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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。
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。
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。
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。
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.
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。
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.
T39787	KRH-3955 hydrochloride
	KRH-3955 hydrochloride is a CXCR4 antagonist with oral bioavailability. It effectively inhibits the binding of SDF-1α to CXCR4, exhibiting an IC 50 of 0.61 nM. Additionally, KRH-3955 hydrochloride displays high potency and selectivity as an inhibitor of X4 HIV-1, with an EC 50 ranging from 0.3 to 1.0 nM.
T78744	IRAK4-IN-24	IRAK	Immunology/Inflammation; NF-κB
	IRAK4-IN-24（compound 16）是IRAK4高效抑制剂，显示高Cl及较低口服生物可用性，适用于炎症与自身免疫性疾病研究。
T14191	Alpelisib hydrochloride BYL-719 hydrochloride	Others	Others
	Alpelisib hydrochloride (BYL-719 hydrochloride) shows antineoplastic activity[1][2]. Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ,
T70951	ELND006
	ELND006 is a novel gamma secretase inhibitor previously under investigation for the oral treatment of Alzheimer's disease. ELND006 shows poor solubility and has moderate to high permeability. The in vivo performance of the ELND006 nanosuspension was tested in fed and fasted beagle dogs and compared with a gelatin capsule containing reference API. The results show that nanosizing ELND006 profoundly improved the oral bioavailability and virtually eliminated variation resulting from food intake.
T38910	mGluR2 antagonist 1
	mGluR2 antagonist 1 is a potent and selective class of negative allosteric modulator targeting the metabotropic glutamate receptor 2 (mGluR2) with high oral bioavailability. It displays a remarkable affinity for mGluR2, with an IC50 value of 9 nM. Furthermore, it exhibits excellent permeability across the blood-brain barrier, making it a promising candidate for central nervous system-related studies or therapies.
T61797	HIV-1 inhibitor-15
	HIV-1 inhibitor-15 (compound 9d) is a potent and broad-spectrum inhibitor targeting HIV-1. It exhibits inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, and E138K with respective EC50 values of 1.7 nM, 4 nM, 2 nM, 6 nM, and 9 nM. In addition to its high efficacy, HIV-1 inhibitor-15 possesses favorable solubility, safety profiles, and oral bioavailability [1].
T69133	Etozolin HCl
	Etozolin HCl is a safe and effective diuretic agent in the treatment of acute cardiac failure. In isolated rings of guinea-pig aorta not responding to acetylcholine, the diuretic dexetozoline did not influence basal vascular tone but inhibited noradrenaline- and histamine-induced contractions. Dexetozoline has a very high bioavailability after oral administration and is fairly lipohilic. The half-life of etozolin is 2.5 h. Dexetozoline accumulates in cirrhosis.
T68547	SNJ-1945
	SNJ-1945 is a calpain inhibitor with more favorable retinal penetration, high oral bioavailability, and long half-life. SNJ1945 rescued defective function in lissencephaly. SNJ-1945 protects SH-SY5Y cells against MPP(+) and rotenone. SNJ-1945 reduces murine retinal cell death in vitro and in vivo. SNJ-1945 has good aqueous solubility, can prevents the heart from KCl arrest-reperfusion injury associated with the impairment of total Ca(2+) handling by inhibiting the proteolysis of alpha-fodrin a...
T61753	MPT0G211 mesylate
	MPT0G211 mesylate is a powerful and selective HDAC6 inhibitor (IC50 = 0.291 nM), with high oral bioavailability. It exhibits remarkable selectivity for HDAC6 over other HDAC isoforms (>1000-fold selectivity). Additionally, MPT0G211 mesylate can effectively cross the blood-brain barrier. In preclinical studies using an Alzheimer's disease model, MPT0G211 mesylate has shown promising results in reducing tau phosphorylation and cognitive deficits. Furthermore, this compound exhibits anti-metastatic...
T39035	FXIa-IN-6
	FXIa-IN-6 是一种有效的 FXIa 抑制剂，对大多数相关丝氨酸蛋白酶具有选择性（Ki= 0.3 nM）。FXIa-IN-6 还在多个临床前物种中展示了出色的药代动力学 (PK) 特性（高口服生物利用度和低清除率）。
T71088	AM-211 sodium
	AM-211 sodium is a novel and potent antagonist of the prostaglandin D2 receptor type 2. AM-211 is active in animal models of allergic inflammation. AM211 has high affinity for human, mouse, rat, and guinea pig DP2 and it shows selectivity over other prostanoid receptors and enzymes. AM211 exhibits good oral bioavailability in rats and dogs and dose-dependently inhibits 13,14-dihydro-15-keto-PGD(2)-induced leukocytosis in a guinea pig pharmacodynamic assay.
T61814	JAK3-IN-9
	JAK3-IN-9 is a potent and orally active inhibitor of the Janus kinase 3 (JAK3) enzyme, displaying an impressive IC50 value of 1.7 nM. It exhibits high selectivity towards the JAK3 signaling pathway, making it a valuable tool for studying autoimmune diseases. Additionally, JAK3-IN-9 possesses desirable characteristics such as low toxicity and excellent oral bioavailability. It also demonstrates promising anti-arthritis activity, thus enhancing its potential as a therapeutic agent [1].
T79833	ROCK-IN-9	ROCK	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
	ROCK-IN-9（Compound T345）为ROCK抑制剂。该化合物在HepG2细胞中表现出IC50为40.8 μM的细胞毒性。在小鼠模型中，ROCK-IN-9展现了良好的药代动力学特性，即使在低剂量下也能获得较高的体内暴露水平及口服生物利用度。
T61693	AAK1-IN-5
	AAK1-IN-5 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), characterized by its ability to penetrate the central nervous system and its oral bioavailability. It displays high selectivity, with an AAK1 inhibitory potency (IC 50) of 1.2 nM, a binding affinity (K i) of 0.05 nM, and an inhibitory potency against cellular AAK1 activity (cell IC 50) of 0.5 nM. AAK1-IN-5 holds promise for investigating neuropathic pain in scientific research [1].
T77630	EP3 antagonist 4	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	EP3 antagonist 4 是一种 EP3 拮抗剂，对 hEP 有抑制作用， Ki 值为 2 nM。EP3 antagonist 4 在大鼠完整 PK 研究中显示出较低的体内清除率、高口服 AUC 和良好的生物利用度。EP3 antagonist 4 可用于研究糖尿病和细胞功能障碍。
T69603	BR103354
	BR103354 is a novel fibroblast activation protein (FAP) inhibitor with anti-diabetic and anti-steatotic effects. BR103354 inhibited FAP with an IC50 value of 14 nM, showing high selectivity against dipeptidyl peptidase (DPP)-related enzymes and prolyl oligopeptidase (PREP). BR103354 exhibited good pharmacokinetic properties as evidenced by oral bioavailability of 48.4% and minimal hERG inhibition. Single co-administration of BR103354 with hFGF21 reduced nonfasting blood glucose concentrations, i...
T80789	WAY-639872
	WAY-639872是一种用于生化反应研究的活性分子。
T80787	WAY-649123
	WAY-649123为一有活性分子，适用于生化反应研究。
T71252	PC-046
	PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with di...
T36308	PF-06843195
	PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy[1]. PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC50s of 62 nM and 32 nM, respectively[1].PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells w...
T35527	PI3Kα-IN-4 PI3Kα-IN-4
	PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1]. PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1]. PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit t...
T36084	PKI-179
	PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo[1][2]. PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].PKI-179 shows inhibitory activity against a panel of 361 other ...

