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GABA Receptor

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Cat. No. Product Name Field of Application Chemical Structure
DC81643 TIPARP-IN-1
TIPARP-IN-1 (Compound 15) is a selective PARP7 (TIPARP) (2,3,7,8-Tetrachlorodiben-zo-p-dioxin(TCDD)-inducible PARP) inhibitor with an IC50 of 2.15 nM. TIPARP-IN-1 can restore IFN signaling pathway in tumors by inhibiting TIPARP. TIPARP-IN-1 selectively activates the anti-tumor immune response in the tumor microenvironment and avoids the production of systemic cytokines. TIPARP-IN-1 can be used for research of head and neck squamous cell carcinoma.
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DC81138 Necopidem
Necopidem (Compound 6) is a GABA A receptor modulator. Necopidem can be used in research on neurological disorders such as anxiety.
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DC80251 AR ligand-48
AR ligand-48 is an AR (Androgen Receptor) inhibitor and a ligand for the target protein for PROTAC (AR). AR ligand-48 can be used to synthesize PROTAC AR Degrader-12.
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DC80136 A-837093 sodium
A-837093 sodium is a potent and orally active inhibitor of the hepatitis C virus (HCV) nonstructural protein 5B (NS5B) polymerase. A-837093 sodium shows potencies against polymerases derived from both HCV genotypes 1a (IC50 = 1.25 nM) and 1b (IC50 = 0.33 nM). A-837093 sodium exhibits antiviral efficacy in HCV-infected chimpanzees. A-837093 sodium can be used for HCV infection research.
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DC80055 3-Amino-5-hydroxybenzoic acid-13C
3-Amino-5-hydroxybenzoic acid-13C is the 13C-labeled 3-Amino-5-hydroxybenzoic acid. 3-Amino-5-hydroxybenzoic acid is a biosynthetic precursor of the mC7N unit of ansamycin antibiotics, including ansatrienin A and geldanamycin, as well as the antitumor antibiotic mitomycin C. 3-Amino-5-hydroxybenzoic acid may be an early intermediate in the shikimic acid pathway from glucose.
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DC79563 (S)-Padsevonil
(S)-Padsevonil is the S-enantiomer of Padsevonil).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.
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DC79562 RO-488684
RO-488684 is a benzodiazepine receptor agonist. RO-488684 can be used for research on sleep and conscious sedation.
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DC79541 CGS-17867A hydrochloride
CGS-17867A (hydrochloride) is a benzodiazepine receptor ligand. CGS-17867A (hydrochloride) has a weak sedative effect and can increase palatable food intake.
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DC79478 Ro 17-1812
Ro 17-1812 is a benzodiazepine receptor partial agonist with anticonvulsant effect.
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DC79471 RP-60503
RP-60503 is an orally active anxiolytic cyclopyrrolone derivative with low sedative potential. RP-60503 binds to the gamma-aminobutyric acidA (GABA)/benzodiazepine receptor with a Ki value of 1.16 nM. RP-60503 can be used for the research of neurological disease.
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DC79232 HDZI 2,4OH
HDZI 2,4OH exerts significant anti anxiety activity through GABA receptors. HDZI 2,4OH can penetrate the blood-brain barrier. HDZI 2,4OH exhibits low toxicity in zebrafish. HDZI 2,4OH can be used for research on neurological disorders such as anxiety disorders.
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DC79208 AHN 070
AHN 070 is an irreversible peripheral benzodiazepine receptor (PBR) ligand. AHN 070 can bind to PBR with nanomolar affinity and is pH-dependent. AHN 070 can be used for studying the structure and function of PBR.
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DC78784 Aminochalcone 4AAF
Aminochalcone 4AAF is a neuroprotective agent that exerts anxiolytic effects through GABAA and 5-HT receptors. Aminochalcone 4AAF has high selectivity for 5-HT3A and 5-HT2C receptors, and stimulates allosteric behavior toward the 5-HT2A receptor. Aminochalcone 4AAF shows hypoglycemic effects and reduces the level of ROS in the liver. Aminochalcone 4AAF delays the clonic stage of the epileptic seizures . Aminochalcone 4AAF can be used in the study of anxiety, hyperglycemia, and seizures.
