whole-cell

VU0134992 hydrochloride 是一个亚型偏好的，具有口服活性和选择性的内向整流钾通道Kir4.1阻滞剂，IC50为 0.97 μM。在 -120 mV 时，VU0134992 hydrochloride 对同分 Kir4.1 比 Kir4.1 5.1 共分通道 (IC50=9 μM) 高出 9 倍的选择性。

VU 0134992 是一个亚型偏好的，口服有效的和选择性的内向整流钾通道 Kir4.1阻滞剂，IC50为 0.97 μM。在 -120 mV 时，VU0134992对同分 Kir4.1 比 Kir4.1 5.1 共分通道 (IC50=9 μM) 高出 9 倍的选择性。

TRPV1-Tat是一种针对瞬时受体电位范烤苷1 (TRPV1) 的肽类拮抗剂。它由来自TRPV1的A-激酶锚蛋白(AKAP)结合域的736-745个氨基酸以及来自HIV Tat的细胞穿透肽序列组成。TRPV1-Tat (200 µM) 能够在使用初级小鼠背根神经节的整细胞膜片钳技术中抑制由热或棕榈酸酯12-肉豆蔻酸13-醋酸酯(PMA014)引起的电流。当以10或30 µM剂量给药时，它能增加大鼠后爪机械痛阈。

Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877).

Narsoplimab (OMS 721) 是一种选择性全人免疫球蛋白γ 4 (IgG4) 单克隆抗体，是一种甘露聚糖结合凝集素相关的丝氨酸蛋白酶-2（MASP-2）抑制剂，可结合 MASP-2 并阻止凝集素通路激活，对凝集素通路有抑制作用。Narsoplimab 可用于研究成人造血干细胞移植相关疾病。

BMS-933043 is a Selective α7 nAChR partial agonist. BMS-933043 showed potent binding affinity to native rat (Ki = 3.3 nM) and recombinant human alpha7 nicotinic acetylcholine receptors (Ki = 8.1 nM). BMS-933043 shows agonist activity in a calcium fluoresc

MitoEbselen-2 is a radiation mitigator which reduces lipid hydroperoxides and prevents apoptotic cell death. When administered 24 hours postirradiation, MitoEbselen-2 was shown to increase the survival of mice exposed to whole body γ-irradiation.

BioA-IN-13 is a highly effective inhibitor of the Mycobacterium tuberculosis BioA enzyme, displaying potent cell permeability and whole-cell activity [1].

SB-408124 Hydrochloride is a non-peptide OX1 receptor antagonist(Ki of 57 nM and 27 nM in both whole cell and membrane, respectively).

Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial cells and accumulated in the cytosol in a biphasic manner[1]. During pelleting hypoxia, Ru360 (10 µM) significantly improves cell viability in wild type cardiomyocytes[3]. Ru360 (15-50 nmol/kg) treatment abolishes the incidence of arrhythmias and haemodynamic dysfunction elicited by reperfusion in a whole rat model. Ru360 administration partially inhibits calcium uptake, preventing mitochondria from depolarization by the opening of the mitochondrial permeability transition pore (mPTP)[1]. [1]. G de J García-Rivas, et al. Ru360, a Specific Mitochondrial Calcium Uptake Inhibitor, Improves Cardiac Post-Ischaemic Functional Recovery in Rats in Vivo. Br J Pharmacol. 2006 Dec;149(7):829-37. [2]. M A Matlib, et al. Oxygen-bridged Dinuclear Ruthenium Amine Complex Specifically Inhibits Ca2+ Uptake Into Mitochondria in Vitro and in Situ in Single Cardiac Myocytes. J Biol Chem. 1998 Apr 24;273(17):10223-31. [3]. Lukas J Motloch, et al. UCP2 Modulates Cardioprotective Effects of Ru360 in Isolated Cardiomyocytes During Ischemia. Pharmaceuticals (Basel). 2015 Aug 4;8(3):474-82.

Dihydroisopimaric acid activates BK channels alphabeta1, which are large conductance Ca 2+ activated K + channels. This compound directly measures the opening of BKalphabeta1 under a whole-cell voltage clamp.

1-Oleoyl-2-acetyl-sn-glycerol (1-oleoyl-2-acetyl-glycerol) 是一种细胞渗透性的钙依赖蛋白激酶C (PKC)激活剂，可调节多种可兴奋细胞中的全细胞 Ca2+ 电流，诱导超氧化物的产生。

SB408124 是一种 OX1 受体的非肽拮抗剂，在全细胞和膜中的 Ki 值分别为 57 和 27 nM，其选择性是 OX2 受体的 50 倍。

A 78773 is a potent, selective, direct, and reversible 5-lipoxygenase inhibitor. It has activity in a variety of purified cells and in more complex biological systems such as whole blood, lung fragments, and tracheal tissues. A 78773 acts against inflamma

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs. Lanz et al (2010) Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. J.Pharmacol.Exp.Ther. 334 269 PMID:20363853

Mycro 3 在全细胞分析中对 c-Myc 具有强效选择性，可用于胰腺癌的研究。

NAZ2329 是受体型蛋白质酪氨酸磷酸酶 (RPTPs) R5 亚家族的一个细胞可渗透抑制剂，与其他 PTPs 相比，其变构且能够优先抑制 PTPRZ (hPTPRZ1 的IC50= 7.5 μM) 和PTPRG (hPTPRGIC50= 4.8 μM)。NAZ2329 能够与PTPRZ 的 D1结构域结合，与PTPRZ 整个 (D1 + D2) 片段相比，其能够更有效地抑制 PTPRZ1-D1片段 (IC50: 1.1 μM)。NAZ2329 能够抑制胶质母细胞瘤细胞的肿瘤生长，并表现出抑制干细胞样特性。

ω-Conotoxin CVIB为非选择性N型及P Q型电压门控钙通道(VGCC)拮抗剂，能够抑制背根神经节(DRG)中神经元去极化后激活全细胞VGCC电流，其pIC50值为7.64。

PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM 40% & 20 μM 60% at pH 9.0, 5 nM 28% & 3 μM 72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM 39% & 10 μM 61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1 2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).

Antibacterialagent 233(Compound 7c)在多方面展示了显著的抗菌和抗肿瘤特性.首先,该化合物对Helicobacter pylori有明显的抑制效果,其MIC值介于0.4-1.6 μg mL.此外,Antibacterialagent 233能有效抑制刀豆脲酶(jack bean urease),IC50值为0.27 μg mL,并能改变H. pylori的细胞膜通透性,导致细胞内容物的渗漏.在体外环境中,该化合物在全血和人工胃液中显示出良好的代谢稳定性.在生物医学研究中,Antibacterialagent 233还在小鼠体内展现对U2OS肿瘤细胞的抑制活性.

Olinciguat (IW-1701) 是一种口服鸟苷酸环化酶 (sGC) 刺激剂，在纯化的大鼠和人类酶测定以及全细胞测定中对 sGC 具有浓度依赖性刺激作用。

FTI 277 TFA is a prodrug form of FTI 276 that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10μM respectively) and disrupts constitutive H-Ras-specific activation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.