化合物

Cat.No: T2086

Synonym: ELN 441958

Target: Bradykinin Receptor

Cat.No: T26863

Synonym: BMS 929075,BMS929075

Target: HCV Protease

Cat.No: T9692

Target: Somatostatin

Cat.No: T73447

Cat.No: T26690

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

Cat.No: T39442

Cat.No: T27374

Synonym: FR181877,FR 181877

Cat.No: T74167

PHA 543613 hydrochloride

Cat.No: T70420

KRH-3955 hydrochloride

Cat.No: T39787

Cat.No: T78744

Target: IRAK

Alpelisib hydrochloride

Cat.No: T14191

Synonym: BYL-719 hydrochloride

Target: Others

Cat.No: T70951

mGluR2 antagonist 1

Cat.No: T38910

HIV-1 inhibitor-15

Cat.No: T61797

Cat.No: T69133

Cat.No: T68547

MPT0G211 mesylate

Cat.No: T61753

Cat.No: T39035

Cat.No: T71088

Cat.No: T61814

Cat.No: T79833

Target: ROCK

Cat.No: T61693

EP3 antagonist 4

Cat.No: T77630

Target: Prostaglandin Receptor

Cat.No: T69603

Cat.No: T80789

Cat.No: T80787

Cat.No: T71252

Cat.No: T36308

Cat.No: T35527

Synonym: PI3Kα-IN-4

Cat.No: T36084

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