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DC78093 Lorotomidate
Lorotomidate (Example 16) is a GABAA receptor agonist. Lorotomidate has anaesthetic effects (ED50: i.v., 2 mg/kg in KM mice; LD50: 46.5 mg/kg in KM mice). Lorotomidate has no inhibitory effect on the secretion of corticosteroids in animals, and thus has good safety.
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DC78074 4''-Oxoavermectin B1a
4''-Oxoavermectin B1a is a potentiator targeting GABA (γ-aminobutyric acid) and glutamate-gated chloride channels with insecticidal and acaricidal activities. 4''-Oxoavermectin B1a is promising for research of agricultural pests.
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DC78063 Cholesteryl γ-aminobutyrate
Cholesteryl γ-aminobutyrate is a γ-aminobutyric acid (GABA)-mimetic prodrug. Cholesteryl γ-aminobutyrate inhibits the orthodromically-evoked discharge of pyramidal cells in the CA1 region of the hippocampus. Cholesteryl γ-aminobutyrate suppresses the open-field activity of mice and rats in a dose-dependent manner and inhibits Bicuculline-induced seizures in mice. Cholesteryl γ-aminobutyrate can be used for the study of CNS diseases related to impaired GABAergic neuronal function.
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DC76761 β-CCM
β-CCM is a benzodiazepine receptor inverse agonist with anxiogenic and proconvulsant effects. β-CCM enhances emotional reactivity and reduces vulnerability to interference in spatial working memory tasks. β-CCM can be used for research on anxiety-related disorders.
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DC76760 TET-13
TET-13 is a positive allosteric modulator of GABAA receptor with an EC50 of 5.65 μM, lower than that of Etomidate (EC50: 9.29 μM). TET-13 shows potent anesthetic effects in both mice and rats (ED50: 0.48 mg/kg and 0.69 mg/kg, respectively).
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DC76759 SKF 10810
SKF 10810 is a GABAA receptor antagonist with an EC50 of 4.3 μM. By blocking GABAergic inhibition of the brain's reward pathways, SKF 10810 may exert antidepressant effects. SKF 10810 can be used for research in neurological disorders.
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DC76758 Rilmazolam
Rilmazolam, a triazolobenzodiazepine, is an active metabolite of Rilmazafone. NSC687852 (b-AP1
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DC76757 Refisolone
Refisolone is an antagonist of the GABAA receptor.
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DC76756 Moxetomidate
Moxetomidate is a GABAA receptor agonist with hypnotic effect.
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DC76755 MIDD0301 sodium
MIDD0301 (GL-II-93) is an orally available, active γ-aminobutyric acid type A receptor (GABAAR) inhibitor and anti-asthmatic agent. MIDD0301 exhibits biological and immunotoxicological safety in mice and does not affect the number of circulating lymphocytes, monocytes, and granulocytes. MIDD0301 has no significant adverse immune response at repeated doses, which is better than Prednisone. MIDD0301 relaxes histamine-contracted guinea pig and human airway smooth muscle and is used in the study of bronchoconstrictive diseases.
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DC76754 Inidascamine
Inidascamine is the modulator for cholinergic, glutamatergic, and GABAB receptor, and can be used for researchs of schizophrenia.
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DC76753 ENX-101
ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models.
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DC76752 Delta3,5-cholestadien-7-one
Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC50 values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.
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DC76751 CMPPE
CMPPE is a GABAB receptor positive allosteric modulator (PAM) that inhibits alcohol self-administration and reinstatement behavior in rats.
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DC76750 Cinazepam
Cinazepam is a partial GABAA receptor agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders.
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DC76749 Ciclotizolam
Ciclotizolam (WE-973) is a thienotriazolodiazepine with anticonvulsant and anti-aggressive activities. Ciclotizolam binds to benzodiazepine receptors in the central nervous system. Ciclotizolam decreases total sleep time in cats.
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DC76748 3-Hydroxy desalkylflurazepam
3-Hydroxy desalkylflurazepam is a benzodiazepine with potential sedative and anxiolytic effects.
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