Catalog No.
Product Name
Application
Product Information
Citations
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CXCR4 antagonist
IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. -
δ-opioid receptor modulator
BMS-986188 is a novel Potent and Selective Positive Allosteric Modulator of the delta-Opioid Receptor. -
δ-opioid receptor modulator
BMS-986187 is a potent and selective positive allosteric modulator (PAM) of the δ-opioid receptor and a G-protein-biased allosteric agonist. -
bovine tubulin oxidation inhibitor
Takeda103A is a potent GRK2-dependent bovine tubulin oxidation inhibitor. -
histamine H1 receptor antagonist
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. -
antiplatelet activities
6-Methoxydihydroavicine is an alkaloid isolated from Zanthoxylum integrifoliolum. 6-Methoxydihydroavicine has antiplatelet activities and inhibits AA-, collagen- and PAF-induced platelet aggregation in vitro. -
A1 adenosine receptor agonist
Adenosine amine congener (ADAC) is a selective A1 adenosine receptor agonist, can ameliorate noise- and Cisplatin-induced cochlear injury. - SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties.
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β-adrenergic receptor (βAR) antagonist
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively.
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histamine H3R antagonist/inverse agonist
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. -
5-HT3 receptor antagonist
5-HT3 antagonist-4i is a 5-HT3 receptor antagonist which modulates the serotonergic system. -
CXCR4 antagonist
Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ??1 nM. -
analgesic agent
Tetrahydropalmatine hydrochloride (DL-Tetrahydropalmatine hydrochloride), an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats. -
leukotriene B4 receptor antagonist
Etalocib, also known as LY293111 and VML295, is a potent and selective inhibitor of the lipoxygenase pathway either directly through 5'-lipoxygenase or via antagonism of the leukotriene B4 (LTB4) receptor. -
melanocortin receptor (MR) agonist
AP1189 is a biased agonist at receptors MC1 and MC3. AP1189 reduced cytokine release, an effect reliant on both MC1 and MC3 as evident from the use of Mc1r(-/-) and Mc3r(-/-) macrophages. -
GLP-1R agonist
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor agonist (GLP-1R) -
5-HT4 receptor partial agonist
PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg. -
5-HT7 receptor antagonist
AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders. -
5-HT receptor agonist
MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively). -
VPAC2 agonist
Bay 55-9837 is a potent and highly selective agonist of VPAC2, with a Kd of 0.65 nM. Bay 55-9837 may be a useful therapy for the research of type 2 diabetes. -
Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research.
- MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
- CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) has anti-obesity effect.
- N-acetyl CCK-(26-30) amide (CCK-(26-30) (sulfated)) is a cholecystokinin (CCK) receptor antagonist.
- CCK (26-31) (non-sulfated) is the N-terminal fragment of CCK, a peptide hormone found in the gut and brain that stimulates digestion, regulates satiety, and is associated with anxiety. CCK (26-31) is also less active in non-sulfated than in sulfated form.
- Urocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) selectively binds to type 2 CRF receptors with Ki values of 13.5, 21.7, and >100 nM for mCRF2β, rCRF2α, and hCRF1, respectively. Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) secretion.
- Somatostatin-28 (sheep, human rat mouse) is a biologically active polypeptide, synthesised in the proximal intestinal epithelial cells. Somatostatin-28 (sheep, human rat mouse) suppresses glucose-stimulated insulin secretion without affecting circulating basal insulin concentration. Somatostatin-28 (sheep, human rat mouse) also targets to somatostatin receptor subtype 5 (SSTR5) to regulate GLP-1 secretion.
- DOTA-LM3 is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 and 68 Ga-DOTA-LM3. 68 Ga-DOTA-LM3 shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis.
- Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury.
