Membrane Transporter/Ion Channel

Crinecerfont tosylate is an effective oral CRF1 receptor antagonist. It is applicable to studies involving congenital adrenal hyperplasia (CAH).

Dehydroindapamide, an indole form of Indapamide, is utilized to quantify the turnover rate of Indapamide in CYP3A4, which is approximately 10 times higher than that of Indoline, with slightly enhanced affinity for CYP3A4.

MSK-195 is an effective TRPV1 agonist.

S9-A13 is a potent and selective inhibitor of SLC26A9, exhibiting an IC50 of 90.9 nM without inhibiting other members of the SLC26 family, such as SLC26A3, SLC26A4, and SLC26A6. It also inhibits the SLC26A9 Cl- current in cells lacking CFTR expression.

(3S,6R)-NML is an NMDA receptor antagonist with pIC50 values of 4.8 [GluN1-GluN2A], 4.6 [GluN1-GluN2B], 5.0 [GluN1-GluN2C], and 5.0 [GluN1-GluN2D]. It is applicable in the study of depression.

(2S,3S,11bR)-Dihydrotetrabenazine ((2S,3S,11bR)-DHTBZ) is a highly selective inhibitor of vesicular monoamine transporter 2 (VMAT2) with a Ki value of 593 nM. It suppresses the vesicular transport of monoamine neurotransmitters, such as dopamine and serotonin, leading to reduced release into the synaptic cleft. This compound holds potential for research in Huntington's disease and other hyperkinetic movement disorders.

Caramboxin, a neurotoxin, can induce acute kidney injury.

BGT1-IN-1 (compound 9) is an effective inhibitor of BGT1, demonstrating IC50 values of 13.9 µM for hBGT1 and 58.3 µM for GAT3. It exhibits no cytotoxic effects and possesses neuroprotective activity.

CFTRcorrector 17 (example 17) is a regulator of the cystic fibrosis transmembrane conductance regulator (CFTR). It is utilized in the study of diseases mediated by CFTR.

NMD670 is an orally active, partial inhibitor of the skeletal muscle-specific chloride channel ClC-1. It enhances muscle excitability and neuromuscular transmission, restoring muscle function and mobility. NMD670 has a favorable safety profile and improves muscle function in rats, particularly in an MG rat model [1].

Cav 3.2 inhibitor 1 targets T-type calcium channels, weakly binds D2 receptors, and aids physical and visceral pain research.

Cav 3.2 inhibitor 3 is a potent inhibitor of the Cav3.2 T-type Ca2+channel (IC50: 0.1534 μM) and has a low binding affinity for D2 receptors.

Probenecid sodium is the sodium salt of Probenecid, a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Additionally, Probenecid acts as an inhibitor of pannexin 1 channels.

Cav 3.2 inhibitor 2 blocks T-type Ca2+ channels (IC50=0.09339 μM) and reduces mouse somatic/visceral pain. Used for intractable pain studies.

Antidepressant agent 8 (Compound 1f) acts as a selective antagonist for the NMDA receptor GluN1/2A (NMDA receptorGluN1/2A), with an IC50 of 2.94 μmol/L. In a hydrocortisone-induced zebrafish depression model, it demonstrates antidepressant-like effects and shows good blood-brain barrier penetration.

S 0960 is a dimeric bile acid analogue, a specific inhibitor of the sodium-dependent bile salt transporter in the ileum, used in metabolic disease research.

SGC-CAMKK2-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) with an IC50 of 30 nM. It effectively inhibits AMPK phosphorylation in C4-2 cells, exhibiting an IC50 value of 1.6 µM.

AqF026 is an AQP1 agonist that enhances AQP1-mediated water transport. It is utilized in research related to peritoneal dialysis and diseases associated with local water metabolism defects, such as subretinal edema and cerebral edema.

SYM2206 is a low affinity non-competitive AMPA receptor antagonist with an IC50 value of 1.6 μM.SYM2206 exhibits anticancer activity by blocking Nav1.6-mediated

Odevixibat (A4250) is a selective oral inhibitor for ileal bile acid transport, potentially treating primary biliary cirrhosis.

Suzetrigine (VX-548) is an oral NaV1.8 inhibitor with analgesic properties for acute pain research.

SDZ 220-040 是一种选择性哺乳动物 NMDA 受体拮抗剂，可诱导根系生长的部分无重力模式 。

(+)-Tetrabenazine ((3R,11bR)-Tetrabenazine) is a reversible vesicular monoamine transporter 2 (VMAT-2) inhibitor, inhibits transport by VMAT2 with 10-fold

5-Hydroxylansoprazole (AG1908) is the active metabolite of plasma Lansoprazole, inhibits the proton pump, and is used in the study of peptic ulcers.

Umbellulone is a natural product isolated from Umbellularia californica, and stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.

(-)-Bicuculline methobromide is a potent antagonist of GABAA receptor .

A-887826 is a selective, orally bioavailable, and voltage-dependent Na(v1.8) channel blocker (IC50: 11 nM). It attenuates neuropathic tactile allodynia in vivo.

(Rac)-Lanicemine ((Rac)-AZD6765) is the racemate of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker with a Ki of 0.56-2.1 μM for the NMDA receptor and IC50 values of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively. Lanicemine shows antidepressant effects [1].

