.No: T11445

Synonym: GNF179 Metabolite

Target: Others

Cat.No: T25234

Synonym: CH 5447240,CH-5447240

Anti-inflammatory agent 8

Cat.No: T61637

Vildagliptin dihydrate

Cat.No: T61076

Cat.No: T74167

Cat.No: T11648

Target: Others

PHA 543613 hydrochloride

Cat.No: T70420

Encequidar, HCl

Cat.No: T68568

Cat.No: T30491

Synonym: BMS-183920,BMS183920

met-kinase-in-2

Cat.No: T8795

Synonym: 1,6-Naphthyridin-4(1H)-one, 5-[[3-fluoro-4-[[7-(2-hydroxy-2-methylpropoxy)-4-quinolinyl]oxy]phenyl]amino]-3-phenyl-

(Rac)-PF-4136309（1341224-83-6 Free base)

Cat.No: T3430L

Synonym: PF-04136309,INCB8761

L-796568 dihydrochloride

Cat.No: T27786

Synonym: L 796568,L-796568,L796568

Cat.No: T61480

EP3 antagonist 3

Cat.No: T61357

Anti-inflammatory agent 9

Cat.No: T61400

Cat. No.	Product Name	Target	Signaling Pathways
TN1918	Medicarpin 美迪紫檀素	Apoptosis; BCL; ROS; JNK	Apoptosis; Immunology/Inflammation; MAPK
	Medicarpin 是从紫花苜蓿中分离出的一种类黄酮。它通过调节 P-gp 介导的药物外流，诱导白血病 P388 细胞凋亡并克服多药耐药性。

天然产物

Cat.No: TN1918

Synonym: 美迪紫檀素

Target: Apoptosis, BCL, ROS, JNK

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