Membrane Transporter/Ion Channel(跨膜转运)

Cat.No. 产品名称 Information

GC47352 FK-506-13C-d2 An internal standard for the quantification of FK-506

GC47338 Fenoxycarb A non-neurotoxic carbamate insecticide

GC47260 Dofetilide-d4 An internal standard for the quantification of dofetilide

GC47158 Cypermethrin A type II pyrethroid insecticide

GC47155 Cyfluthrin A pyrethroid insecticide

GC46957 Bumetanide-d5 An internal standard for the quantification of bumetanide

GC46891 ATPA (hydrate) An agonist of GluR5

GC46831 Alloisolithocholic Acid An allomonohydroxy bile acid

GC46464 17R(18S)-EpETE An EPA metabolite and activator of K_Ca1.1/BK channels

GC46366 1,2,3,4-Tetrahydro-β-carboline A serotonin reuptake inhibitor and metabolite of tryptamine

GC61379 VU0463271 quarterhydrate VU0463271quarterhydrate是神经特异性氯钾协同转运蛋白2(KCC2)的有效抑制剂，其IC50值为61nM。

GC61374 Vonoprazan Fumarate A selective and reversible proton pump inhibitor

GC61345 Transdermal Peptide Disulfide TFA TransdermalPeptideDisulfideTFA(TD1Disulfide(peptide)TFA)是由11个氨基酸组成的多肽，可以与Na+/K+-ATPasebeta-subunit(ATP1B1)结合，主要与ATP1B1的C末端相互作用。TransdermalPeptideDisulfideTFA能够增强一些大分子在皮肤中的传递。

GC61342 TPC2-A1-N TPC2-A1-N是一种亲脂性的、膜透异位选择性双孔通道2（TPC2)小分子激动剂。TPC2-A1-N通过在独立结合位点模拟NAADP和PI(3,5)P2的生理作用发挥作用。TPC2-A1-N对溶酶体活性有反向作用，并以TPC2依赖的方式增加溶酶体腔内的pH。

GC61317 Tebanicline dihydrochloride Tebaniclinedihydrochloride(Ebaniclinedihydrochloride)是nAChR的调节物，具有有效的口服止痛活性。抑制cytisine与神经元nAChR的结合的Ki值为37pM。

GC61292 SR33805 SR33805是一种有效的Ca2+通道拮抗剂，在去极化和极化条件下的EC50值分别为4.1nM和33nM。SR33805阻止L型而不是T型Ca2+通道。SR33805可用于研究急性或慢性心脏衰竭。

GC61288 Spadin TFA SpadinTFA是一种从血液中释放的前肽衍生的天然肽，能够阻断TREK-1(KCNK2或K2P2.1)通道的活性。SpadinTFA与TREK-1特异性结合，亲和力为10nM。SpadinTFA是一种有效的抗抑郁药。

GC61251 Rosuvastatin D3 RosuvastatinD3(ZD4522D3)是Rosuvastatin的一种氘代化合物。Rosuvastatin(ZD4522)是一种竞争性HMG-CoA还原酶抑制剂，IC50为11nM。Rosuvastatin有效阻断人类醚-a-go-go相关基因(hERG)电流，IC50为195nM，延迟心脏复极化，从而延长动作电位持续时间(APDs)和校正QT间期(QTc)间隔。

GC61250 Ropivacaine Ropivacaine is a member of the amino amide class of local anesthetics.

GC61248 RO2959 monohydrochloride RO2959monohydrochloride是一种有效的选择性CRAC通道抑制剂，IC50为402nM。RO2959monohydrochloride是由Orai1/Stim1通道介导的钙存储进入(SOCE)的有效阻滞剂，IC50为25nM。RO2959monohydrochloride还是人IL-2产生的有效抑制剂，有效阻断T细胞受体触发的基因表达和T细胞功能途径。

GC61186 Picrotoxinin Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAAA receptors.

GC61175 PF-06305591 dihydrate PF-06305591dihydrate是一种有效的、高选择性的电压门控钠通道NaV1.8的阻断剂，其IC50值为15nM。具有良好的临床前体外ADME(吸收、分布、代谢和排泄)和安全性。

GC61155 Omeprazole sodium An irreversible inhibitor of the gastric proton pump

GC61141 NSC 15364 NSC15364是一种VDAC1寡聚化和细胞凋亡(apoptosis)抑制剂。

GC61139 Nothofagin Nothofagin是一种二氢查尔酮，是从如意宝(Aspalathuslinearis)中分离得到的。Nothofagin通过阻断钙(calcium)内流来下调NF-κB的转运。Nothofagin具有抗氧化活性，可改善各种炎症反应，例如脓毒症反应和血管炎症。

GC61110 Nav1.1 activator 1 Nav1.1activator1(compound4)是强有效的、能透过血脑屏障的、Nav1.1激动剂，0.03μM可增加衰减Nav1.1电流的时间常数τ。对Nav1.2、Nav1.5、Nav1.6有显著的选择性。

GC61066 Minoxidil sulfate Minoxidil (U-58838) is a potent direct-acting peripheral vasodilator that reduces peripheral resistance and produces a fall in blood pressure.

