rodent-active

Lu AF27139 是一种有效的选择性 P2X7 受体拮抗剂（人和大鼠的 IC50 分别为 12 和 2.4 nM，小鼠、人和大鼠的 Ki 分别为 22、54 和 13 nM）。 Lu AF27139 可用于中枢神经系统疾病研究。

AHR antagonist 5 free base 是一种具有口服活性的 AHR 拮抗剂，在人和啮齿动物细胞系中的 IC50 约为 35-150 nM,具有抗癌活性。

SB-277011 hydrochloride (SB-277011A hydrochloride) 是一种可口服且具有选择性、强效性和脑渗透性的多巴胺 D3 受体(D3R) 拮抗剂，在大鼠中诱导的射精延迟。SB-277011 hydrochloride 可用于研究神经系统疾病。

PF-0463481 succinate is a potent and orally active dual antagonist of CCR2 CCR5 with comparable human and rodent CCR2 potency with IC50 of 20.8 nM.

PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2 CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481

ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.

Apoptone 是 3β- 雄烷二醇合成类似物，是一种具有口服生物可利用度的抗癌剂。Apoptone 在前列腺癌和乳腺癌的啮齿类动物模型中具有活性。

Tebuquine is an antimalarial agent. Tebuquine is active against P. falciparum in vitro. Tebuquine in vitro shows a chloroquine-like effect, but not in vivo, suggesting that its mode of action in vivo is different from that of chloroquine. Tebuquine has no

Deethylindanomycin is a polyether antibiotic that has been found in S. setonii. It is active against a variety of Gram-positive bacteria, including various strains of S. aureus and Streptococcus, as well as one strain of S. pneumoniae (MICs = 4, 4, and 2 μg ml, respectively). It is also active against coccidia in vitro, inhibiting E. tenella development, but is inactive against E. tenella infection in chicks when administered at a dose of 200 μg g in the diet. Deethylindanomycin acts as an ionophore in lipid bilayer membranes and is more selective for potassium ions than calcium, magnesium, and sodium ions. It induces histamine release from rodent mast cells and human basophils in vitro in a calcium-dependent manner.

CP-346086 dihydrate is a potent and orally active inhibitor of microsomal triglyceride transfer protein (MTP), exhibiting an IC50 value of 2.0 nM for both human and rodent MTP. This compound effectively lowers plasma cholesterol and triglyceride levels in vivo.

APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease.

ARUK3001185 (Compound 8l) 是选择性的、口服有效的、脑渗透性的 Notum 抑制剂（IC50 = 6.7 nM），适合在啮齿动物疾病模型中口服给药。

APJ receptor agonist 5 (compound 3) 是一种有效的、口服具有活力的 apelin 受体 (APJ) 激动剂 (EC50: 0.4 nM)。APJ receptor agonist 5 在啮齿动物心力衰竭 (HF) 模型中具有出色的药代动力学特征，在临床前毒理学研究中也具有可接受的安全性。APJ receptor agonist 5 能够改善心脏功能，可用于 HF 疾病的研究。

(6R)-ML753286 是 ML753286 的异构体。ML753286 是一种口服活性和选择性 BCRP(抗乳腺癌蛋白) 抑制剂，IC50为 0.6 μM。 ML753286 在啮齿动物和人类肝脏 S9 组分中具有高渗透性和低至中等清除率，并且在不同物种中都具有血浆稳定性。

MAO-B-IN-4（Compound 26）是一款口服活性MAO-B选择性可逆抑制剂，IC50为9 nM。它展现出优良的代谢稳定性和血脑屏障渗透能力，以及在安全性方面的良好特性。此外，MAO-B-IN-4在大鼠及小鼠中表现出显著的抗抑郁效果，并在星形胶质细胞中具有神经保护作用，适用于阿尔茨海默病相关的研究。

CVN417，一种含 α6 亚基的口服nAChR拮抗剂，通过脉冲依赖的方式调控多巴胺能神经传递，并对nAChR亚基介导的Ca(2+)流出显示出抑制效应，其IC50s为0.086 μM (α6)，2.56 μM (α3)，以及0.657 μM (α4)。在啮齿类动物模型之研究中，CVN417减缓静息震颤，并展现对帕金森病等运动功能障碍改善的可能性。

Connexin mimetic peptide 40,37GAP26是一种生物活性肽，对应Cx37和Cx40主要血管连接蛋白的胞外环GAP26结构域，命名基于Cx同源性为37,40Gap26。本化合物主要用于研究间隙连接对环吡嗪酸(CPA)通过啮齿动物髂动脉壁导致的内皮超极化扩散的影响。Cx37和Cx40形成的间隙连接斑块在内皮细胞中高度丰富，而Connexin mimetic peptide 40,37GAP26能抑制内膜下超极化。

Hemoregulatory peptide 5b is a synthetic analog of granulocyte chalone which initially identified in extracts of rodent bone marrow and human leukocytes. Monomer inhibits both formations of GM-CFC colonies and cytotoxic drug-induced recruitment of murine