Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5513 |
RO-3
|
P2X Receptor | Membrane transporter/Ion channel; Neuroscience |
RO3 是一种能透过大脑的P2X3和P2X2/3拮抗剂,口服有活性。它对人同型多聚体 P2X3和异型多聚体 P2X2/3受体的 pIC50分别为 5.9 和 7.0。 | |||
T60003 |
AC1-IN-1
|
Adenylyl cyclase | Neuroscience |
AC1-IN-1 是 1 型腺苷酸环化酶的选择性抑制剂(AC1,IC50 = 0.54 µM)。 | |||
T6039 |
TAK-285
TAK285,TAK 285 |
EGFR; MEK; HER; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Tyrosine Kinase/Adaptors |
TAK-285 是一种新型 HER2 和 EGFR(HER1) 双重抑制剂,IC50 分别为 17 和 23 nM。它可穿过血脑屏障,有抗肿瘤活性,对 HER1/2 的选择性是 HER4 的 10 倍以上。 | |||
T0682 |
Lamivudine
GR109714X,BCH-189,拉米夫定 |
HIV Protease; Reverse Transcriptase | Microbiology/Virology; Proteases/Proteasome |
Lamivudine (BCH-189) 是一种核苷逆转录酶抑制剂,可抑制HIV 逆转录酶1和2 以及乙型肝炎病毒的逆转录酶。 | |||
T24047 |
Etilevodopa hydrochloride
Levodopa ethyl ester,Etilevodopa HCl, L-DOPA ethyl ester |
Others; Dopamine Receptor; Drug Metabolite | GPCR/G Protein; Metabolism; Neuroscience; Others |
Etilevodopa hydrochloride (L-DOPA ethyl ester) 是 Levodopa 的前药,在胃肠道中被非特异性酯酶快速水解产生 Levodopa 和乙醇。Levodopa 是多巴胺的前体,有助于中枢神经系统的渗透和传递多巴胺。Etilevodopa HCl 可用于帕金森病 (PD)的相关研究。 | |||
T0688 |
Ganciclovir
BW 759,更昔洛韦,RS-21592,2'-Nor-2'-deoxyguanosine |
Nucleoside Antimetabolite/Analog; Others; Antibiotic; Antifection; HSV | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others |
Ganciclovir (2'-Nor-2'-deoxyguanosine) 是核苷类似物和口服抗病毒药物,对CMV 具有抗病毒活性。它用于治疗与艾滋病相关的巨细胞病毒感染的并发症。 | |||
T22337 |
Ganciclovir sodium
RS-21592 sodium,Cytovene IV sodium,2'-Nor-2'-deoxyguanosine sodium,BW 759 sodium,更昔洛韦钠 |
Nucleoside Antimetabolite/Analog; Others; Antifection; HSV | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others |
Ganciclovir sodium (Cytovene IV sodium) 是核苷类似物和口服抗病毒药物,具有抗病毒活性,尤其是针对巨细胞病毒和单纯疱疹病毒 1 型。 | |||
T12679 |
(Rac)-VU 6008667
|
Others; AChR | Neuroscience; Others |
(Rac)-VU 6008667 是一种选择性的毒蕈碱乙酰胆碱受体亚型 5(M5 NAM)负异位调节剂,IC50 为 1.8 μM,pIC50 为 5.75,具有较高的中枢神经系统渗透性。 | |||
T26722 |
AZD7268
AZD-7268,AZD 7268 |
||
AZD7268 is a potent, selective, reversible, and orally bioavailable agonist of δ-opioid receptor with CNS penetration. | |||
T25124 |
AZ599
AZ-599,AZ 599 |
||
AZ599 is a full agonist of CB1 with good solubility and low CNS penetration. | |||
T29142 |
VU6001966
VU 6001966,VU-6001966 |
||
VU6001966 is a potent and selective mGlu2 inhibitor (mGlu2 IC50 = 78 nM) and negative allosteric modulator. VU6001966 exhibits excellent central nervous system (CNS) penetration. | |||
T27474 |
GSK-345931A
GSK-345931A free acid,GSK 345931A free acid,GSK 345931A |
||
GSK-345931A, an EP(1) receptor antagonist, shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain. | |||
T28067 |
ML372
ML 372,ML-372 |
||
ML372 is a potent and selective SMN Modulator (EC50 = 12 nM, 325% increase inSMN2) with good potency, pharmacokinetics, tolerance, and CNS penetration. | |||
T17241 |
Auglurant
VU0424238 |
Others | Others |
Auglurant is a novel and selective mGlu5 antagonist (IC50: 11 nM (rat) and an IC50: 14 nM (human)). Auglurant has an acceptable CNS penetration. | |||
T35081 |
VU0486321
VU 0486321,VU-0486321 |
||
VU0486321 is a potent mGlu1 PAM with moderate rat PK (CLp = 13.3. mL/min/kg,t1/2 = 54 min), good free fraction (human fu = 0.05, rat fu =0.03) and excellent CNS penetration (Kp = 1.02). | |||
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. | |||