GC61046 Methocarbamol D5 An internal standard for the quantification of methocarbamol

GC60975 Lansoprazole Sulfide D4 LansoprazoleSulfideD4是LansoprazoleSulfide的氘代物。LansoprazoleSulfide是质子泵抑制剂Lansoprazole的活性代谢产物。LansoprazoleSulfide是一种口服活性抗结核药，细胞内的IC50值为0.59µM，肉汤中的IC50值为0.46µM。

GC60929 Ilaprazole sodium A gastric proton pump inhibitor

GC60890 Guvacine An inhibitor of GABA uptake

GC60862 GABAA receptor agent 1 GABAA receptor agent 1 is a high affinity ligand for Gamma-aminobutyric acid A (GABAA) receptor that exerts potent anticonvulsant activity.

GC60834 Fenamic acid Fenamic acid (N-Phenylanthranilic acid, 2-(Phenylamino)benzoic acid, 2-Anilinobenzoic acid, Diphenylamine-2-carboxylic acid) serves as a parent structure for several nonsteroidal anti-inflammatory drugs (NSAIDs), including mefenamic acid, tolfenamic acid, flufenamic acid, and meclofenamic acid.

GC60797 D-Tubocurarine chloride pentahydrate

D-Tubocurarinechloridepentahydrate是微管尿素的氯化物盐形式，是烟碱乙酰胆碱受体(AChR)的拮抗剂，可在手术或机械通气期间用作骨骼肌松弛剂。D-Tubocurarinechloridepentahydrate也是一种有效的神经肌肉阻滞剂。

GC60750 Dehydrosoyasaponin I DehydrosoyasaponinI(SoyasaponinBe;DHS-I)，一种三萜糖苷，是一种有效且可逆的钙激活钾(maxi-K)通道激活剂。

GC60723 COR659 COR659是GABAB的阳性变构调节剂(PAM)。COR659可缓解大鼠对酒精和巧克力的药物成瘾。

GC60718 Cloperastine hydrochloride Cloperastine (HT-11) is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.

GC60709 Cinnarizine D8 An internal standard for the quantification of cinnarizine

GC60642 Bifenthrin A synthetic pyrethroid insecticide

GC60596 Arecaidine Arecaidine，一种吡啶生物碱，是一种有效的GABA吸收抑制剂。Arecaidine是H+偶联的氨基酸转运蛋白1(PAT1，SLC36A1)的底物，竞争性抑制L-脯氨酸的摄取。

GC60549 ABT-418 hydrochloride ABT-418hydrochloride是一种高效、选择性的nAChRs激动剂，具有增强认知和抗焦虑的作用。ABT-418hydrochloride激活胆碱能通道，可用于阿尔茨海默病的研究。

GC60545 A2793 A2793 (Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate) is an efficient inhibitor of TWIK-related spinal cord potassium channel (TRESK, K2P18, KCNK18) and TASK-1 (KCNK3) with IC50 of 6.8 μM for mouse TRESK.

GC60542 8-Gingerol A natural TRPV1 agonist

GC60530 5-Hydroxylansoprazole 5-Hydroxylansoprazole(AG1908)是血浆中Lansoprazole的活性代谢产物。Lansoprazole由CYP2C19代谢形成5-Hydroxylansoprazole。Lansoprazole是一种胃质子泵(proton-pump)抑制剂，可有效研究各种消化系统疾病。

GC60455 2,2,2-Trichloroethanol 2,2,2-Trichloroethanol是镇静催眠药水合氯醛的活性形式，是非经典的K2P通道TREK-1和TRAAK的激动剂。

GC60425 (S)-Verapamil D7 hydrochloride (S)-VerapamilD7hydrochloride((S)-(-)-VerapamilD7hydrochloride)是(S)-Verapamilhydrochloride的一种氘代化合物。(S)-Verapamilhydrochloride(S(-)-Verapamilhydrochloride)通过MRP1抑制白三烯C4(LTC4)和钙黄绿素的转运。(S)-Verapamilhydrochloride导致潜在耐药性肿瘤细胞死亡。

GC60423 (S)-UFR2709 hydrochloride (S)-UFR2709(hydrochloride)是一种竞争性的nAChR拮抗剂，并显示出较强的亲和力，对α4β2nAChR的亲和力比对α7nAChR的高。(S)-UFR2709(hydrochloride)在偏好酒精的老鼠中减少焦虑，并且可以减少其酒精摄入和对酒精偏好。(S)-UFR2709(hydrochloride)是抗焦虑试剂，可用于研究尼古丁成瘾。

GC60418 (S)-Lercanidipine hydrochloride (S)-Lercanidipinehydrochloride是Lercanidipinehydrochloride的S-对映体。(S)-lercanidipinehydrochloride是一个高效的钙离子通道阻断剂。

GC60413 (Rac)-NMDAR antagonist 1 (Rac)-NMDARantagonist1是NMDARantagonist1的消旋体。NMDARantagonist1是一种有效且口服生物可利用的，NR2B选择性的NMDAR拮抗剂。

GC60408 (R)-Verapamil hydrochloride (R)-Verapamilhydrochloride((R)-(+)-Verapamilhydrochloride)是一种P-糖蛋白(P-Glycoprotein)抑制剂。(R)-Verapamilhydrochloride抑制MRP1介导的转运，导致MRP1过表达细胞对抗癌药产生化学敏感性。