NSC-609249 hydrochloride, an impurity of Verapamil, is a calcium channel blocker with potent orally active properties. It also functions as a first-generation P-glycoprotein (P-gp) inhibitor.

PF-06761281 is a partially selective sodium-coupled citrate transporter protein (NaCT/SLC13A5) inhibitor, oral, reducing plasma glucose concentration.

<p>Apcin A HCL is an Apcin derivative. Apcin A HCL is an anaphase-promoting complex (APC) inhibitor. Apcin-A HCL interacts strongly with Cdc20, and inhibits the ubiquitination of Cdc20 substrates. Apcin-A HCL can be used to synthesize the PROTAC CP5V [1].</p>

3-Methylglutaconic acid, a primary metabolite accumulating in 3-Methylglutaconic aciduria (MGTA), induces lipid and protein oxidation, while diminishing non-enzymatic antioxidant defenses in cerebral cortex supernatants, thereby promoting oxidative stress in the cerebral cortex. This compound is utilized in research concerning brain damage diseases [1].

GNE-9278 is a highly selective NMDAR orthosteric modulator that targets the GluN1 transmembrane structural domain (TMD), enhancing peak current and agonist affinity in activated NMDAR.

2-(Trifluoromethyl)cinnamic acid is a useful organic compound for research related to life sciences. The catalog number is T64859 and the CAS number is 2062-25-1.

L-Cysteine S-sulfate sodium salt sesquihydrate is a useful organic compound for research related to life sciences. The catalog number is T64782 and the CAS number is 150465-29-5.

Indoxacarb is an Oxadiazine insecticide.

Filapixant, a purinoreceptor antagonist. This compound serves as the active reference substance for Eliapixant.

Zastaprazan (JP-1366, compound 6) is a potassium-competitive acid blocker and proton pump inhibitor that suppresses gastric acid secretion, indicated for GERD.

22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22(S)-hydroxy Cholesterol also reduces fatty acid synthase (FAS) reporter activity through an LXR response element in the promoter region in COS-1 cells transfected with RXRα and LXRα and decreases the expression of MCP-1 and CCR2 in a mouse model of chronic ethanol consumption.[1] [2] Dietary supplementation of 22(S)-hydroxy cholesterol (30 mg/kg per day) leads to less body weight gain and lower liver triacylglycerol levels in rats when fed either a regular chow or high-fat diet as well as prevents an increase in plasma triacylglycerol levels resulting from a high-fat diet.[3]

2-AEMP TFA is a potent and rapidly acting antagonist of GABA(A)-ρ1 receptors. 2-AEMP is an analog of GABA.

Dexivacaine is an type of anesthetic.

Alfadolone acetate is a gamma-aminobutyric acid (GABA) receptor agonist.

<p>Vonoprazan fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase.</p>

<p>Motugivatrep is a potent and selective TRPV1 antagonist that can be used to study TRPV1-related respiratory diseases.</p>

Gacyclidine (OTO311), an NMDA receptor blocker, treats tinnitus and injuries in the brain and spinal cord.

CGP 44532 a GABAB receptor agonist.

AKOS-22: potent VDAC1 inhibitor, Kd=15.4 μM; prevents mitochondrial dysfunction and apoptosis.

Tifenazoxide is an effective and SUR1/Kir6.2 selective KATP channels opener. Tifenazoxide has an anti-diabetic effect, can inhibit glucose-stimulated insulin release in vitro and in vivo.

Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity.

Pipequaline (PK-8165) is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely related to other drugs of this type. The drug has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and very little sedative, amnestic or anticonvulsant effects, and so is classified as a nonbenzodiazepine anxiolytic.

T16A(inh)-C01 is the Ca(2+)-activated Cl(-) Channel, Ano1 class C inhibitor.

CMPDA is a positive allosteric modulator of AMPA receptors [EC50s: 45.4 nM/63.4 nM for GluA2i/GluA2o receptor].

TRPP3 channel inhibitor

Fostedil enhances heart function, maintains blood flow during partial/total coronary occlusions, and lowers aortic pressure.

Bumetanide sodium, a potent diuretic, blocks NKCC1 (IC50: 0.68 μM) and NKCC2 (IC50: 4.0 μM).

<p>VMAT2-IN-2 tosylate is a potent inhibitor of VMAT2 and is applicable in the research of tardive dyskinesia [1].</p>

<p>LFS-1107, a reversible CRM1 inhibitor (Kd: 12.5 pM), selectively targets and eliminates ENKTL cells, offering potential for cancer research applications [1].</p>

UBP310 (UBP 310) is a GLUK5 kainate receptor antagonist

Belfosdil is a blocker of antihypertensive calcium channel.

CGP 56999A is a GABA(B) receptor antagonist; it boosts BDNF and reduces dopamine loss in rat striatum.

<p>Xilmenolone acts as a positive allosteric modulator of the GABA_A receptor [1].</p>

HMR 1556 is a chromanol derivative and is an IKs blocker (IC50s of 10.5 nM and 34 nM in canine and guinea pig left ventricular myocytes, respectively).