T36644 | Rezivertinib | ||
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI) with potent activity against both common activation EGFR and resistance T790M mutations. Additionally, Rezivertinib demonstrates excellent central nervous system (CNS) penetration and exhibits antitumor activity[1][2]. | |||
T25819 |
ML350
SR-2311,SR 2311,SR2311,ML-350,ML 350 |
||
ML350 (CYM-50202) is a KOR (IC50: 12.6 nM) antagonist with good and moderate selectivity against the DOR and MOR. CYM-50202 displayed high solubility and excellent CNS penetration. CYM-50202 did not display long-lasting pharmacodynamic effects observed wi | |||
T69850 |
SHR0687
|
||
SHR0687 is a Highly Potent KOR Agonist. SHR0687 showed excellent selectivity over other opioid receptors, such as MOR and DOR. In addition, SHR0687 displayed favorable PK profiles across species, as well as robust in vivo efficacy in a rat carrageenan-induced pain model. Notably, SHR0687 exhibited negligible blood−brain barrier penetration, which was meaningful in minimizing CNS-related side effects. | |||
T39343 |
MW-150 hydrochloride
MW01-18-150SRM hydrochloride,MW-150 hydrochloride |
||
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a potent and selective inhibitor of p38α MAPK, with a Ki value of 101 nM. It exhibits excellent CNS penetration and oral bioavailability. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) effectively suppresses the phosphorylation of MK2, a substrate of endogenous p38α MAPK, in activated glial cells. | |||
T69780 |
VU6007477
|
||
VU6007477 is a novel M1 PAM. VU6007477 resulted in good rat M1 PAM potency (EC50 = 230 nM, 93% ACh max), minimal M1 agonist activity (agonist EC50 > 10 μM), good CNS penetration (rat brain/plasma Kp = 0.28, Kp,uu = 0.32; mouse Kp = 0.16, Kp,uu = 0.18), and no cholinergic adverse events (AEs, e.g., seizures). | |||
T61210 |
R-PSOP
|
||
R-PSOP is a potent and selective nonpeptidic NMUR2 antagonist, exhibiting binding affinity to human and rat NMUR2 with Ki values of 52 nM and 32 nM, respectively. This compound demonstrates moderate central nervous system (CNS) penetration and is valuable in the study of eating disorders, obesity, pain, and stress-related disorders [1]. | |||
T73176 |
LRRK2-IN-7
|
||
LRRK2-IN-7为一种高效、选择性、具有中枢神经系统(CNS)渗透性的LRRK2激酶抑制剂,其IC50值为0.9 nM。该化合物对LRRK2以外的其他激酶、离子通道及CYP酶表现出超过1000倍的选择性。 | |||
T33950 |
PF-06767832
PF-6767832,PF6767832,PF 6767832,PF 06767832 |
||
PF-06767832 is a high quality M1 selective PAM (M1 PAM EC50 = 60 nM; M2-M5 PAM EC50 > 10 microM; CNS MPO = 4.9). PF-06767832 has well aligned physicochemical properties, good brain penetration and pharmacokinetic properties. Extensive safety profiling | |||
T68356 | AM-3189 | ||
AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good oral bioavai... | |||
T71577 | KOS-1584 | ||
KOS-1584 is a second-generation epothilone with potential antineoplastic activity. Epothilone KOS-1584 binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to first-generation epothilones, this agent exhibits greater safety and efficacy with an enhanced pharmaceutical profile, including enhanced water solubility and tumor penetration,... | |||
T21750 |
A 784168
|
||
A-784168 是一种有效的、口服活性的香草素受体 1 型 (TRPV1) 抑制剂。香草素受体 1 型 (TRPV1) 是一种配体门控非选择性阳离子通道,被认为是各种疼痛刺激 (如内源性脂质、辣椒素、热和低 pH 值) 的重要整合剂。口服给药时,A-784168 具有良好的 CNS 渗透性。 |