sprague-dawley

Ziprasidone hydrochloride (CP-88059 hydrochloride) 是一种联合 5-HT（5-羟色胺）和多巴胺受体拮抗剂，具有抗精神病活性的强效作用。它也是去甲肾上腺素再摄取抑制剂。

Methyl L-histidinate dihydrochloride (L-Histidine methyl ester dihydrochloride) 在Sprague-Dawley 大鼠胃中组氨酸脱羧酶的抑制作用被评估为 14CO2 产生减少，活性值为 1.8 μM。

2H-Naphth[2′,1′:4,5]indeno[1,2-d][1,3]dioxole, pregn-4-ene-3,20-dione deriv在Sprague Dawley大鼠上进行测试时显示出高局部抗炎效力和高肺选择性。

Ensartinib (X-396) is a potent and dual ALK MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC50: 9 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC50s of 68 nM, 156 nM, 9.644 μM and 2.989 μM, respectively[1]. The effects of Ensartinib (X-396) in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that Ensartinib shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with Ensartinib at 25mg kg bid. Ensartinib significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, Ensartinib appears well-tolerated in vivo. Mouse weight is unaffected by Ensartinib treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of Ensartinib, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of Ensartinib at 20, 40, 80 mg kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 80mg kg for Ensartinib. At NST levels, Ensartinib achieves an AUC of 66 μM×hr and a Cmax of 7.19 μM[1]. [1]. Lovly CM, et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinaseinhibitors. Cancer Res. 2011 Jul 15;71(14):4920-31.

Metyrapone (NSC-25265) 是 STEROID 11-BETA-MONOOXYGENASE 酶抑制剂。 它被用作库欣综合征诊断中下丘脑-垂体反馈机制的测试。

VPC171 是一种新型腺苷 A1 受体正变构调节剂 (PAM)。

Myosinmodulator 2 (Compound B172) 是一种肌球蛋白 (myosin) 调节剂，它能够抑制兔腰大肌、猪心房和猪心室的 ATP 酶，其 IC25 值分别为 2.013、2.94 和 20.93 μM。Myosinmodulator 2 可调节 Sprague Dawley 大鼠的心脏收缩性能。

Recainam (Wy-42362) hydrochloride 是一种口服有效的抗心律失常药，具有 I 类电生理特性，可抑制复杂性室性心律失常。在 Sprague Dawley 大鼠中，Recainam hydrochloride 展示了良好的药代动力学特征。

Trimethylolpropane caprate has developmental toxicity in Sprague-Dawley rats.

(+)-Osbeckic acid，一种Tartary Buckwheat中提取的血管松弛剂，对Sprague-Dawley大鼠胸主动脉环展现出显著的血管舒张效应，其半数有效浓度(EC50)为887 μM。

CK-963 是一种心肌肌钙蛋白(cTnC)的激活剂，Ki 为 11.5 μM，并能够增强 Sprague-Dawley 大鼠的心肌收缩力。

Triptolidepalmitate 是 Triptolide 的衍生物，对癌细胞 MCF-7 和 A549 具有细胞毒性，IC50 分别为 7.5 和 6.4 μM。在 Sprague Dawley 大鼠模型中的半衰期（T1 2）为 50.4 分钟。Triptolidepalmitate 可用作药物输送载体。

Big endothelin-1 (rat 1-39) 是一个由39个氨基酸残基组成的多肽。它能在清醒状态的Sprague-Dawley大鼠中诱导利尿和利钠的反应，并可导致小鼠血压上升。

Ajugasterone C shows significant inhibitory effect at 100 mg kg dose on rat paw oedema development due to carrageenan-induced inflammation in Sprague Dawley rats.

GS-9770 是一种口服有效的HIV蛋白酶抑制剂，Ki为0.16 nM。它对HIV-1和HIV-2菌株显示出抗病毒活性，EC50分别为1.9-26 nM和26 nM。在人肝微粒体中，GS-9770 展现出代谢稳定性，并在Sprague-Dawley大鼠体内具有良好的药代动力学特征。

DS-1558 is a potent and orally available GPR40 agonist.DS-1558 was found to have potent glucose lowering effects during an oral glucose tolerance test in ZDF rats. DS-1558 significantly and dose-dependently improved hyperglycemia and increased insulin secretion during the oral glucose tolerance test in Zucker fatty rats, the model of insulin resistance and glucose intolerance. DS-1558 not only increased the glucose-stimulated insulin secretion by GLP-1 but also potentiated the maximum insulinogenic effects of GLP-1 after an intravenous glucose injection in normal Sprague Dawley rats.

Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 μM[1]. Sepimostat (1 to 100 nmol eye, intravitreal injection) exhibits significant neuroprotective effect[1]. Animal Model: Male Sprague Dawley rats weighing 150-300 g[1]. [1]. Masahiro Fuwa, et al. Nafamostat and Sepimostat Identified as Novel Neuroprotective Agents via NR2B N-methyl-D-aspartate Receptor Antagonism Using a Rat Retinal Excitotoxicity Model. Sci Rep. 2019 Dec 31;9(1):20409.

Myosin modulator 1 (Compound B141) 是一种肌球蛋白 (myosin) 调节剂，能够抑制兔腰大肌、猪心房及猪心室的 ATP 酶活性，其 IC25 分别为 0.42，0.13 和 3.09 μM。Myosinmodulator 1 还可以调节 Sprague Dawley 大鼠的心脏收缩功能。

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].

The truncated glucagon-like peptides GLP-1(7-37) is naturally occurring peptide product of the preproglucagon gene that are synthesized primarily in the intestine and acts as incretin that are released from the intestine into the bloodstream in response to food and stimulate insulin secretion. GLP-1(7-37) produced a dose-related enhancement of the glucose-stimulated increase in plasma insulin concentration and an increased rate of glucose infusion in Sprague-Dawley Rats at a dosing rang of 0.5, 5, or 50 pmol/min/kg. Further, infusion of GLP-1(7-37) for 60 mins produced a small transitory increase in plasma insulin concentration in fasted rats and fed rats and a slight transitory decrease in plasma glucose concentration. Moreover, GLP-1(7-37) (5 pmol/min/kg IV) infusion for 6 h in Sprague-Dawley rats produced a sustained increase in plasma insulin concentration relative to levels in rats infused with vehicle[1].