Transporteur membranaire/Canal ionique

4alpha-PDD activates transient receptor potential vanilloid 4 (TRPV4) channels and is inactive for signaling through PKC.

DS88790512, IC50 at 11 nM, is an effective, selective, oral bioeffective TRPC6 inhibitor.

hURAT1 inhibitor 2 (Compound 5) is an inhibitor of hURAT1 (uric acid transporter 1, SLC22A12) with an IC50 of 18 nM. It also exhibits some inhibitory activity against OATP1B1, with an IC50 of 0.73 μM. hURAT1 inhibitor 2 can be used in research related to hyperuricemia, gout, and other diseases associated with abnormal uric acid metabolism.

Kv3 modulator 5 (Example 5), a Kv3 channel modulator, enhances the Kv3.2 current and may be employed in research of hearing disorders [1].

TRPC4/5-IN-1, a TRPC5/4 inhibitor with IC50s 0.54 μM/2.06 μM, targets skin inflammation and proteinuric kidney diseases.

KPH2f: dual URAT1/GLUT9 inhibitor, orally active, IC50: 0.24μM (URAT1), 9.37μM (GLUT9), minimal OAT1/ABCG2 impact.

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.

(RS)-AMPA monohydrate, potent glutamate analogue, selectively activates L-glutamic acid without affecting kainic acid or NMDA receptors.

8-Prenylchrysin is a C8-isopentenyl flavonoid compound. It acts as an inhibitor of P-glycoprotein (P-gp) and can be utilized in cancer research.

URAT1-IN-14 is a potent and orally active inhibitor of uric acid transporter 1 (URAT1). It demonstrates an IC50 value of 0.72 μM for inhibiting human URAT1 in HEK293 cells and exhibits low cytotoxicity in Hep-G2 cells. URAT1-IN-14 reduces uric acid levels in a hyperuricemia mouse model and is applicable in research on hyperuricemia and gout.

INCB-056868 is the metabolite M11 of Epacadostat. It serves as a substrate for BCRP and holds potential for use in the study of metabolic diseases.

Unoprostone isopropyl, a prostanoid and synthetic docosanoid, is approved for the treatment of ocular hypertension and open-angle glaucoma.

<p>KV1.3-IN-2 (Compound I) selectively inhibits the kv1.3 potassium channel without affecting the hERG channel. It is applicable in research related to immune-associated diseases such as psoriasis, rheumatoid arthritis, and systemic lupus erythematosus.</p>

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.

Vormatrigine effectively inhibits sodium channels (sodium channel).

ELP-004 is a TRPC channel inhibitor that blocks Ca2+ entry mediated by TRPC channels. It serves as an osteoclast inhibitor by preventing osteoclast differentiation. ELP-004 also hinders basal Ca2+ levels and the associated translocation of NFATc1 in inflammatory osteoclastogenesis. Additionally, it reduces bone erosion in mouse models of rheumatoid arthritis.

Cyproflanilide is a GABAR antagonist that exhibits high activity against a variety of pests, including those from the Lepidoptera, Coleoptera, and Thysanoptera orders.

(R)-Duloxetine, an isomer of Duloxetine, induces tonic and use-dependent blockade of neuronal Na+ channels. This compound is utilized in pain research.

P-gp modulator 1 is a high affinity and orally available P-glycoprotein (Pgp) modulator

<p>TP003 is a novel non-selective GABAA receptor benzodiazepine site agonist with affinity for α1β2gam2, α2β3gam2, α3β3gam2, α5β2gam2, EC50 of 20.3, 10.6, 3.24, 5.</p>

P-gp modulator 3 (Compound 37) is a potent, competitive, metabotropic P-glycoprotein (P-gp) modulator.

NSC73306 is a thiosemicarbazone known for its role as a cell-permeable agent, exhibiting increased toxicity towards cells expressing p-glycoprotein.

DAD dichloride is a 3rd-gen photoelectric switch, blocks K+ channels, and helps in visual function research.

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

Opakalim is an activator of potassium channels (potassium channel) and exhibits anticonvulsant activity.

Thiomuscimol hydrobromide is an agonist of GABAA receptor.

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.

DAD is an ion channel blocker (blocks voltage-gated potassium channels) and is a third generation photoelectric switch that responds to visible light.

DL-AP5 (2-APV) lithium is a competitive antagonist of the NMDA (N-Methyl-D-aspartate) receptor. It exhibits notable analgesic activity and specifically blocks channels in the rabbit retina.

Compound 3e, a potent GABAA agonist, targets GABA sites and has potential anti-depressive effects in mice.

P-gp/BCRP-IN-1, safe and oral, inhibits P-gp/BCRP transporters, enhancing Paclitaxel bioavailability.

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.

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

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 。

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 .

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

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.

<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>

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.

(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].

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.

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

Dexivacaine is an type of anesthetic.

Indoxacarb is an Oxadiazine insecticide.

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].

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

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]

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

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

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

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.

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

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

CGP 44532 a GABAB receptor agonist.

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

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

TRPP3 channel inhibitor

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

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

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.

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

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.

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

UBP310 (UBP 310) is a GLUK5 kainate receptor antagonist

<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>

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

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

Belfosdil is a blocker of antihypertensive calcium channel.

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

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).

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