GPCR/G Protein

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Items 101-150 of 322

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Catalog No.
Product Name
Application
Product Information
Product Citation
  1. H3R antagonist/TRPV1 antagonist

    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
  2. 5-HT6 antagonist

    SB 399885 hydrochloride is a potent, brain penetrant, and orally active SR-6 antagonist. It displays > 200-fold selectivity for SR-6 over other serotonin receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human SR-6 receptors, respectively).
  3. CRF1 receptor antagonist

    Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1??0.6 nM for human CRF1 receptor.
  4. JWH 250 is a cannabimimetic indole that shows a high-affinity for both the central cannabinoid (CB1) and the peripheral cannabinoid (CB2) receptors
  5. JWH 370 is a (1-naphthoyl)pyrrole analog of JWH 018 that potently activates both CB1 and CB2 receptors (Ki values of 5.6 and 4.0 nM, respectively)
  6. JWH 249 is a synthetic cannabinoid (CB) that potently activates the central CB1 and peripheral CB2 receptors (Ki = 8.4 and 20 nM, respectively).
  7. cannabinoid agonist

    JWH 307 is a (1-naphthoyl)pyrrole cannabimimetic that potently activates both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors (Ki values of 7.7 and 3.3 nM, respectively).
  8. AM1220 is a potent synthetic cannabinoid (CB) with preference for the central CB1 receptor (Ki = 3.88 nM) over the CB2 receptor (Ki = 73.4 nM).
  9. AM2233 is a full agonist of the central cannabinoid (CB1) receptor (Ki = 2.8 nM).
  10. κ1-opioid receptor agonist

    U-69593 is a potent, selective κ1-opioid receptor agonist (EC50 = 80-109 nM). Active in vivo. Antinociceptive.
  11. OX1/OX2 Antagonist

    Almorexant HCl is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor 3.
  12. mGluR-2 modulator

    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.
  13. peptide Oxytocin Receptor Inhibitor

    Atosiban is a peptide Oxytocin Receptor Inhibitor.
  14. Adenosine A3-R agonist

    IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nM for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively.
  15. 5-HT6 receptor antagonist

    LuAE58054 is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia.
  16. ETBR antagonist

    BQ-788 sodium salt is a selective ETBR (Endothelin receptor B ) antagonist.
  17. Dopamine receptor agonist

    (+)-PD 128907 hydrochloride is a potent D3DR (dopamine receptor) agonist (Ki = 2.3 nM).
  18. serotonin/NE reuptake inhibitor

    Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.
  19. Corticotropin Releasing Factor, bovine, neurotransmitter and CRF receptor antagonist.
  20. Endothelin-2, human, endogenous peptide found predominately in the kidney and intestine. Displays similar selectivity for ETA and ETB endothelin receptors.
  21. μ-opioid receptor agonist

    Alvimopan dihydrate(LY 246736, ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  22. μ-opioid receptor agonist

    Alvimopan monohydrate is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  23. CXCR4 antagonist

    AMD-070 hydrochloride is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
  24. adrenergic receptor/5-HT receptor inhibitor

    Asenapine hydrochloride inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
  25. H3 receptor antagonist

    Bavisant dihydrochloride is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.
  26. H3 receptor antagonist

    Bavisant dihydrochloride hydrate is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.
  27. D3/D2 Dopamine Receptor Antagonist

    Cariprazine hydrochloride is a novel antipsychotic drug candidate that exhibits high selectivity and affinity to dopamine D3(Ki=0.09 nM) and D2 (Ki=0.5 nM) receptors and moderate affinity to serotonin 5-HT(1A) receptors.
  28. GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 (GPR120).
  29. GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 (GPR120).
  30. Metabolites of tulobuterol

    HOKU-81, a new bronchodilator, is one of the metabolites of tulobuterol.
  31. k-opioid receptor antagonist

    LY2795050 is a novel selective κ-opioid Receptor (KOR) antagonist (IC50=0.72 nM) and has the potential as a PET tracer to image KOR in vivo.
  32. CGRP Receptor antagonist

    MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.
  33. NK1 receptor antagonist

    NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.
  34. CB1 receptor antagonist

    Otenabant is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.
  35. Dopamine reuptake inhibitor

    Phenylpiracetam is a phenylated derivative of the nootropic drug piracetam. It is used as a stimulant nootropic drug that can be up to 30-60 times more potent than piracetam.
  36. CXCL8 receptor inhibitor

    Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models.
  37. NK3 receptor antagonist

    SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier.
  38. NK3 receptor antagonist

    Talnetant is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.
  39. NK3 receptor antagonist

    Talnetant Hcl is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.
  40. 5HT1A antagonist

    WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 - 0.12 nM for 5-HT.
  41. LPA2 agonist

    GRI 977143, selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 uM).
  42. 5-HT Receptor Antagonist

    SB271046 is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.
  43. CXCL chemokines antagonist

    UNBS5162 is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers; the mean antiproliferative activity IC50 value is 17.9 uM for 9 cancer cell lines; hydrolysis product of UNBS3157.
  44. 5-HT3 receptor antagonist

    Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor.
  45. 5-HT3 antagonist

    LY278584 is a potent and selective antagonist of 5-HT3 receptors. LY278584 is a useful ligand for studying the localization of 5-HT3 receptors in rat brain
  46. 5HT3 receptor antagonist

    Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity.
  47. NA reuptake inhibitor

    MCI-225 is a selective NA reuptake inhibitor with 5-HT3 receptor antagonism.
  48. 5-HT4 receptor antagonist

    Piboserod is a selective 5-HT(4) receptor antagonist.
  49. vasopressin V1 antagonist

    OPC21268 is a non-peptide AVP Receptor V (Vasopressin Receptor) antagonist that shows 1000-fold selectivity for V1 receptors over V2 receptors.
  50. mGlu2 receptor modulator

    CBiPES hydrochloride is a selective positive allosteric modulator of the mGluR-2 with IC50 value of 98.2 nM

Items 101-150 of 322

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